L-654284 is an alpha2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for alpha2 and alpha1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing alpha2-adrenergic receptor blocking activity in the central nervous system[1].
Molekulargewicht:
364.46
CAS Nummer:
[98719-20-1]
Formel:
C18H24N2O4S
Target-Kategorie:
Adrenergic Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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