L-654284

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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 K_i 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 K_i 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

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 K_i 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 K_i 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.	98719-20-1
SMILES	OCCS(N([C@H]1C[C@@]2([H])C3=C(CCN2CC1)C4=CC=CC=C4O3)C)(=O)=O
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (268 KB) Handling Instructions (2659 KB)
References	[1]. L-654,284 a new potent and selective alpha 2-adrenoceptor antagonist

L-654284 Related Classifications

Neurological Disease

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-65428498719-20-1L654284L 654284OthersInhibitorinhibitorinhibit

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L-654284

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