Use of selective 244 ~ 1b ~ -adrenergic receptor antagonists to improve sexual dysfunction

摘要

"USE OF SELECTIVE ANTAGONISTS OF RECEPTOR 244 ~ 1b ~ -ADRENERGIC FOR IMPROVING SEXUAL DYSFUNCTION". Compounds (I) (A = 2 furyl, 2-substituted furyl, 2-tetrahydrofuryl, substituted alkoxy or substituted phenoxyalkyl; B = B ~ 1 ~, B ~ 2 ~ or B ~ 3 ~ but if B = B ~ 1 ~ , then A = substituted phenoxyalkyl) and its enantiomers, diastereoisomers and pharmaceutically acceptable salts are useful for the preparation of a medicament for the treatment of sexual dysfunction in men and women. Compounds II (I: B = B ~ 3 ~, A sym 2-furyl) are new and are claimed properly. Pharmaceutical compositions containing compounds II are also claimed, as are pharmaceutical compositions containing compounds I and one or more of prostaglandin, a direct vasodilator and an inhibitor of 5 cGMP phosphodiesterase (e.g., sildenafil). Compounds that bind to 244 - ~ 1b ~ adrenergic receptors with an affinity of at least 10 ^ -8 ^ M and that bind to 244 ~ 1b ~ adrenergic receptors with at least 10 times greater affinity than the affinity with which the compound binds to the 244 ~ 1a ~ or 244 ~ 1d ~ or 244 ~ 1l ~ mammalian adrenergic receptors are also useful for preparing a drug for the treatment of dysfunction sex in men and women. a process for identifying such compounds is also disclosed and claimed.