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Titolo:
Functional and molecular biological evidence for a possible beta(3)-adrenoceptor in the human detrusor muscle
Autore:
Igawa, Y; Yamazaki, Z; Takeda, H; Hayakawa, K; Akahane, M; Ajisawa, Y; Yoneyama, T; Nishizawa, O; Andersson, KE;
Indirizzi:
Shinshu Univ, Sch Med, Dept Urol, Matsumoto, Nagano 3908621, Japan ShinshuUniv Matsumoto Nagano Japan 3908621 sumoto, Nagano 3908621, Japan Kissei Pharmaceut Co Ltd, Div Discovery Res, Nagano 3998304, Japan Kissei Pharmaceut Co Ltd Nagano Japan 3998304 Res, Nagano 3998304, Japan Univ Lund Hosp, Dept Clin Pharmacol, S-22185 Lund, Sweden Univ Lund Hosp Lund Sweden S-22185 Clin Pharmacol, S-22185 Lund, Sweden
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 3, volume: 126, anno: 1999,
pagine: 819 - 825
SICI:
0007-1188(199902)126:3<819:FAMBEF>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENOCEPTOR SUBTYPES; URINARY-BLADDER; BETA-3-ADRENERGIC RECEPTOR; ALPHA-ADRENOCEPTORS; MESSENGER-RNA; RAT; RELAXATION; DOBUTAMINE; RABBIT; PIG;
Keywords:
human bladder; beta-adrenoceptor subtypes; functional analysis; mRNA analysis;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Igawa, Y Shinshuapanv, Sch Med, Dept Urol, 3-1-1 Asahi, Matsumoto, Nagano 3908621, J Shinshu Univ 3-1-1 Asahi Matsumoto Nagano Japan 3908621 908621, J
Citazione:
Y. Igawa et al., "Functional and molecular biological evidence for a possible beta(3)-adrenoceptor in the human detrusor muscle", BR J PHARM, 126(3), 1999, pp. 819-825

Abstract

1 The possible existence of a beta(3)-adrenergic receptor (beta(3)-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression.2 Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD(2) 6.37 +/- 0.07) greater than or equal to noradrenaline (pD(2) 6.07 +/- 0.12) greater than or equal to adrenaline (pD(2) 5.88 +/- 0.11).3 Neither dobutamine (beta(1)- and beta(2)-AR agonist) nor procaterol (beta(2)-AR agonist) produced any significant relaxation at concentrations up to 10(-5) M. BRL37344A, CL316243 and CGP-12177A (beta(3)-AR agonists), relaxed the preparations significantly at concentrations higher than 10(-6) M. The pot values for BRL37344A, CL316243 and CGP-12177A were 6.42 +/- 0.25, 5.53 +/- 0.09 and 5.74 +/- 0.14, respectively.4 CGP-20712A (10(-7)-10(-5) M), a beta(1)-AR antagonist, did not affect the isoprenaline-induced relaxation. On the other hand, ICI-118,551, a beta(2)-AR antagonist, produced a rightward parallel shift of the concentration-relaxation curve for isoprenaline only at the highest concentration used (10(-5) M) and its pK(B) value was 5.71 +/- 0.19. Moreover, SR58894A (10(-7)-10(-5) M), a beta(3)-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA(2) value and slope obtained from Schild plots were 6.24 +/- 0.20 and 0.68 +/- 0.31.5 The beta(1)-, beta(2)- and beta(3)-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay.6 In conclusion, the present results provide the first evidence for the existence of the beta(3)-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusoris mediated mainly through beta(3)-AR activation.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/09/20 alle ore 20:22:42