Publication
1: Gessi S, Poloni TE, Negro G, Varani K, Pasquini S, Vincenzi F, Borea PA,
Merighi S. A<sub>2A</sub> Adenosine Receptor as a Potential Biomarker and a
Possible Therapeutic Target in Alzheimer's Disease. Cells. 2021 Sep
7;10(9):2344. doi: 10.3390/cells10092344. PMID: 34571993; PMCID: PMC8469578.
2: Capone F, Salati S, Vincenzi F, Liberti M, Aicardi G, Apollonio F, Varani K,
Cadossi R, Di Lazzaro V. Pulsed Electromagnetic Fields: A Novel Attractive
Therapeutic Opportunity for Neuroprotection After Acute Cerebral Ischemia.
Neuromodulation. 2021 Sep 4. doi: 10.1111/ner.13489. Epub ahead of print. PMID:
34480781.
3: Pasquini S, Contri C, Borea PA, Vincenzi F, Varani K. Adenosine and
Inflammation: Here, There and Everywhere. Int J Mol Sci. 2021 Jul
19;22(14):7685. doi: 10.3390/ijms22147685. PMID: 34299305; PMCID: PMC8304851.
4: Viaro R, Longo F, Vincenzi F, Varani K, Morari M. l-DOPA promotes striatal
dopamine release through D1 receptors and reversal of dopamine transporter.
Brain Res. 2021 Oct 1;1768:147583. doi: 10.1016/j.brainres.2021.147583. Epub
2021 Jul 17. PMID: 34284020.
5: Merighi S, Poloni TE, Pelloni L, Pasquini S, Varani K, Vincenzi F, Borea PA,
Gessi S. An Open Question: Is the A<sub>2A</sub> Adenosine Receptor a Novel
Target for Alzheimer's Disease Treatment? Front Pharmacol. 2021 Mar
22;12:652455. doi: 10.3389/fphar.2021.652455. PMID: 33828485; PMCID: PMC8019913.
6: Merighi S, Battistello E, Casetta I, Gragnaniello D, Poloni TE, Medici V,
Cirrincione A, Varani K, Vincenzi F, Borea PA, Gessi S. Upregulation of Cortical
A2A Adenosine Receptors Is Reflected in Platelets of Patients with Alzheimer's
Disease. J Alzheimers Dis. 2021;80(3):1105-1117. doi: 10.3233/JAD-201437. PMID:
33646165.
7: Ferrante A, Boussadia Z, Borreca A, Mallozzi C, Pedini G, Pacini L, Pezzola
A, Armida M, Vincenzi F, Varani K, Bagni C, Popoli P, Martire A. Adenosine
A<sub>2A</sub> receptor inhibition reduces synaptic and cognitive hippocampal
alterations in Fmr1 KO mice. Transl Psychiatry. 2021 Feb 5;11(1):112. doi:
10.1038/s41398-021-01238-5. PMID: 33547274; PMCID: PMC7864914.
8: Varani K, Vincenzi F, Pasquini S, Blo I, Salati S, Cadossi M, De Mattei M.
Pulsed Electromagnetic Field Stimulation in Osteogenesis and Chondrogenesis:
Signaling Pathways and Therapeutic Implications. Int J Mol Sci. 2021 Jan
15;22(2):809. doi: 10.3390/ijms22020809. PMID: 33467447; PMCID: PMC7830993.
9: Vincenzi F, Pasquini S, Battistello E, Merighi S, Gessi S, Borea PA, Varani
K. A<sub>1</sub> Adenosine Receptor Partial Agonists and Allosteric Modulators:
Advancing Toward the Clinic? Front Pharmacol. 2020 Dec 9;11:625134. doi:
10.3389/fphar.2020.625134. PMID: 33362567; PMCID: PMC7756085.
10: Vincenzi F, Pasquini S, Borea PA, Varani K. Targeting Adenosine Receptors: A
Potential Pharmacological Avenue for Acute and Chronic Pain. Int J Mol Sci. 2020
Nov 18;21(22):8710. doi: 10.3390/ijms21228710. PMID: 33218074; PMCID:
PMC7698931.
11: Vincenzi F, Pasquini S, Setti S, Salati S, Cadossi R, Borea PA, Varani K.
Pulsed Electromagnetic Fields Stimulate HIF-1α-Independent VEGF Release in
1321N1 Human Astrocytes Protecting Neuron-Like SH-SY5Y Cells from Oxygen-Glucose
Deprivation. Int J Mol Sci. 2020 Oct 28;21(21):8053. doi: 10.3390/ijms21218053.
PMID: 33126773; PMCID: PMC7663527.
12: Colombini A, Perucca Orfei C, Vincenzi F, De Luca P, Ragni E, Viganò M,
Setti S, Varani K, de Girolamo L. A2A adenosine receptors are involved in the
reparative response of tendon cells to pulsed electromagnetic fields. PLoS One.
2020 Sep 30;15(9):e0239807. doi: 10.1371/journal.pone.0239807. PMID: 32998161;
PMCID: PMC7527253.
13: Varano F, Catarzi D, Vigiani E, Vincenzi F, Pasquini S, Varani K, Colotta V.
Piperazine- and Piperidine-Containing Thiazolo[5,4-<i>d</i>]pyrimidine
Derivatives as New Potent and Selective Adenosine A<sub>2A</sub> Receptor
Inverse Agonists. Pharmaceuticals (Basel). 2020 Jul 24;13(8):161. doi:
10.3390/ph13080161. PMID: 32722122; PMCID: PMC7465344.
14: Navarro G, Varani K, Lillo A, Vincenzi F, Rivas-Santisteban R, Raïch I,
Reyes-Resina I, Ferreiro-Vera C, Borea PA, Sánchez de Medina V, Nadal X, Franco
R. Pharmacological data of cannabidiol- and cannabigerol-type phytocannabinoids
acting on cannabinoid CB<sub>1</sub>, CB<sub>2</sub> and
CB<sub>1</sub>/CB<sub>2</sub> heteromer receptors. Pharmacol Res. 2020
Sep;159:104940. doi: 10.1016/j.phrs.2020.104940. Epub 2020 May 26. PMID:
32470563.
15: Vincenzi F, Pasquini S, Gessi S, Merighi S, Romagnoli R, Borea PA, Varani K.
The Detrimental Action of Adenosine on Glutamate-Induced Cytotoxicity in PC12
Cells Can Be Shifted towards a Neuroprotective Role through A<sub>1</sub>AR
Positive Allosteric Modulation. Cells. 2020 May 18;9(5):1242. doi:
10.3390/cells9051242. PMID: 32443448; PMCID: PMC7290574.
16: Pasquini S, Vincenzi F, Casetta I, Laudisi M, Merighi S, Gessi S, Borea PA,
Varani K. Adenosinergic System Involvement in Ischemic Stroke Patients'
Lymphocytes. Cells. 2020 Apr 25;9(5):1072. doi: 10.3390/cells9051072. PMID:
32344922; PMCID: PMC7290971.
17: Varano F, Catarzi D, Vincenzi F, Pasquini S, Pelletier J, Lopes Rangel
Fietto J, Espindola Gelsleichter N, Sarlandie M, Guilbaud A, Sévigny J, Varani
K, Colotta V. Structural investigation on thiazolo[5,4-d]pyrimidines to obtain
dual-acting blockers of CD73 and adenosine A<sub>2A</sub> receptor as potential
antitumor agents. Bioorg Med Chem Lett. 2020 May 1;30(9):127067. doi:
10.1016/j.bmcl.2020.127067. Epub 2020 Feb 29. PMID: 32165041.
18: Catarzi D, Varano F, Varani K, Vincenzi F, Pasquini S, Dal Ben D, Volpini R,
Colotta V. Amino-3,5-Dicyanopyridines Targeting the Adenosine Receptors Ranging
from Pan Ligands to Combined A<sub>1</sub>/A<sub>2B</sub> Partial Agonists.
Pharmaceuticals (Basel). 2019 Oct 22;12(4):159. doi: 10.3390/ph12040159. PMID:
31652622; PMCID: PMC6958422.
19: Merighi S, Gessi S, Bencivenni S, Battistello E, Vincenzi F, Setti S,
Cadossi M, Borea PA, Cadossi R, Varani K. Signaling pathways involved in anti-
inflammatory effects of Pulsed Electromagnetic Field in microglial cells.
Cytokine. 2020 Jan;125:154777. doi: 10.1016/j.cyto.2019.154777. Epub 2019 Aug 7.
PMID: 31400640.
20: Betti M, Catarzi D, Varano F, Falsini M, Varani K, Vincenzi F, Pasquini S,
di Cesare Mannelli L, Ghelardini C, Lucarini E, Dal Ben D, Spinaci A, Bartolucci
G, Menicatti M, Colotta V. Modifications on the Amino-3,5-dicyanopyridine Core
To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.
J Med Chem. 2019 Aug 8;62(15):6894-6912. doi: 10.1021/acs.jmedchem.9b00106. Epub
2019 Jul 26. PMID: 31306001.
21: Merighi S, Battistello E, Giacomelli L, Varani K, Vincenzi F, Borea PA,
Gessi S. Targeting A3 and A2A adenosine receptors in the fight against cancer.
Expert Opin Ther Targets. 2019 Aug;23(8):669-678. doi:
10.1080/14728222.2019.1630380. Epub 2019 Jun 12. PMID: 31189400.
22: Gessi S, Merighi S, Bencivenni S, Battistello E, Vincenzi F, Setti S,
Cadossi M, Borea PA, Cadossi R, Varani K. Pulsed electromagnetic field and
relief of hypoxia-induced neuronal cell death: The signaling pathway. J Cell
Physiol. 2019 Jan 17. doi: 10.1002/jcp.28149. Epub ahead of print. PMID:
30656694.
23: Navarro G, Varani K, Reyes-Resina I, Sánchez de Medina V, Rivas-Santisteban
R, Sánchez-Carnerero Callado C, Vincenzi F, Casano S, Ferreiro-Vera C, Canela
EI, Borea PA, Nadal X, Franco R. Cannabigerol Action at Cannabinoid
CB<sub>1</sub> and CB<sub>2</sub> Receptors and at CB<sub>1</sub>-CB<sub>2</sub>
Heteroreceptor Complexes. Front Pharmacol. 2018 Jun 21;9:632. doi:
10.3389/fphar.2018.00632. PMID: 29977202; PMCID: PMC6021502.
24: Varano F, Catarzi D, Vincenzi F, Falsini M, Pasquini S, Borea PA, Colotta V,
Varani K. Structure-activity relationship studies and pharmacological
characterization of N<sup>5</sup>-heteroarylalkyl-
substituted-2-(2-furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine-based derivatives
as inverse agonists at human A<sub>2A</sub> adenosine receptor. Eur J Med Chem.
2018 Jul 15;155:552-561. doi: 10.1016/j.ejmech.2018.06.020. Epub 2018 Jun 9.
PMID: 29909340.
25: Varano F, Catarzi D, Falsini M, Vincenzi F, Pasquini S, Varani K, Colotta V.
Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human
A<sub>1</sub> and A<sub>2A</sub> adenosine receptor antagonists/inverse
agonists. Bioorg Med Chem. 2018 Jul 23;26(12):3688-3695. doi:
10.1016/j.bmc.2018.05.048. Epub 2018 May 31. PMID: 29880250.
26: Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of
Adenosine Receptors: The State of the Art. Physiol Rev. 2018 Jul
1;98(3):1591-1625. doi: 10.1152/physrev.00049.2017. PMID: 29848236.
27: Catarzi D, Varano F, Falsini M, Varani K, Vincenzi F, Pasquini S, Dal Ben D,
Colotta V. Development of novel pyridazinone-based adenosine receptor ligands.
Bioorg Med Chem Lett. 2018 May 15;28(9):1484-1489. doi:
10.1016/j.bmcl.2018.03.086. Epub 2018 Mar 30. PMID: 29627261.
28: Betti M, Catarzi D, Varano F, Falsini M, Varani K, Vincenzi F, Dal Ben D,
Lambertucci C, Colotta V. The aminopyridine-3,5-dicarbonitrile core for the
design of new non-nucleoside-like agonists of the human adenosine A<sub>2B</sub>
receptor. Eur J Med Chem. 2018 Apr 25;150:127-139. doi:
10.1016/j.ejmech.2018.02.081. Epub 2018 Mar 6. PMID: 29525433.
29: Gessi S, Bencivenni S, Battistello E, Vincenzi F, Colotta V, Catarzi D,
Varano F, Merighi S, Borea PA, Varani K. Inhibition of A<sub>2A</sub> Adenosine
Receptor Signaling in Cancer Cells Proliferation by the Novel Antagonist TP455.
Front Pharmacol. 2017 Dec 1;8:888. doi: 10.3389/fphar.2017.00888. PMID:
29249971; PMCID: PMC5716981.
30: Martínez-Pinilla E, Varani K, Reyes-Resina I, Angelats E, Vincenzi F,
Ferreiro-Vera C, Oyarzabal J, Canela EI, Lanciego JL, Nadal X, Navarro G, Borea
PA, Franco R. Binding and Signaling Studies Disclose a Potential Allosteric Site
for Cannabidiol in Cannabinoid CB<sub>2</sub> Receptors. Front Pharmacol. 2017
Oct 23;8:744. doi: 10.3389/fphar.2017.00744. PMID: 29109685; PMCID: PMC5660261.
31: Ossato A, Uccelli L, Bilel S, Canazza I, Di Domenico G, Pasquali M, Pupillo
G, De Luca MA, Boschi A, Vincenzi F, Rimondo C, Beggiato S, Ferraro L, Varani K,
Borea PA, Serpelloni G, De-Giorgio F, Marti M. Psychostimulant Effect of the
Synthetic Cannabinoid JWH-018 and AKB48: Behavioral, Neurochemical, and Dopamine
Transporter Scan Imaging Studies in Mice. Front Psychiatry. 2017 Aug 4;8:130.
doi: 10.3389/fpsyt.2017.00130. PMID: 28824464; PMCID: PMC5543288.
32: Tschon M, Veronesi F, Contartese D, Sartori M, Martini L, Vincenzi F, Ravani
A, Varani K, Fini M. Effects of pulsed electromagnetic fields and platelet rich
plasma in preventing osteoclastogenesis in an in vitro model of osteolysis. J
Cell Physiol. 2018 Mar;233(3):2645-2656. doi: 10.1002/jcp.26143. Epub 2017 Sep
4. PMID: 28786478.
33: Varani K, Vincenzi F, Merighi S, Gessi S, Borea PA. Biochemical and
Pharmacological Role of A<sub>1</sub> Adenosine Receptors and Their Modulation
as Novel Therapeutic Strategy. Adv Exp Med Biol. 2017;1051:193-232. doi:
10.1007/5584_2017_61. PMID: 28676923.
34: Canazza I, Ossato A, Vincenzi F, Gregori A, Di Rosa F, Nigro F, Rimessi A,
Pinton P, Varani K, Borea PA, Marti M. Pharmaco-toxicological effects of the
novel third-generation fluorinate synthetic cannabinoids, 5F-ADBINACA, AB-
FUBINACA, and STS-135 in mice. In vitro and in vivo studies. Hum
Psychopharmacol. 2017 May;32(3). doi: 10.1002/hup.2601. Epub 2017 Jun 9. PMID:
28597570.
35: Ravani A, Vincenzi F, Bortoluzzi A, Padovan M, Pasquini S, Gessi S, Merighi
S, Borea PA, Govoni M, Varani K. Role and Function of A<sub>2A</sub> and A₃
Adenosine Receptors in Patients with Ankylosing Spondylitis, Psoriatic Arthritis
and Rheumatoid Arthritis. Int J Mol Sci. 2017 Mar 24;18(4):697. doi:
10.3390/ijms18040697. PMID: 28338619; PMCID: PMC5412283.
36: Longo F, Mercatelli D, Novello S, Arcuri L, Brugnoli A, Vincenzi F, Russo I,
Berti G, Mabrouk OS, Kennedy RT, Shimshek DR, Varani K, Bubacco L, Greggio E,
Morari M. Age-dependent dopamine transporter dysfunction and Serine129 phospho-
α-synuclein overload in G2019S LRRK2 mice. Acta Neuropathol Commun. 2017 Mar
14;5(1):22. doi: 10.1186/s40478-017-0426-8. PMID: 28292328; PMCID: PMC5351259.
37: Varani K, Vincenzi F, Ravani A, Pasquini S, Merighi S, Gessi S, Setti S,
Cadossi M, Borea PA, Cadossi R. Adenosine Receptors as a Biological Pathway for
the Anti-Inflammatory and Beneficial Effects of Low Frequency Low Energy Pulsed
Electromagnetic Fields. Mediators Inflamm. 2017;2017:2740963. doi:
10.1155/2017/2740963. Epub 2017 Feb 1. PMID: 28255202; PMCID: PMC5309410.
38: Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pathological
overproduction: the bad side of adenosine. Br J Pharmacol. 2017
Jul;174(13):1945-1960. doi: 10.1111/bph.13763. Epub 2017 Mar 31. PMID: 28252203;
PMCID: PMC6398520.
39: Squarcialupi L, Betti M, Catarzi D, Varano F, Falsini M, Ravani A, Pasquini
S, Vincenzi F, Salmaso V, Sturlese M, Varani K, Moro S, Colotta V. The role of
5-arylalkylamino- and 5-piperazino- moieties on the
7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A<sub>1</sub> and
A<sub>2A</sub> receptor affinity and selectivity profiles. J Enzyme Inhib Med
Chem. 2017 Dec;32(1):248-263. doi: 10.1080/14756366.2016.1247060. PMID:
28114825; PMCID: PMC6009979.
40: Vincenzi F, Borea PA, Varani K. Anxiolytic properties of A1 adenosine
receptor PAMs. Oncotarget. 2017 Jan 31;8(5):7216-7217. doi:
10.18632/oncotarget.13802. PMID: 28055953; PMCID: PMC5352310.
41: Merighi S, Bencivenni S, Vincenzi F, Varani K, Borea PA, Gessi S.
A<sub>2B</sub> adenosine receptors stimulate IL-6 production in primary murine
microglia through p38 MAPK kinase pathway. Pharmacol Res. 2017 Mar;117:9-19.
doi: 10.1016/j.phrs.2016.11.024. Epub 2016 Dec 11. PMID: 27974241.
42: Varano F, Catarzi D, Vincenzi F, Betti M, Falsini M, Ravani A, Borea PA,
Colotta V, Varani K. Design, Synthesis, and Pharmacological Characterization of
2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly
Potent A<sub>2A</sub> Adenosine Receptor Inverse Agonists with Antinociceptive
Activity. J Med Chem. 2016 Dec 8;59(23):10564-10576. doi:
10.1021/acs.jmedchem.6b01068. Epub 2016 Nov 29. PMID: 27933962.
43: Sartori M, Vincenzi F, Ravani A, Cepollaro S, Martini L, Varani K, Fini M,
Tschon M. RAW 264.7 co-cultured with ultra-high molecular weight polyethylene
particles spontaneously differentiate into osteoclasts: an in vitro model of
periprosthetic osteolysis. J Biomed Mater Res A. 2017 Feb;105(2):510-520. doi:
10.1002/jbm.a.35912. Epub 2016 Nov 3. PMID: 27667508.
44: Poli D, Falsini M, Varano F, Betti M, Varani K, Vincenzi F, Pugliese AM,
Pedata F, Dal Ben D, Thomas A, Palchetti I, Bettazzi F, Catarzi D, Colotta V.
Imidazo[1,2-a]pyrazin-8-amine core for the design of new adenosine receptor
antagonists: Structural exploration to target the A<sub>3</sub> and
A<sub>2A</sub> subtypes. Eur J Med Chem. 2017 Jan 5;125:611-628. doi:
10.1016/j.ejmech.2016.09.076. Epub 2016 Sep 26. PMID: 27721147.
45: Vincenzi F, Ravani A, Pasquini S, Merighi S, Gessi S, Romagnoli R, Baraldi
PG, Borea PA, Varani K. Positive allosteric modulation of A<sub>1</sub>
adenosine receptors as a novel and promising therapeutic strategy for anxiety.
Neuropharmacology. 2016 Dec;111:283-292. doi: 10.1016/j.neuropharm.2016.09.015.
Epub 2016 Sep 14. PMID: 27639989.
46: Vincenzi F, Ravani A, Pasquini S, Merighi S, Gessi S, Setti S, Cadossi R,
Borea PA, Varani K. Pulsed Electromagnetic Field Exposure Reduces Hypoxia and
Inflammation Damage in Neuron-Like and Microglial Cells. J Cell Physiol. 2017
May;232(5):1200-1208. doi: 10.1002/jcp.25606. Epub 2016 Oct 7. PMID: 27639248.
47: Bortoluzzi A, Vincenzi F, Govoni M, Padovan M, Ravani A, Borea PA, Varani K.
A2A adenosine receptor upregulation correlates with disease activity in patients
with systemic lupus erythematosus. Arthritis Res Ther. 2016 Aug 26;18(1):192.
doi: 10.1186/s13075-016-1089-8. PMID: 27566294; PMCID: PMC5002091.
48: Canazza I, Ossato A, Trapella C, Fantinati A, De Luca MA, Margiani G,
Vincenzi F, Rimondo C, Di Rosa F, Gregori A, Varani K, Borea PA, Serpelloni G,
Marti M. Effect of the novel synthetic cannabinoids AKB48 and 5F-AKB48 on
"tetrad", sensorimotor, neurological and neurochemical responses in mice. In
vitro and in vivo pharmacological studies. Psychopharmacology (Berl). 2016
Oct;233(21-22):3685-3709. doi: 10.1007/s00213-016-4402-y. Epub 2016 Aug 15.
PMID: 27527584.
49: Squarcialupi L, Falsini M, Catarzi D, Varano F, Betti M, Varani K, Vincenzi
F, Dal Ben D, Lambertucci C, Volpini R, Colotta V. Exploring the 2- and
5-positions of the pyrazolo[4,3-d]pyrimidin-7-amino scaffold to target human A1
and A2A adenosine receptors. Bioorg Med Chem. 2016 Jun 15;24(12):2794-808. doi:
10.1016/j.bmc.2016.04.048. Epub 2016 Apr 23. PMID: 27161878.
50: Aghazadeh Tabrizi M, Baraldi PG, Ruggiero E, Saponaro G, Baraldi S, Poli G,
Tuccinardi T, Ravani A, Vincenzi F, Borea PA, Varani K. Synthesis and structure
activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2
cannabinoid receptor inverse agonists. Eur J Med Chem. 2016 May 4;113:11-27.
doi: 10.1016/j.ejmech.2016.02.032. Epub 2016 Feb 16. PMID: 26922225.
51: Varani K, Vincenzi F, Targa M, Ravani A, Bastia E, Storoni L, Brambilla S,
Almirante N, Impagnatiello F. Repeated Dosing with NCX1404, a Nitric Oxide-
Donating Pregabalin, Re-establishes Normal Nociceptive Responses in Mice with
Streptozotocin-Induced Painful Diabetic Neuropathy. J Pharmacol Exp Ther. 2016
May;357(2):240-7. doi: 10.1124/jpet.115.230193. Epub 2016 Feb 23. PMID:
26907623.
52: Ossato A, Canazza I, Trapella C, Vincenzi F, De Luca MA, Rimondo C, Varani
K, Borea PA, Serpelloni G, Marti M. Effect of JWH-250, JWH-073 and their
interaction on "tetrad", sensorimotor, neurological and neurochemical responses
in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Jun 3;67:31-50. doi:
10.1016/j.pnpbp.2016.01.007. Epub 2016 Jan 15. PMID: 26780169.
53: Squarcialupi L, Catarzi D, Varano F, Betti M, Falsini M, Vincenzi F, Ravani
A, Ciancetta A, Varani K, Moro S, Colotta V. Structural refinement of
pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective
antagonists for the human A3 adenosine receptor. Eur J Med Chem. 2016 Jan
27;108:117-133. doi: 10.1016/j.ejmech.2015.11.015. Epub 2015 Nov 17. PMID:
26638043.
54: Romagnoli R, Baraldi PG, Lopez-Cara C, Cruz-Lopez O, Moorman AR, Massink A,
IJzerman AP, Vincenzi F, Borea PA, Varani K. Synthesis and biological evaluation
of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric
modulators of the A1 adenosine receptor. A position-dependent effect study. Eur
J Med Chem. 2015 Aug 28;101:185-204. doi: 10.1016/j.ejmech.2015.06.041. Epub
2015 Jun 24. PMID: 26141910.
55: Baraldi PG, Baraldi S, Saponaro G, Aghazadeh Tabrizi M, Romagnoli R,
Ruggiero E, Vincenzi F, Borea PA, Varani K. One-pot reaction to obtain
N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine
scaffold as human A3 adenosine receptor antagonists. J Med Chem. 2015 Jul
9;58(13):5355-60. doi: 10.1021/acs.jmedchem.5b00551. Epub 2015 Jun 17. PMID:
26046697.
56: Varano F, Catarzi D, Squarcialupi L, Betti M, Vincenzi F, Ravani A, Varani
K, Dal Ben D, Thomas A, Volpini R, Colotta V. Exploring the 7-oxo-
thiazolo[5,4-d]pyrimidine core for the design of new human adenosine A3 receptor
antagonists. Synthesis, molecular modeling studies and pharmacological
evaluation. Eur J Med Chem. 2015;96:105-21. doi: 10.1016/j.ejmech.2015.04.010.
Epub 2015 Apr 4. PMID: 25874336.
57: Preti D, Baraldi PG, Saponaro G, Romagnoli R, Aghazadeh Tabrizi M, Baraldi
S, Cosconati S, Bruno A, Novellino E, Vincenzi F, Ravani A, Borea PA, Varani K.
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phen
ylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and
selective agonists of the A2A adenosine receptor. J Med Chem. 2015 Apr
9;58(7):3253-67. doi: 10.1021/acs.jmedchem.5b00215. Epub 2015 Mar 25. PMID:
25780876.
58: Vigolo A, Ossato A, Trapella C, Vincenzi F, Rimondo C, Seri C, Varani K,
Serpelloni G, Marti M. Novel halogenated derivates of JWH-018: Behavioral and
binding studies in mice. Neuropharmacology. 2015 Aug;95:68-82. doi:
10.1016/j.neuropharm.2015.02.008. Epub 2015 Mar 11. PMID: 25769232.
59: Borea PA, Varani K, Vincenzi F, Baraldi PG, Tabrizi MA, Merighi S, Gessi S.
The A3 adenosine receptor: history and perspectives. Pharmacol Rev.
2015;67(1):74-102. doi: 10.1124/pr.113.008540. PMID: 25387804.
60: Romagnoli R, Baraldi PG, IJzerman AP, Massink A, Cruz-Lopez O, Lopez-Cara
LC, Saponaro G, Preti D, Aghazadeh Tabrizi M, Baraldi S, Moorman AR, Vincenzi F,
Borea PA, Varani K. Synthesis and biological evaluation of novel allosteric
enhancers of the A1 adenosine receptor based on
2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. J Med Chem.
2014 Sep 25;57(18):7673-86. doi: 10.1021/jm5008853. Epub 2014 Sep 12. PMID:
25181013.
61: Ferrante A, Martire A, Pepponi R, Varani K, Vincenzi F, Ferraro L, Beggiato
S, Tebano MT, Popoli P. Expression, pharmacology and functional activity of
adenosine A1 receptors in genetic models of Huntington's disease. Neurobiol Dis.
2014 Nov;71:193-204. doi: 10.1016/j.nbd.2014.08.013. Epub 2014 Aug 15. PMID:
25132555.
62: Squarcialupi L, Colotta V, Catarzi D, Varano F, Betti M, Varani K, Vincenzi
F, Borea PA, Porta N, Ciancetta A, Moro S.
7-Amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives: structural investigations
at the 5-position to target human A₁ and A(2A) adenosine receptors. Molecular
modeling and pharmacological studies. Eur J Med Chem. 2014 Sep 12;84:614-27.
doi: 10.1016/j.ejmech.2014.07.060. Epub 2014 Jul 19. PMID: 25063944.
63: Vincenzi F, Targa M, Romagnoli R, Merighi S, Gessi S, Baraldi PG, Borea PA,
Varani K. TRR469, a potent A(1) adenosine receptor allosteric modulator,
exhibits anti-nociceptive properties in acute and neuropathic pain models in
mice. Neuropharmacology. 2014 Jun;81:6-14. doi:
10.1016/j.neuropharm.2014.01.028. Epub 2014 Jan 31. PMID: 24486382.
64: Romagnoli R, Baraldi PG, Carrion MD, Cruz-Lopez O, Cara CL, Saponaro G,
Preti D, Tabrizi MA, Baraldi S, Moorman AR, Vincenzi F, Borea PA, Varani K.
Synthesis and biological evaluation of novel
2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric
enhancers of the A₁ adenosine receptor. Bioorg Med Chem. 2014 Jan
1;22(1):148-66. doi: 10.1016/j.bmc.2013.11.043. Epub 2013 Dec 1. PMID: 24332652.
65: Casetta I, Vincenzi F, Bencivelli D, Corciulo C, Gentile M, Granieri E,
Borea PA, Varani K. A(2A) adenosine receptors and Parkinson's disease severity.
Acta Neurol Scand. 2014 Apr;129(4):276-81. doi: 10.1111/ane.12181. Epub 2013 Aug
30. PMID: 24032478.
66: Romagnoli R, Baraldi PG, Carrion MD, Lopez Cara C, Kimatrai Salvador M,
Preti D, Aghazadeh Tabrizi M, Moorman AR, Vincenzi F, Borea PA, Varani K.
Synthesis and biological effects of novel
2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers
of the A1 adenosine receptor. Eur J Med Chem. 2013 Sep;67:409-27. doi:
10.1016/j.ejmech.2013.07.002. Epub 2013 Jul 13. PMID: 23911855.
67: Vincenzi F, Targa M, Corciulo C, Gessi S, Merighi S, Setti S, Cadossi R,
Goldring MB, Borea PA, Varani K. Pulsed electromagnetic fields increased the
anti-inflammatory effect of A₂A and A₃ adenosine receptors in human T/C-28a2
chondrocytes and hFOB 1.19 osteoblasts. PLoS One. 2013 May 31;8(5):e65561. doi:
10.1371/journal.pone.0065561. PMID: 23741498; PMCID: PMC3669296.
68: Aghazadeh Tabrizi M, Baraldi PG, Saponaro G, Moorman AR, Romagnoli R, Preti
D, Baraldi S, Ruggiero E, Tintori C, Tuccinardi T, Vincenzi F, Borea PA, Varani
K. Discovery of 7-oxopyrazolo[1,5-a]pyrimidine-6-carboxamides as potent and
selective CB(2) cannabinoid receptor inverse agonists. J Med Chem. 2013 Jun
13;56(11):4482-96. doi: 10.1021/jm400182t. Epub 2013 Jun 4. PMID: 23697626.
69: Vincenzi F, Corciulo C, Targa M, Casetta I, Gentile M, Granieri E, Borea PA,
Popoli P, Varani K. A2A adenosine receptors are up-regulated in lymphocytes from
amyotrophic lateral sclerosis patients. Amyotroph Lateral Scler Frontotemporal
Degener. 2013 Sep;14(5-6):406-13. doi: 10.3109/21678421.2013.793358. Epub 2013
May 16. PMID: 23679925.
70: Vincenzi F, Corciulo C, Targa M, Merighi S, Gessi S, Casetta I, Gentile M,
Granieri E, Borea PA, Varani K. Multiple sclerosis lymphocytes upregulate A2A
adenosine receptors that are antiinflammatory when stimulated. Eur J Immunol.
2013 Aug;43(8):2206-16. doi: 10.1002/eji.201343314. Epub 2013 Jun 3. PMID:
23661562.
71: Vincenzi F, Targa M, Corciulo C, Tabrizi MA, Merighi S, Gessi S, Saponaro G,
Baraldi PG, Borea PA, Varani K. Antinociceptive effects of the selective CB2
agonist MT178 in inflammatory and chronic rodent pain models. Pain. 2013
Jun;154(6):864-73. doi: 10.1016/j.pain.2013.02.007. Epub 2013 Feb 26. PMID:
23518609.
72: Squarcialupi L, Colotta V, Catarzi D, Varano F, Filacchioni G, Varani K,
Corciulo C, Vincenzi F, Borea PA, Ghelardini C, Di Cesare Mannelli L, Ciancetta
A, Moro S. 2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and
selective human A3 adenosine receptor antagonists. Molecular modeling studies
and pharmacological evaluation. J Med Chem. 2013 Mar 28;56(6):2256-69. doi:
10.1021/jm400068e. Epub 2013 Mar 7. PMID: 23427825.
73: Aghazadeh Tabrizi M, Baraldi PG, Saponaro G, Moorman AR, Romagnoli R, Preti
D, Baraldi S, Corciulo C, Vincenzi F, Borea PA, Varani K. Design, synthesis, and
pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine
derivatives as CB(2) cannabinoid receptor partial agonists. J Med Chem. 2013 Feb
14;56(3):1098-112. doi: 10.1021/jm301527r. Epub 2013 Feb 1. PMID: 23350768.
74: Fini M, Pagani S, Giavaresi G, De Mattei M, Ongaro A, Varani K, Vincenzi F,
Massari L, Cadossi M. Functional tissue engineering in articular cartilage
repair: is there a role for electromagnetic biophysical stimulation? Tissue Eng
Part B Rev. 2013 Aug;19(4):353-67. doi: 10.1089/ten.TEB.2012.0501. Epub 2013 Mar
19. PMID: 23339690.
75: Vincenzi F, Padovan M, Targa M, Corciulo C, Giacuzzo S, Merighi S, Gessi S,
Govoni M, Borea PA, Varani K. A(2A) adenosine receptors are differentially
modulated by pharmacological treatments in rheumatoid arthritis patients and
their stimulation ameliorates adjuvant-induced arthritis in rats. PLoS One.
2013;8(1):e54195. doi: 10.1371/journal.pone.0054195. Epub 2013 Jan 11. PMID:
23326596; PMCID: PMC3543361.
76: Catarzi D, Colotta V, Varano F, Poli D, Squarcialupi L, Filacchioni G,
Varani K, Vincenzi F, Borea PA, Dal Ben D, Lambertucci C, Cristalli G.
Pyrazolo[1,5-c]quinazoline derivatives and their simplified analogues as
adenosine receptor antagonists: synthesis, structure-affinity relationships and
molecular modeling studies. Bioorg Med Chem. 2013 Jan 1;21(1):283-94. doi:
10.1016/j.bmc.2012.10.031. Epub 2012 Oct 29. PMID: 23171656.
77: Romagnoli R, Baraldi PG, Carrion MD, Cara CL, Cruz-Lopez O, Salvador MK,
Preti D, Tabrizi MA, Moorman AR, Vincenzi F, Borea PA, Varani K. Synthesis and
biological evaluation of
2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-
thiophenes. effect of the 5-modification on allosteric enhancer activity at the
A1 adenosine receptor. J Med Chem. 2012 Sep 13;55(17):7719-35. doi:
10.1021/jm3007504. Epub 2012 Aug 28. PMID: 22889387.
78: Varani K, Vincenzi F, Targa M, Paradiso B, Parrilli A, Fini M, Lanza G,
Borea PA. The stimulation of A(3) adenosine receptors reduces bone-residing
breast cancer in a rat preclinical model. Eur J Cancer. 2013 Jan;49(2):482-91.
doi: 10.1016/j.ejca.2012.06.005. Epub 2012 Jul 5. PMID: 22770890.
79: Vincenzi F, Targa M, Corciulo C, Gessi S, Merighi S, Setti S, Cadossi R,
Borea PA, Varani K. The anti-tumor effect of A3 adenosine receptors is
potentiated by pulsed electromagnetic fields in cultured neural cancer cells.
PLoS One. 2012;7(6):e39317. doi: 10.1371/journal.pone.0039317. Epub 2012 Jun 25.
PMID: 22761760; PMCID: PMC3382599.
80: Baraldi PG, Saponaro G, Moorman AR, Romagnoli R, Preti D, Baraldi S,
Ruggiero E, Varani K, Targa M, Vincenzi F, Borea PA, Aghazadeh Tabrizi M.
7-Oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxamides as selective CB(2)
cannabinoid receptor ligands: structural investigations around a novel class of
full agonists. J Med Chem. 2012 Jul 26;55(14):6608-23. doi: 10.1021/jm300763w.
Epub 2012 Jul 11. PMID: 22738271.
81: Dalpiaz A, Cacciari B, Vicentini CB, Bortolotti F, Spalluto G, Federico S,
Pavan B, Vincenzi F, Borea PA, Varani K. A novel conjugated agent between
dopamine and an A2A adenosine receptor antagonist as a potential anti-Parkinson
multitarget approach. Mol Pharm. 2012 Mar 5;9(3):591-604. doi:
10.1021/mp200489d. Epub 2012 Feb 9. PMID: 22292533.
82: Romagnoli R, Baraldi PG, Carrion MD, Cara CL, Cruz-Lopez O, Salvador MK,
Preti D, Tabrizi MA, Shryock JC, Moorman AR, Vincenzi F, Varani K, Borea PA.
Structure-activity relationships of
2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the
influence of diverse substituents at the phenyl of the arylpiperazine moiety on
allosteric enhancer activity at the A₁ adenosine receptor. Bioorg Med Chem. 2012
Jan 15;20(2):996-1007. doi: 10.1016/j.bmc.2011.11.044. Epub 2011 Dec 1. PMID:
22182575.
83: Varani K, Padovan M, Vincenzi F, Targa M, Trotta F, Govoni M, Borea PA. A2A
and A3 adenosine receptor expression in rheumatoid arthritis: upregulation,
inverse correlation with disease activity score and suppression of inflammatory
cytokine and metalloproteinase release. Arthritis Res Ther. 2011;13(6):R197.
doi: 10.1186/ar3527. Epub 2011 Dec 6. PMID: 22146575; PMCID: PMC3334647.
84: Varani K, Vincenzi F, Targa M, Corciulo C, Fini M, Setti S, Cadossi R, Borea
PA. Effect of pulsed electromagnetic field exposure on adenosine receptors in
rat brain. Bioelectromagnetics. 2012 May;33(4):279-87. doi: 10.1002/bem.20704.
Epub 2011 Oct 19. PMID: 22012856.
85: Ongaro A, Varani K, Masieri FF, Pellati A, Massari L, Cadossi R, Vincenzi F,
Borea PA, Fini M, Caruso A, De Mattei M. Electromagnetic fields (EMFs) and
adenosine receptors modulate prostaglandin E(2) and cytokine release in human
osteoarthritic synovial fibroblasts. J Cell Physiol. 2012 Jun;227(6):2461-9.
doi: 10.1002/jcp.22981. PMID: 21830213.
86: Lenzi O, Colotta V, Catarzi D, Varano F, Squarcialupi L, Filacchioni G,
Varani K, Vincenzi F, Borea PA, Dal Ben D, Lambertucci C, Cristalli G.
Synthesis, structure-affinity relationships, and molecular modeling studies of
novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Bioorg Med Chem. 2011 Jun 15;19(12):3757-68. doi: 10.1016/j.bmc.2011.05.001.
Epub 2011 May 6. PMID: 21616671.
87: Varani K, Maniero S, Vincenzi F, Targa M, Stefanelli A, Maniscalco P,
Martini F, Tognon M, Borea PA. A₃ receptors are overexpressed in pleura from
patients with mesothelioma and reduce cell growth via Akt/nuclear factor-κB
pathway. Am J Respir Crit Care Med. 2011 Feb 15;183(4):522-30. doi:
10.1164/rccm.201006-0980OC. Epub 2010 Sep 24. PMID: 20870754.
88: Varani K, Padovan M, Govoni M, Vincenzi F, Trotta F, Borea PA. The role of
adenosine receptors in rheumatoid arthritis. Autoimmun Rev. 2010 Dec;10(2):61-4.
doi: 10.1016/j.autrev.2010.07.019. Epub 2010 Aug 5. PMID: 20691813.
89: Varani K, Vincenzi F, Tosi A, Targa M, Masieri FF, Ongaro A, De Mattei M,
Massari L, Borea PA. Expression and functional role of adenosine receptors in
regulating inflammatory responses in human synoviocytes. Br J Pharmacol. 2010
May;160(1):101-15. doi: 10.1111/j.1476-5381.2010.00667.x. Epub 2010 Mar 19.
PMID: 20331607; PMCID: PMC2860211.
90: Varani K, De Mattei M, Vincenzi F, Tosi A, Targa M, Masieri FF, Pellati A,
Massari L, Borea PA. P2X(1) and P2X(3) purinergic receptors differentially
modulate the inflammatory response in human osteoarthritic synovial fibroblasts.
Cell Physiol Biochem. 2010;25(2-3):325-36. doi: 10.1159/000276565. Epub 2010 Jan
12. PMID: 20110693.
91: Varani K, Caramori G, Vincenzi F, Tosi A, Barczyk A, Contoli M, Casolari P,
Triggiani M, Hansel T, Leung E, Maclennan S, Barnes PJ, Chung KF, Adcock I, Papi
A, Borea PA. Oxidative/nitrosative stress selectively altered A(2B) adenosine
receptors in chronic obstructive pulmonary disease. FASEB J. 2010
Apr;24(4):1192-204. doi: 10.1096/fj.09-139485. Epub 2009 Dec 14. PMID: 20008542.
92: Varani K, Massara A, Vincenzi F, Tosi A, Padovan M, Trotta F, Borea PA.
Normalization of A2A and A3 adenosine receptor up-regulation in rheumatoid
arthritis patients by treatment with anti-tumor necrosis factor alpha but not
methotrexate. Arthritis Rheum. 2009 Oct;60(10):2880-91. doi: 10.1002/art.24794.
PMID: 19790066.
93: Varani K, Vincenzi F, Tosi A, Gessi S, Casetta I, Granieri G, Fazio P, Leung
E, MacLennan S, Granieri E, Borea PA. A2A adenosine receptor overexpression and
functionality, as well as TNF-alpha levels, correlate with motor symptoms in
Parkinson's disease. FASEB J. 2010 Feb;24(2):587-98. doi: 10.1096/fj.09-141044.
Epub 2009 Sep 23. PMID: 19776336.
94: Lenzi O, Colotta V, Catarzi D, Varano F, Poli D, Filacchioni G, Varani K,
Vincenzi F, Borea PA, Paoletta S, Morizzo E, Moro S.
2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and
selective human A3 adenosine receptor antagonists: new insights into the
receptor-antagonist recognition. J Med Chem. 2009 Dec 10;52(23):7640-52. doi:
10.1021/jm900718w. PMID: 19743865.
95: Aguiari G, Varani K, Bogo M, Mangolini A, Vincenzi F, Durante C, Gessi S,
Sacchetto V, Catizone L, Harris P, Rizzuto R, Borea PA, Del Senno L. Deficiency
of polycystic kidney disease-1 gene (PKD1) expression increases A(3) adenosine
receptors in human renal cells: implications for cAMP-dependent signalling and
proliferation of PKD1-mutated cystic cells. Biochim Biophys Acta. 2009
Jun;1792(6):531-40. doi: 10.1016/j.bbadis.2009.03.001. Epub 2009 Mar 11. PMID:
19285554.
96: Colotta V, Capelli F, Lenzi O, Catarzi D, Varano F, Poli D, Vincenzi F,
Varani K, Borea PA, Dal Ben D, Volpini R, Cristalli G, Filacchioni G. Novel
potent and highly selective human A(3) adenosine receptor antagonists belonging
to the 4-amido-2-arylpyrazolo[3,4-c]quinoline series: molecular docking analysis
and pharmacological studies. Bioorg Med Chem. 2009 Jan 1;17(1):401-10. doi:
10.1016/j.bmc.2008.10.018. Epub 2008 Oct 11. PMID: 18996701.
97: Romagnoli R, Baraldi PG, Carrion MD, Cara CL, Cruz-Lopez O, Iaconinoto MA,
Preti D, Shryock JC, Moorman AR, Vincenzi F, Varani K, Andrea Borea P. Synthesis
and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted)
piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine
receptor. J Med Chem. 2008 Sep 25;51(18):5875-9. doi: 10.1021/jm800586p. Epub
2008 Aug 26. PMID: 18729349.
98: De Mattei M, Varani K, Masieri FF, Pellati A, Ongaro A, Fini M, Cadossi R,
Vincenzi F, Borea PA, Caruso A. Adenosine analogs and electromagnetic fields
inhibit prostaglandin E2 release in bovine synovial fibroblasts. Osteoarthritis
Cartilage. 2009 Feb;17(2):252-62. doi: 10.1016/j.joca.2008.06.002. Epub 2008 Jul
18. PMID: 18640059.
99: Varani K, De Mattei M, Vincenzi F, Tosi A, Gessi S, Merighi S, Pellati A,
Masieri F, Ongaro A, Borea PA. Pharmacological characterization of P2X1 and P2X3
purinergic receptors in bovine chondrocytes. Osteoarthritis Cartilage. 2008
Nov;16(11):1421-9. doi: 10.1016/j.joca.2008.03.016. Epub 2008 Apr 29. PMID:
18448363.
100: Varani K, Surprenant A, Vincenzi F, Tosi A, Gessi S, Merighi S, Borea PA.
Binding thermodynamic characterization of human P2X1 and P2X3 purinergic
receptors. Biochem Pharmacol. 2008 Mar 1;75(5):1198-208. doi:
10.1016/j.bcp.2007.10.034. Epub 2007 Nov 9. PMID: 18076867.
101: Morizzo E, Capelli F, Lenzi O, Catarzi D, Varano F, Filacchioni G, Vincenzi
F, Varani K, Borea PA, Colotta V, Moro S. Scouting human A3 adenosine receptor
antagonist binding mode using a molecular simplification approach: from
triazoloquinoxaline to a pyrimidine skeleton as a key study. J Med Chem. 2007
Dec 27;50(26):6596-606. doi: 10.1021/jm070852a. Epub 2007 Nov 30. PMID:
18047262.
102: Varani K, De Mattei M, Vincenzi F, Gessi S, Merighi S, Pellati A, Ongaro A,
Caruso A, Cadossi R, Borea PA. Characterization of adenosine receptors in bovine
chondrocytes and fibroblast-like synoviocytes exposed to low frequency low
energy pulsed electromagnetic fields. Osteoarthritis Cartilage. 2008
Mar;16(3):292-304. doi: 10.1016/j.joca.2007.07.004. Epub 2007 Aug 16. PMID:
17698373.
103: Stasi MA, Borsini F, Varani K, Vincenzi F, Di Cesare MA, Minetti P,
Ghirardi O, Carminati P. ST 1535: a preferential A2A adenosine receptor
antagonist. Int J Neuropsychopharmacol. 2006 Oct;9(5):575-84. doi:
10.1017/S1461145705006188. Epub 2005 Nov 23. PMID: 16867213.
104: Varani K, Caramori G, Vincenzi F, Adcock I, Casolari P, Leung E, Maclennan
S, Gessi S, Morello S, Barnes PJ, Ito K, Chung KF, Cavallesco G, Azzena G, Papi
A, Borea PA. Alteration of adenosine receptors in patients with chronic
obstructive pulmonary disease. Am J Respir Crit Care Med. 2006 Feb
15;173(4):398-406. doi: 10.1164/rccm.200506-869OC. Epub 2005 Dec 1. PMID:
16322645.
105: Baraldi PG, Pavani MG, Leung E, Moorman AR, Varani K, Vincenzi F, Borea PA,
Romagnoli R. Synthesis and biological characterization of [3H]
(2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone,
the first radiolabelled adenosine A1 allosteric enhancer. Bioorg Med Chem Lett.
2006 Mar 1;16(5):1402-4. doi: 10.1016/j.bmcl.2005.11.037. PMID: 16321527.
106: Varani K, Gessi S, Merighi S, Vincenzi F, Cattabriga E, Benini A, Klotz KN,
Baraldi PG, Tabrizi MA, Lennan SM, Leung E, Borea PA. Pharmacological
characterization of novel adenosine ligands in recombinant and native human A2B
receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12. doi:
10.1016/j.bcp.2005.08.018. Epub 2005 Oct 10. PMID: 16219300.
107: Varani K, Portaluppi F, Gessi S, Merighi S, Vincenzi F, Cattabriga E,
Dalpiaz A, Bortolotti F, Belardinelli L, Borea PA. Caffeine intake induces an
alteration in human neutrophil A2A adenosine receptors. Cell Mol Life Sci. 2005
Oct;62(19-20):2350-8. doi: 10.1007/s00018-005-5312-z. PMID: 16143823.