L-654284 - CAS 98719-20-1

L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.

Adrenergic Receptor, Others

Neuroscience, GPCR/G Protein, Others

98698

C18H24N2O4S

364.46

N(S(CCO)(=O)=O)(C)[C@H]1C[C@]2(C3=C(C=4C(O3)=CC=CC4)CCN2CC1)[H]

-20°C

Ice Packs

Small Compound