Selective, high affinity, non-competitive α1A adrenoceptor antagonist
Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate muscle in vitro and on intra-urethral pressure in rats.
Palea et al (2013) Effects of ρ-Da1a a peptidic α1A-adrenoceptor antagonist in human isolated prostatic adenoma and anaesthetized rats. Br.J.Pharmacol. 168 618 PMID:23005263 |Quinton et al (2010) Isolation and pharmacological characterization of AdTx1, a natural peptide displaying specific insurmountable antagonism of the α1A-adrenoceptor. Br.J.Pharmacol. 159 316 PMID:20015090
动态评分
0.0