AM-2389 - Revision history

Adm1n at 23:26, 14 February 2015

2015-02-14T23:26:32Z

Adm1n at 23:26, 14 February 2015

2015-02-14T23:26:10Z

Adm1n: Created page with "AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the CB1 receptor, with a Ki of 0.16 nM, and 26x selectivity over..."

2015-02-14T23:25:37Z

Created page with "AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the CB1 receptor, with a Ki of 0.16 nM, and 26x selectivity over..."

New page

AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the [[CB1]] receptor, with a Ki of 0.16 nM, and 26x selectivity over the related [[CB2 receptor]]. It has high potency in animal tests of cannabinoid activity, and a medium duration of action. Replacing the 1',1'-dimethyl substitution of the dimethylheptyl side chain of classical cannabinoids with cyclopropyl or cyclopentyl results in higher potency than cyclobutyl, but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to achieve (cf. [[AM-906]], [[AM-1235]]), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only truly highly selective CB1 agonists known as of 2012 are eicosanoid derivatives such as [[O-1812]].

==See also==

* [[9-nor-9β-Hydroxyhexahydrocannabinol|HHC]]
* [[AMG-36]]
* [[AMG-41]]

← Older revision		Revision as of 23:26, 14 February 2015
Line 1:		Line 1:
−	AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the [[CB1 ~~receptor~~]], with a Ki of 0.16 nM, and 26x selectivity over the related [[CB2 receptor]]. It has high potency in animal tests of cannabinoid activity, and a medium duration of action. Replacing the 1',1'-dimethyl substitution of the dimethylheptyl side chain of classical cannabinoids with cyclopropyl or cyclopentyl results in higher potency than cyclobutyl, but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to achieve (cf. [[AM-906]], [[AM-1235]]), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only truly highly selective CB1 agonists known as of 2012 are eicosanoid derivatives such as [[O-1812]].	+	AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the [[CB1]] receptor, with a Ki of 0.16 nM, and 26x selectivity over the related [[CB2 receptor]]. It has high potency in animal tests of cannabinoid activity, and a medium duration of action. Replacing the 1',1'-dimethyl substitution of the dimethylheptyl side chain of classical cannabinoids with cyclopropyl or cyclopentyl results in higher potency than cyclobutyl, but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to achieve (cf. [[AM-906]], [[AM-1235]]), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only truly highly selective CB1 agonists known as of 2012 are eicosanoid derivatives such as [[O-1812]].

← Older revision		Revision as of 23:26, 14 February 2015
Line 1:		Line 1:
−	AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the [[CB1]] ~~receptor~~, with a Ki of 0.16 nM, and 26x selectivity over the related [[CB2 receptor]]. It has high potency in animal tests of cannabinoid activity, and a medium duration of action. Replacing the 1',1'-dimethyl substitution of the dimethylheptyl side chain of classical cannabinoids with cyclopropyl or cyclopentyl results in higher potency than cyclobutyl, but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to achieve (cf. [[AM-906]], [[AM-1235]]), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only truly highly selective CB1 agonists known as of 2012 are eicosanoid derivatives such as [[O-1812]].	+	AM-2389 is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the [[CB1 receptor]], with a Ki of 0.16 nM, and 26x selectivity over the related [[CB2 receptor]]. It has high potency in animal tests of cannabinoid activity, and a medium duration of action. Replacing the 1',1'-dimethyl substitution of the dimethylheptyl side chain of classical cannabinoids with cyclopropyl or cyclopentyl results in higher potency than cyclobutyl, but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to achieve (cf. [[AM-906]], [[AM-1235]]), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only truly highly selective CB1 agonists known as of 2012 are eicosanoid derivatives such as [[O-1812]].