RS 127445 hydrochloride

Solubility:Soluble to 30 mM in ethanol and to 100 mM in DMSO and to 20 mM in Tocrisolve (Cat.No.1684)

Storage:Store at +4°C

Biologieal

Nanomolar affinity cannabinoid receptor agonist (K_i values are 62.3 and 3.3 nM at the human cloned CB₁ and CB₂ receptors respectively). Also available as part of the Cannabinoid Receptor Agonist Tocriset™. S-enantiomer WIN 55,212-3 mesylate (Cat. No. 2327) also available

Reference

D'Ambra et al (1992) Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. J.Med.Chem. 35 124. PMID: 1732519.

Felder et al (1995) Comparison of the pharmacology and signal transduction of the human cannabinoid CB₁ and CB₂ receptors. Mol.Pharmacol. 48 443. PMID: 7565624.

Griffin et al (1998) Evaluation of cannabinoid receptor agonists and antagonists using the guanosine-5'-O-(3-[35S]thio)-triphosphate binding assay in rat cerebellar membranes. J.Pharmacol.Exp.Ther. 285 553. PMID: 9580597.