Salvinorin A

Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum. IC50 & Target:Ki:4.3 nm (kappa-opioid receptor)^[1] In Vitro:Salvinorin A (Divinorin A)(0.01-10 pM; pre-30 minues; 24 hours) does not affect the membrane function after 24-h exposure in macrophages^[1].
Salvinorin A (Divinorin A) (0.01-10 pM; pre-30 minues; 18 hours) before LPS stimulation causes a significant and concentrationdependent manner reduction of LPS-stimulated nitrite levels, the IC50 (95% CL) of salvinorin A inhibitory effect was 6.5×10⁻¹³M^[1].
Salvinorin A (Divinorin A) (0.01-10 pM; pre-30 minues; 18 hours) incubates 30 min before LPS stimulation, reduces in concentration-dependent manner the LPSinduced iNOS, but not COX-2, hyperexpression, reaching a statistical significance at the 10 pM concentration^[1].
In Vivo:Salvinorin A (intraperitoneal injection; 0.5-2 mg/kg; pre-treatment 30 minutes) at the 0.5 mg/kg dose is the most effective one, at the dose of 0.5 mg/kg, significantly inhibits oedema during the first 6 h; at the dose of 1 mg/kg, salvinorin A significantly reduces the oedema only 4 h after carrageenan injection; at the highest doses tested (2 mg/kg), salvinorin A fails to evoke significant changes on the carrageenan-induced paw oedema^[1].