Product Data Sheet

L-654284

Catalog No. A58433

main product photo
L-654284 is a selective α2-adrenergic receptor antagonist that effectively competes with the binding of radiolabeled 3H-clonidine and 3H-rauwolscine, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. This compound demonstrates the ability to block the effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. Additionally, L-654284 shows notable selectivity towards α2 and α1 adrenergic receptors, with a Ki of 110 nM against 3H-prazosin binding. In vivo studies reveal that L-654284 enhances norepinephrine turnover in the rat cerebral cortex, highlighting its potential applications in research related to central nervous system pharmacology.
Chemical Information
Catalog NumA58433
M. Wt364.46
FormulaC18H24N2O4S
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.98719-20-1
Synonyms
SMILESOCCS(N([C@H]1C[C@@]2([H])C3=C(CCN2CC1)C4=CC=CC=C4O3)C)(=O)=O
Biological Activity
DescriptionL-654284 is a selective α2-adrenergic receptor antagonist that effectively competes with the binding of radiolabeled 3H-clonidine and 3H-rauwolscine, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. This compound demonstrates the ability to block the effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. Additionally, L-654284 shows notable selectivity towards α2 and α1 adrenergic receptors, with a Ki of 110 nM against 3H-prazosin binding. In vivo studies reveal that L-654284 enhances norepinephrine turnover in the rat cerebral cortex, highlighting its potential applications in research related to central nervous system pharmacology.
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