General pharmacology · 1999
Age-related change of the role of alpha1L-adrenoceptor in canine urethral smooth muscle.
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Suzuki Y, Moriyama N, Okaya Y, Nishimatsu H, Kawabe K, Aisaka K
Аннотация
To examine age-related alteration of the role of alpha1L-adrenoceptor in the urethra, young non-parous and aged parous female dogs were used. In a functional study, we evaluated phenylephrine-induced contraction and antagonistic effects of JTH-601, a newly synthesized alpha1-adrenoceptor antagonist, and prazosin; in a localization survey using autoradiographic technique, we investigated specific [3H]JTH-601 and [3H]tamsulosin binding. Concentration-response curves were obtained for phenylephrine (pD2 = 5.0-5.3). JTH-601 and prazosin antagonized this contraction with pA2 values of 8.2-8.3 and 8.0-8.1, respectively. Specific binding of both [3H]JTH-601 and [3H]tamsulosin were observed in the bladder neck and proximal section of urethra. There were no significant differences of the pD2, pA2, and radio ligand binding between young non-parous and aged parous dogs.
Предметные рубрики MeSH
Adrenergic alpha-1 Receptor AntagonistsAdrenergic alpha-AntagonistsAgingAnimalsAutoradiographyBinding, CompetitiveCresolsDogsDose-Response Relationship, DrugFemaleIn Vitro TechniquesMuscle ContractionMuscle, SmoothParityPhentolaminePhenylephrinePrazosinReceptors, Adrenergic, alpha-1SulfonamidesTamsulosinUrethraVasoconstrictor Agents