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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2017.1
- 수록면
- 20 - 28 (9page)
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초록· 키워드
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Purpose: The aim of this study was to assess the potential involvement of a specific subtype of 5-hydroxytryptamine (5-HT), 5HT2 receptors in neurally-induced contractions of the human detrusor.
Methods: Contractile responses to electrical field stimulation (EFS) were examined in human isolated urinary bladder muscle strips. The potentiation of EFS-induced detrusor contraction was examined by adding cumulative concentrations of a 5-HT and 5-HT2 receptor agonist, α-methyl-serotonin (α-Me-5-HT) (1nM–100μM) in the presence or absence of a 5-HT2 antagonist, ketanserin (5-HT2A>5-HT2C) or naftopidil (5-HT2B>5-HT2A) (0.3–3μM).
Results: 5-HT and α-Me-5-HT potentiated EFS-induced contraction with a maximal effect (Emax) of 37.6% and 38.6%, respectively, and with pEC50 (negative logarithm of the concentration required for a half-maximal response to an agonist) values of 8.3 and 6.8, respectively. Neither ketanserin nor naftopidil at any concentration produced a rightward displacement of the α-Me-5-HT concentration response curve. Instead, the Emax of α-Me-5-HT increased in the presence of ketanserin at 0.3–1μM and in the presence of naftopidil at 1μM to 51% and 56%, respectively, while the Emax in the presence of vehicle alone was 36%.
The highest concentration (3μM) of either drug, however, fully reversed the enhancement.
Conclusions: The potentiating effect of α-Me-5-HT on neurally-induced contraction of human urinary bladder muscle strips was not found to be mediated via any 5-HT2 receptor subtypes. The underlying mechanism for the enhancement of the α-Me- 5-HT potentiating effect on detrusor contractility by ketanserin and naftopidil remains unknown; however, our results suggest that these drugs may be useful for treating contractile dysfunction of the detrusor, as manifested in conditions such as underactive bladder.
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참고문헌 (24)
참고문헌 신청
Alexander SP / 2015 / The Concise Guide to PHARMACOLOGY 2015/16 : G protein-coupled receptors / Br J Pharmacol 172 : 5744 ~ 5869
Anderson KE / 1993 / Pharmacology of lower urinary tract smooth muscles and penile erectile tissues / Pharmacol Rev 45 : 253 ~ 308
Baxter G / 1995 / 5-HT2 receptor subtypes:a family re-united? / Trends Pharmacol Sci 16 : 105 ~ 110
Campos-Bedolla P / 2006 / Alpha-methyl-5-HT, a 5-HT2 receptor agonist, stimulates beta2-adrenoceptors in guinea pig airway smooth muscle / Pharmacol Res 54 : 468 ~ 473
Candura SM / 1996 / Neural 5-HT4 receptors in the human isolated detrusor muscle: effects of indole, benzimidazolone and substituted benzamide agonists and antagonists / Br J
Anderson KE / 1993 / Pharmacology of lower urinary tract smooth muscles and penile erectile tissues / Pharmacol Rev 45 : 253 ~ 308
Baxter G / 1995 / 5-HT2 receptor subtypes:a family re-united? / Trends Pharmacol Sci 16 : 105 ~ 110
Campos-Bedolla P / 2006 / Alpha-methyl-5-HT, a 5-HT2 receptor agonist, stimulates beta2-adrenoceptors in guinea pig airway smooth muscle / Pharmacol Res 54 : 468 ~ 473
Candura SM / 1996 / Neural 5-HT4 receptors in the human isolated detrusor muscle: effects of indole, benzimidazolone and substituted benzamide agonists and antagonists / Br J
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