Functional and molecular biological evidence for a possible β 3 -adrenoceptor in the human detrusor muscle
| Autor: | Yoshinobu Yamazaki, Takehisa Yoneyama, Karl-Erik Andersson, Osamu Nishizawa, Yasuhiko Igawa, Hiroo Takeda, Kohichi Hayakawa, Yukiyoshi Ajisawa, Masuo Akahane |
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| Rok vydání: | 1999 |
| Předmět: |
Pharmacology
Detrusor muscle Beta-3 adrenergic receptor medicine.medical_specialty Forskolin Chemistry Antagonist Adrenergic musculoskeletal system chemistry.chemical_compound medicine.anatomical_structure Endocrinology Muscle relaxation Isoprenaline Internal medicine medicine Receptor medicine.drug |
| Zdroj: | British Journal of Pharmacology. 126:819-825 |
| ISSN: | 0007-1188 |
| Popis: | The possible existence of a beta3-adrenergic receptor (beta3-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD2 6.37+/-0.07) > or = noradrenaline (pD2 6.07+/-0.12) > or = adrenaline (pD2 5.88 M) and its pKB value was 5.71+/-0.19. Moreover, SR58894A (10(-7) - 10(-5) M), a beta3-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA2 value and slope obtained from Schild plots were 6.24+/-0.20 and 0.68+/-0.31. The beta1-, beta2- and beta3-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay. In conclusion, the present results provide the first evidence for the existence of the beta3-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusor is mediated mainly through beta3-AR activation. |
| Databáze: | OpenAIRE |
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