AM-938
AM-938 is an analgesic drug which is a cannabinoid receptor agonist. It is a derivative of HU-210 which has been substituted with a 6尾-(3-hydroxyprop-1-ynyl) group. This adds a "southern" aliphatic hydroxyl group to the molecule as seen in the CP-series of nonclassical cannabinoid drugs, and so AM-938 represents a hybrid structure between the classical and nonclassical cannabinoid families,[1] with the 6-hydroxyalkyl chain rigidified with a triple bond. This gives AM-938 a greater degree of selectivity, so while it is still a potent agonist at both CB1 and CB2, it is reasonably selective for CB2, with a Ki of 0.3nM at CB2 and 1.2nM at CB1, a selectivity of around 4x.[2][3]
See also
References
- ^ Roger Pertwee. Cannabinoids. Handbook of Experimental Pharmacology Volume 168, p 269. Springer. ISBN 3-540-22565-X
- ^ Tius MA, Hill WA, Zou XL, Busch-Petersen J, Kawakami JK, Fernandez-Garcia MC, Drake DJ, Abadji V, Makriyannis A. Classical/non-classical cannabinoid hybrids; stereochemical requirements for the southern hydroxyalkyl chain. Life Sciences. 1995;56(23-24):2007-12. PMID 7776825
- ^ Drake DJ, Jensen RS, Busch-Petersen J, Kawakami JK, Concepcion Fernandez-Garcia M, Fan P, Makriyannis A, Tius MA. Classical/nonclassical hybrid cannabinoids: southern aliphatic chain-functionalized C-6beta methyl, ethyl, and propyl analogues. Journal of Medicinal Chemistry. 1998 Sep 10;41(19):3596-608. PMID 9733485
|
|
Plant cannabinoids |
|
|
Cannabinoid metabolites |
|
|
Endogenous cannabinoids |
|
|
Synthetic cannabinoid
receptor agonists |
Classical cannabinoids
(Dibenzopyrans)
|
|
|
Nonclassical cannabinoids
|
|
|
Benzoylindoles
|
|
|
Naphthoylindoles
|
|
|
Naphthylmethylindoles
|
JWH-175 路 JWH-184 路 JWH-185 路 JWH-192 路 JWH-194 路 JWH-195 路 JWH-196 路 JWH-197 路 JWH-199
|
|
Phenylacetylindoles
|
|
|
Naphthoylpyrroles
|
|
|
Eicosanoids
|
|
|
Others
|
|
|
|
Allosteric modulators of
cannabinoid receptors |
|
|
Endocannabinoid
activity enhancers |
|
|
Cannabinoid receptor
antagonists and
inverse agonists |
|
|