The potency of KUL-7211, a selective ureteral relaxant, in isolated canine ureter: comparison with various spasmolytics
| العنوان: | The potency of KUL-7211, a selective ureteral relaxant, in isolated canine ureter: comparison with various spasmolytics |
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| المؤلفون: | Masami Kojima, Yoshitaka Tomiyama, Mariko Tadachi, Mamoru Kobayashi, Nobuo Shibata, Yoshinobu Yamazaki, Isao Wanajo |
| المصدر: | Urological Research. 33:409-414 |
| بيانات النشر: | Springer Science and Business Media LLC, 2005. |
| سنة النشر: | 2005 |
| مصطلحات موضوعية: | Male, Agonist, medicine.medical_specialty, Colic, medicine.drug_class, Muscle Relaxation, Urology, Acetates, In Vitro Techniques, Pharmacology, Dinoprost, Potassium Chloride, Phenylephrine, Dogs, Tamsulosin, Internal medicine, Receptors, Adrenergic, beta, medicine, Prazosin, Animals, Humans, Ureteral Diseases, Phosphodiesterase inhibitor, Papaverine, Chemistry, Antagonist, Parasympatholytics, Muscarinic antagonist, Adrenergic beta-Agonists, Endocrinology, Verapamil, Urinary Calculi, Ureter, Ureteral Obstruction, medicine.drug |
| الوصف: | We compared the potency of a selective ureteral relaxant KUL-7211 (beta(2)/beta(3)-adrenoceptor agonist; (-)-2-[4-(2-{[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino}ethyl)phenyloxy]acetic acid) with those of various spasmolytics on contractions in isolated canine ureteral preparations. Drug effects were evaluated on the tonic contraction induced by KCl (80 mM) and on spontaneous, 1x10(-5) M phenylephrine-, and 1x10(-6) M PGF(2alpha)-induced rhythmic contractions in isolated canine ureteral preparations using a functional experimental technique. The potencies (pD(2) value) of the following drugs were compared: KUL-7211, tamsulosin (an alpha(1A/1D)-adrenoceptor antagonist), prazosin (an alpha(1)-adrenoceptor antagonist), verapamil (a Ca(2+)-channel blocker), butylscopolamine (a nonselective muscarinic antagonist), and papaverine (a phosphodiesterase inhibitor). The rank order of relaxing potencies against KCl-induced tonic contraction was KUL-7211 (6.60)tamsulosin(5.90)verapamil(5.70)papaverine(4.88)prazosin (4.54). The rank order of potencies for reductions in spontaneous rhythmic contractions was KUL-7211 (6.80)verapamil(6.12)papaverine(5.05). Conversely, high concentrations of the two alpha-adrenoceptor antagonists (tamsulosin and prazosin) and of butylscopolamine enhanced the spontaneous contractions, although at low concentrations (up to 1x10(-6) M) they had no significant effects. For suppression of spasmogen-induced rhythmic contractions, the rank order of potencies was, against phenylephrine-induced contractions: KUL-7211 (6.95)tamsulosin(6.26)prazosin(5.68)verapamil(5.64)papaverine (5.03), and against PGF(2alpha)-induced contractions: KUL-7211 (7.05)verapamil(6.70)papaverine (5.27). Our results suggest that in dogs, the beta(2)/beta(3)-adrenoceptor agonist KUL-7211 is the most efficacious ureteral relaxant among the spasmolytics tested against various contractions. Possibly, KUL-7211 might be useful for promoting stone passage and relieving ureteral colic in urolithiasis patients. |
| تدمد: | 1434-0879 0300-5623 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85e8ee4a96371d5a20e7ed1c432be332Test https://doi.org/10.1007/s00240-005-0475-5Test |
| حقوق: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....85e8ee4a96371d5a20e7ed1c432be332 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14340879 03005623 |
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