L-771688 hydrochloride

Description

L-771688 hydrochloride is a potent and highly selective ?1A-adrenoceptor antagonist Kd=43-90 pM . L-771688 hydrochloride is effective against cloned human, rat and dog ?1A-adrenergic receptors. L-771688 exhibits high affinity Ki ? 1 nM and over 500-fold selectivity over the ?1B and ?1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models.