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  4. L-654284

L-654284 is an α2-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 α2 and α1 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 α2-adrenergic receptor blocking activity in the central nervous system.

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L-654284 Chemical Structure

L-654284 Chemical Structure

CAS No. : 98719-20-1

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Description

L-654284 is an α2-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 α2 and α1 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 α2-adrenergic receptor blocking activity in the central nervous system[1].

Molecular Weight

364.46

Formula

C18H24N2O4S
CAS No.
SMILES

OCCS(N([C@H]1C[C@@]2([H])C3=C(CCN2CC1)C4=CC=CC=C4O3)C)(=O)=O
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L-654284 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

L-65428498719-20-1L654284L 654284OthersInhibitorinhibitorinhibit

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