Effects of salvinorin A, a kappa-opioid hallucinogen, on a neuroendocrine biomarker assay in nonhuman primates with high kappa-receptor homology to humans.
The Journal of pharmacology and experimental therapeutics January 1, 2007 Eduardo R Butelman, Marek Mandau, Kevin Tidgewell et al. 64 citations
The hallucinogen salvinorin A, derived from the plant Salvia divinorum, acts as a high-efficacy kappa-opioid agonist in nonhuman primates. In a neuroendocrine biomarker assay measuring the anterior pituitary hormone prolactin, salvinorin A produced dose- and time-dependent effects in adult male and female rhesus monkeys (n = 4 each). It was approximately equipotent to the synthetic kappa-agonist U69,593 (ED50 0.015 mg/kg vs. 0.0098 mg/kg) but had a shorter duration. The effects were blocked by a high dose of the opioid antagonist nalmefene (0.1 mg/kg) but not by a low dose (0.01 mg/kg) or by the 5HT2 receptor antagonist ketanserin. Effects were more robust in females. Cloning of the rhesus monkey kappa-opioid receptor gene showed high homology with the human gene.