Plants - Drugs Mind - Spirit Freedom - Law Arts - Culture Library  
Erowid References Database
Lee DY, Karnati VV, He M, Liu-Chen LY, Kondaveti L, Ma Z, Wang Y, Chen Y, Beguin C, Carlezon WA, Cohen B. 
“Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues”. 
Bioorg Med Chem Lett. 2005 Aug 25;15(16):3744-7.
Salvinorin A is the most potent naturally occurring opioid agonist yet discovered with high selectivity and affinity for kappa-opioid receptor. To explore its structure and activity relationships, a series of salvinorin A derivatives modified at the C2 position were prepared and studied. These salvinorin A derivatives were screened for binding and functional activities at the human kappa-opioid receptor. Compound 4, containing a methoxymethyl group at the 2-position, was a full kappa-agonist with an EC50 value at 0.6 nM, which is about 7 times more potent than salvinorin A.
Comments and Responses to this Article
Submit Comment
[ Cite HTML ]