Relaxation of human detrusor muscle by selective beta-2 and beta-3 agonists and endogenous catecholamines
| Autor: | Sun-Tscheol Kwon, Jasmin Katrin Badawi, Sigrun Langbein, Patrick Honeck, Stephan Bross, Hatice Uecelehan, Tobias Seja |
|---|---|
| Přispěvatelé: | Urology |
| Jazyk: | angličtina |
| Rok vydání: | 2007 |
| Předmět: |
Beta-3 adrenergic receptor
Detrusor muscle Agonist Male medicine.medical_specialty medicine.drug_class Urology Muscle Relaxation Terbutaline Urinary Bladder Endogeny In Vitro Techniques Phenoxyacetates Phenoxypropanolamines Propanolamines Catecholamines Internal medicine Isoprenaline medicine Potency Humans Clenbuterol Aged Dose-Response Relationship Drug business.industry Isoproterenol Muscle Smooth Adrenergic beta-Agonists medicine.anatomical_structure Endocrinology Ethanolamines Female business medicine.drug |
| Zdroj: | Urology, 69(4), 785-790. Elsevier Inc. |
| ISSN: | 0090-4295 |
| Popis: | Objectives The goal of this study was to identify potent relaxant agents of the human detrusor muscle. Therefore, the relaxant effects of different selective beta (β)-adrenoceptor agonists were examined. Also, the relaxant effects of the endogenous catecholamines were investigated to functionally characterize the β-adrenoceptor subtype mainly responsible for adrenergic-mediated relaxation in the detrusor muscle of humans. Methods Experiments were performed on muscle strips of human detrusor suspended in a tissue bath. The tissue originated from patients who had undergone total cystectomy. The selective β3-agonists BRL 37344, ZD 7114, and CGP 12177, the selective β2-agonists terbutaline and clenbuterol, and the nonselective β-agonist isoprenaline were investigated. Concentration-relaxation curves of the catecholamines were performed to determine the rank order of potency. Results The maximal relaxation induced by BRL 37344, ZD 7114, and CGP 12177 was 36%, 39%, and 37%, respectively. The corresponding pD2 values were 6.73, 4.82, and 6.09, respectively. Terbutaline and clenbuterol induced a maximal relaxation of 48% and 27%, and their pD2 value was 4.97 and 5.34, respectively. Isoprenaline, adrenaline, and noradrenaline induced a maximal relaxation of 72%, 58%, and 79%, respectively. The corresponding pD2 values were 6.18, 6.16, and 6.09, respectively. Because their differences were not significant, no rank order of potency was determined. Conclusions β-Adrenergic agonists are potent relaxant agents of the human detrusor muscle in vitro. Both β2 and β3-adrenoceptors contribute to adrenergic-mediated relaxation. Our results point to a slightly greater role for the β3-receptor in human detrusor muscle. |
| Databáze: | OpenAIRE |
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