A ligand for the κ-opioid DREADD (EC50s = 11.8 and 160 nM with high or low levels of KORD expression

Salvinorin B – 5 mg

Brand:
Cayman
CAS:
92545-30-7
Storage:
-20
UN-No:
Non-Hazardous - /

Salvinorin B is the major deacetylated metabolite of salvinorin A (Item No. 11487).{36003,34652} It reportedly lacks pharmacological activity in vitro and in vivo when used in unperturbed systems. It binds as an agonist at the κ-opioid receptor (Ki = 2,950 nM; EC50 = 248 nM) but does not elicit antinociceptive effects even after i.c.v. administration. However, salvinorin B is a ligand for the inhibitory G protein-coupled κ-opioid designer receptor exclusively activated by designer drugs (DREADD; KORD; EC50s = 11.8 and 160 nM with high or low levels of KORD expression, respectively).{38358} It leads to hyperpolarization and inhibition of neuronal firing in neurons expressing KORD and has no effect on neurons transduced with mCherry as a control. Salvinorin B increases locomotor activity in VGAT-ires-Cre mice expressing KORD in the ventral tegmental area and substantia nigra, increases food intake in SIM1-Cre mice expressing KORD in the paraventricular hypothalamus, and decreases food intake in AGRP-ires-Cre mice expressing KORD in the arcuate nucleus. Salvinorin B can be used in combination with clozapine N-oxide (CNO; Item No. 16882) because it is inactive at Gq-based DREADDs. Salvinorin B is also available as an analytical reference standard (Item No. 11488).  

 

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Description

A ligand for the κ-opioid DREADD (EC50s = 11.8 and 160 nM with high or low levels of KORD expression, respectively); pharmacology inactive in unperturbed systems (Ki = 2,950 nM; EC50 = 248 nM); inhibits neuronal firing in neurons expressing KORD with effects dependent upon which brain region is expressing KORD; can be used in combination with CNO because it is inactive at Gq-based DREADDs

Formal name: (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(3-furanyl)dodecahydro-9-hydroxy-6a,10b-dimethyl-4,10-dioxo-2H-naphtho[2,1-c]pyran-7-carboxylic acid, methyl ester

Synonyms:  Divinorin B

Molecular weight: 390.4

CAS: 92545-30-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Research Area|Neuroscience|Behavioral Neuroscience|Food Intake||Research Area|Neuroscience|DREADD Research||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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