98719-20-1
Chemical Structure
L-654284
- CAS No.: 98719-20-1
- Formula:C18H24N2O4S
- Molecular Weight:364.46
IUPAC Name: N-((2R,12bS)-1,3,4,6,7,12b-hexahydro-2H-benzofuro[2,3-a]quinolizin-2-yl)-2-hydroxy-N-methylethane-1-sulfonamide
InChIKey: KPPZSBMFUSDGBU-CJNGLKHVSA-N
SMILES: OCCS(N([C@H]1C[C@@]2([H])C3=C(CCN2CC1)C4=CC=CC=C4O3)C)(=O)=O
Biological Activity: 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].
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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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Keywords
