O-1918 Explained
O-1918 is a synthetic compound related to cannabidiol, which is an antagonist at two former orphan receptors GPR18 and GPR55, that appear to be related to the cannabinoid receptors. O-1918 is used in the study of these receptors, which have been found to be targets for a number of endogenous and synthetic cannabinoid compounds, and are thought to be responsible for most of the non-CB1, non-CB2 mediated effects that have become evident in the course of cannabinoid research.[1] [2] [3] [4] [5]
Subsequent research by using electrophysiological approach has shown that O-1918 is a potent BKCa channel inhibitor.[6] [7] [8]
See also
Notes and References
- Offertáler L, Mo FM, Bátkai S, Liu J, Begg M, Razdan RK, Martin BR, Bukoski RD, Kunos G . Selective ligands and cellular effectors of a G protein-coupled endothelial cannabinoid receptor . Molecular Pharmacology . 63 . 3 . 699–705 . March 2003 . 12606780 . 10.1124/mol.63.3.699 .
- Zakrzeska A, Schlicker E, Baranowska M, Kozłowska H, Kwolek G, Malinowska B . A cannabinoid receptor, sensitive to O-1918, is involved in the delayed hypotension induced by anandamide in anaesthetized rats . British Journal of Pharmacology . 160 . 3 . 574–84 . June 2010 . 20105178 . 2931558 . 10.1111/j.1476-5381.2009.00579.x .
- Schuelert N, McDougall JJ . The abnormal cannabidiol analogue O-1602 reduces nociception in a rat model of acute arthritis via the putative cannabinoid receptor GPR55 . Neuroscience Letters . 500 . 1 . 72–6 . August 2011 . 21683763 . 10.1016/j.neulet.2011.06.004 . 3410391 .
- Szczesniak AM, Maor Y, Robertson H, Hung O, Kelly ME . Nonpsychotropic cannabinoids, abnormal cannabidiol and canabigerol-dimethyl heptyl, act at novel cannabinoid receptors to reduce intraocular pressure . Journal of Ocular Pharmacology and Therapeutics . 27 . 5 . 427–35 . October 2011 . 21770780 . 10.1089/jop.2011.0041 .
- Caldwell MD, Hu SS, Viswanathan S, Bradshaw H, Kelly ME, Straiker A . A GPR18-based signalling system regulates IOP in murine eye . British Journal of Pharmacology . 169 . 4 . 834–43 . June 2013 . 23461720 . 3687663 . 10.1111/bph.12136 .
- Godlewski G, Offertáler L, Osei-Hyiaman D, Mo FM, Harvey-White J, Liu J, Davis MI, Zhang L, Razdan RK, Milman G, Pacher P, Mukhopadhyay P, Lovinger DM, Kunos G . The endogenous brain constituent N-arachidonoyl L-serine is an activator of large conductance Ca2+-activated K+ channels . The Journal of Pharmacology and Experimental Therapeutics . 328 . 1 . 351–361 . January 2009 . 18923087 . 2605781 . 10.1124/jpet.108.144717 .
- Bondarenko AI, Panasiuk O, Drachuk K, Montecucco F, Brandt KJ, Mach F . The quest for endothelial atypical cannabinoid receptor: BKCa channels act as cellular sensors for cannabinoids in in vitro and in situ endothelial cells . Vascular Pharmacology . 102 . 44–55 . March 2018 . 29355732 . 6481560 . 10.1016/j.vph.2018.01.004 .
- Bondarenko AI, Panasiuk O, Okhai I, Montecucco F, Brandt KJ, Mach F . Direct activation of Ca2+ and voltage-gated potassium channels of large conductance by anandamide in endothelial cells does not support the presence of endothelial atypical cannabinoid receptor . European Journal of Pharmacology . 805 . 14–24 . June 2017 . 28327344 . 6520242 . 10.1016/j.ejphar.2017.03.038 .