salvinorin a

Salvinorin A 是一种非含氮 κ-opioid 样物质选择性激动剂。

Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .

Salvinorin A carbamate, a potent κ-opioid receptor (KOR) full agonist, exhibits nearly the same potency as salvinorin A, with EC50 values of 6.2 and 4.5 nM, respectively, for activating the human KOR to augment the binding of [35S]GTPγS. Enhancing biological stability, the addition of a carbamate group to salvinorin A reduces deacetylation.

Mesyl Salvinorin B is a selective and potent full KOP receptor agonist. It acts by preventing cocaine-seeking and reducing excessive alcohol drinking via the KOP-r-mediated mechanism.

RB-64 (22-Thiocyanatosalvinorin A)为一种kappa-opioid receptor选择性激动剂，展现出高效性，其EC50值仅为0.077 nM。

Herkinorin is an opioid analgesic and an analogue of the natural product Salvinorin A. herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic c

Enadoline (Free Base) is a kappa-opioid receptor agonist; PD 129290 (CAM 570; CI 977) is the S,S(-)-enantiomer; PD 129289 (CAM 569) is the corresponding R,R(+)-enantiomer. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist. There was mention of its potential in treating comatose head injury or stroke victims, where that type of side effect would be immaterial.