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.
Skip Nav Destination
Article navigation
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
Search for other works by this author on:
Masayuki TAKEDA;
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Correspondence: Dr M. Takeda.
Search for other works by this author on:
Takeshi KOMEYAMA;
Takeshi KOMEYAMA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Akihiko HATANO;
Akihiko HATANO
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Makoto TAMAKI;
Makoto TAMAKI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Takaki MIZUSAWA;
Takaki MIZUSAWA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Toshiki TSUTSUI;
Toshiki TSUTSUI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Kenji OBARA;
Kenji OBARA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Yoshihiko TOMITA;
Yoshihiko TOMITA
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Kei ARAI;
Kei ARAI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Kota TAKAHASHI
Kota TAKAHASHI
1Department of Urology, Niigata University, School of Medicine, Asahimachi 1, Niigata 951–8510, Japan
Search for other works by this author on:
Publisher: Portland Press Ltd
Online ISSN: 1470-8736
Print ISSN: 0143-5221
The Biochemical Society and the Medical Research Society © 1999
1999
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
Download citation file:
Sign in
Don't already have an account? Register
Sign in to your personal account
You could not be signed in. Please check your email address / username and password and try again.
Captcha Validation Error. Please try again.