The aim of this study was to characterize endothelin receptor subtypes of the detrusor muscle of the human urinary bladder. The receptor subtypes mediating endothelin (ET)-1-induced activity in the human detrusor smooth muscles have been characterized using isometric contraction and reverse transcription–polymerase chain reaction (RT–PCR). ET-1 (a non-selective ET receptor agonist; 10-10 M to 10-6 M) exhibited concentration-dependent contractions in human urinary bladder with a plateau at concentrations above 3×10-7 M. Neither IRL1620 nor sarafotoxin S6c (both ETB-selective agonists; 10-10 M to 10-6 M) elicited contractile activity in the human urinary bladder detrusor smooth muscle. FR139317 (an ETA-selective antagonist; 10-7 M to 10-5 M) produced a marked shift to the right of the ET-1 concentration–response curve in human urinary bladder detrusor smooth muscle (from the Schild plot TpA2 = 7.96; slope = 0.95). In contrast, RES701-1 (an ETB-selective antagonist; 10-7 M to 10-5 M) had no effect on the ET-1 concentration–response curve. RT–PCR revealed positive amplification of ETA receptor mRNA fragment, but not ETB. These results indicate that the ET-1-induced contractile effects of urinary bladder detrusor smooth muscle seem to be mediated mainly by the ETA receptor, not by the ETB receptor.
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April 1999
Research Article|
April 01 1999
Pharmacological and molecular biological evidence for ETA endothelin receptor subtype mediating mechanical responses in the detrusor smooth muscle of the human urinary bladder
Takako OKAMOTO-KOIZUMI;
Takako OKAMOTO-KOIZUMI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Masayuki TAKEDA;
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Correspondence: Dr M. Takeda.
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Takeshi KOMEYAMA;
Takeshi KOMEYAMA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Akihiko HATANO;
Akihiko HATANO
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Makoto TAMAKI;
Makoto TAMAKI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Takaki MIZUSAWA;
Takaki MIZUSAWA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Toshiki TSUTSUI;
Toshiki TSUTSUI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Kenji OBARA;
Kenji OBARA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Yoshihiko TOMITA;
Yoshihiko TOMITA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Kei ARAI;
Kei ARAI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Kota TAKAHASHI
Kota TAKAHASHI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
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Clin Sci (Lond) (1999) 96 (4): 397–402.
Citation
Takako OKAMOTO-KOIZUMI, Masayuki TAKEDA, Takeshi KOMEYAMA, Akihiko HATANO, Makoto TAMAKI, Takaki MIZUSAWA, Toshiki TSUTSUI, Kenji OBARA, Yoshihiko TOMITA, Kei ARAI, Kota TAKAHASHI; Pharmacological and molecular biological evidence for ETA endothelin receptor subtype mediating mechanical responses in the detrusor smooth muscle of the human urinary bladder. Clin Sci (Lond) 1 April 1999; 96 (4): 397–402. doi: https://doi.org/10.1042/cs0960397
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