RB-64 (22-thiocyanatosalvinorin A) is a semi-synthetic
salvinorin derivative and a
κ-opioid receptor
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind op ...
(KOR)
agonist which is used in scientific research. Its most remarkable property is its
functional selectivity for
G protein
G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their a ...
versus
β-arrestin-2. RB-64 has a
bias factor of 96 and is
analgesic with fewer of the side-effects associated with unbiased KOR agonists. The analgesia-like effect is long-lasting. Compared with unbiased agonists, RB-64 evokes considerably less
receptor internalization.
See also
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Herkinorin
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Salvinorin B methoxymethyl ether
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Salvinorin A
Salvinorin A is the main active psychotropic molecule in ''Salvia divinorum''. Salvinorin A is considered a dissociative hallucinogen.
It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psilocybin, an ...
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Nalfurafine
Nalfurafine (International Nonproprietary Name, INN, United States Adopted Name, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment ...
References
Further reading
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Synthetic opioids
Kappa-opioid receptor agonists
Kappa-opioid receptor antagonists
Thiocyanates
Biased ligands
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