Ethanesulfonamide, N-[(2R,12bS)-1,3,4,6,7,12b-hexahydro-2H-benzofuro[2,3-a]quinolizin-2-yl]-2-hydroxy-N-methyl-

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].

[1] L-654,284 a new potent and selective alpha 2-adrenoceptor antagonist