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Dual role of the second extracellular loop of the cannabinoid receptor 1: ligand binding and receptor localization.

Ahn KH, Bertalovitz AC, Mierke DF, Kendall DA.

Mol Pharmacol. 2009 Oct;76(4):833-42. doi: 10.1124/mol.109.057356. Epub 2009 Jul 30.


Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2.

Marcu J, Shore DM, Kapur A, Trznadel M, Makriyannis A, Reggio PH, Abood ME.

J Pharmacol Exp Ther. 2013 May;345(2):189-97. doi: 10.1124/jpet.112.201046. Epub 2013 Feb 20.


Allosteric modulation of the cannabinoid CB1 receptor.

Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, Pertwee RG, Ross RA.

Mol Pharmacol. 2005 Nov;68(5):1484-95. Epub 2005 Aug 19.


Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor.

Khajehali E, Malone DT, Glass M, Sexton PM, Christopoulos A, Leach K.

Mol Pharmacol. 2015 Aug;88(2):368-79. doi: 10.1124/mol.115.099192. Epub 2015 Jun 4.


Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1.

Bertalovitz AC, Ahn KH, Kendall DA.

Drug Dev Res. 2010 Nov 1;71(7):404-411.


Allosteric modulation of a cannabinoid G protein-coupled receptor: binding site elucidation and relationship to G protein signaling.

Shore DM, Baillie GL, Hurst DH, Navas F 3rd, Seltzman HH, Marcu JP, Abood ME, Ross RA, Reggio PH.

J Biol Chem. 2014 Feb 28;289(9):5828-45. doi: 10.1074/jbc.M113.478495. Epub 2013 Dec 23.


Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction.

Hurst D, Umejiego U, Lynch D, Seltzman H, Hyatt S, Roche M, McAllister S, Fleischer D, Kapur A, Abood M, Shi S, Jones J, Lewis D, Reggio P.

J Med Chem. 2006 Oct 5;49(20):5969-87.


Anandamide-mediated CB1/CB2 cannabinoid receptor--independent nitric oxide production in rabbit aortic endothelial cells.

McCollum L, Howlett AC, Mukhopadhyay S.

J Pharmacol Exp Ther. 2007 Jun;321(3):930-7. Epub 2007 Mar 22.


A cannabinoid receptor 1 mutation proximal to the DRY motif results in constitutive activity and reveals intramolecular interactions involved in receptor activation.

D'Antona AM, Ahn KH, Wang L, Mierke DF, Lucas-Lenard J, Kendall DA.

Brain Res. 2006 Sep 7;1108(1):1-11. Epub 2006 Jul 31.


(-)-7'-Isothiocyanato-11-hydroxy-1',1'-dimethylheptylhexahydrocannabinol (AM841), a high-affinity electrophilic ligand, interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor.

Picone RP, Khanolkar AD, Xu W, Ayotte LA, Thakur GA, Hurst DP, Abood ME, Reggio PH, Fournier DJ, Makriyannis A.

Mol Pharmacol. 2005 Dec;68(6):1623-35. Epub 2005 Sep 12.


Sphingosine and its analog, the immunosuppressant 2-amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol, interact with the CB1 cannabinoid receptor.

Paugh SW, Cassidy MP, He H, Milstien S, Sim-Selley LJ, Spiegel S, Selley DE.

Mol Pharmacol. 2006 Jul;70(1):41-50. Epub 2006 Mar 29.


3-Substituted pyrazole analogs of the cannabinoid type 1 (CB₁) receptor antagonist rimonabant: cannabinoid agonist-like effects in mice via non-CB₁, non-CB₂ mechanism.

Wiley JL, Selley DE, Wang P, Kottani R, Gadthula S, Mahadeven A.

J Pharmacol Exp Ther. 2012 Feb;340(2):433-44. doi: 10.1124/jpet.111.187815. Epub 2011 Nov 15.


N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor.

Hurst DP, Lynch DL, Barnett-Norris J, Hyatt SM, Seltzman HH, Zhong M, Song ZH, Nie J, Lewis D, Reggio PH.

Mol Pharmacol. 2002 Dec;62(6):1274-87.


Involvement of cannabinoid receptors in the regulation of neurotransmitter release in the rodent striatum: a combined immunochemical and pharmacological analysis.

Köfalvi A, Rodrigues RJ, Ledent C, Mackie K, Vizi ES, Cunha RA, Sperlágh B.

J Neurosci. 2005 Mar 16;25(11):2874-84.


Mutation studies of Ser7.39 and Ser2.60 in the human CB1 cannabinoid receptor: evidence for a serine-induced bend in CB1 transmembrane helix 7.

Kapur A, Hurst DP, Fleischer D, Whitnell R, Thakur GA, Makriyannis A, Reggio PH, Abood ME.

Mol Pharmacol. 2007 Jun;71(6):1512-24. Epub 2007 Mar 23.


An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region.

McAllister SD, Rizvi G, Anavi-Goffer S, Hurst DP, Barnett-Norris J, Lynch DL, Reggio PH, Abood ME.

J Med Chem. 2003 Nov 20;46(24):5139-52.


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