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Titolo:
The involvement of L-type Ca2+ channels in the relaxant effects of the ATP-sensitive K+ channel opener ZD6169 on pig urethral smooth muscle
Autore:
Teramoto, N; Yunoki, T; Ikawa, S; Takano, Z; Tanaka, K; Seki, N; Naito, S; Ito, Y;
Indirizzi:
Kyushu Univ, Grad Sch Med Sci, Dept Pharmacol, Fukuoka 8128582, Japan Kyushu Univ Fukuoka Japan 8128582 Dept Pharmacol, Fukuoka 8128582, Japan Kyushu Univ, Grad Sch Med Sci, Dept Urol, Fukuoka 8128582, Japan Kyushu Univ Fukuoka Japan 8128582 Sci, Dept Urol, Fukuoka 8128582, Japan
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 7, volume: 134, anno: 2001,
pagine: 1505 - 1515
SICI:
0007-1188(200112)134:7<1505:TIOLCC>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
POTASSIUM CHANNELS; OPENING ACTIVITY; CALCIUM-CHANNEL; BLADDER; CELLS; ANTAGONISTS; DETRUSOR; CURRENTS; ANALOGS;
Keywords:
(alpha 1C) subunit; Ca2+ channel blocker; K+ channel opener; voltage-dependent Ca2+ channels; ZD6169;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Teramoto, N Kyushu Univ, Grad Sch Med Sci, Dept Pharmacol, 3-1-1 Maidashi,Higashi Ward, Fukuoka 8128582, Japan Kyushu Univ 3-1-1 Maidashi,Higashi Ward Fukuoka Japan 8128582
Citazione:
N. Teramoto et al., "The involvement of L-type Ca2+ channels in the relaxant effects of the ATP-sensitive K+ channel opener ZD6169 on pig urethral smooth muscle", BR J PHARM, 134(7), 2001, pp. 1505-1515

Abstract

1 The effects of ZD6169, a novel ATP-sensitive K+ channel (K-ATP channel) opener, were investigated on membrane currents in isolated myocytes using patch-clamp techniques. Tension measurement was also performed to study the effects of ZD6169 on the resting tone of pig urethral smooth muscle.2 Levcromakalim was more potent than ZD6169 in lowering the resting urethral tone. Relaxation induced by low concentrations of ZD6169 (less than or equal to3 muM) was completely suppressed by additional application of glibenclamide (1 muM). In contrast, glibenclamide (1-10 muM) only partially inhibited the relaxation induced by higher concentrations of ZD6169 (greater than or equal to 10 muM).3 Bay K8644 (1 muM) reduced the maximum relaxation produced by ZD6169 (greater than or equal to 10 muM).4 In whole-cell configuration, ZD6169 suppressed the peak amplitude of voltage-dependent Ba2+ currents in a concentration- and voltage-dependent manner, and at 100 muM, shifted the steady-state inactivation curve of the voltage-dependent Ba2+ currents to the left at a holding potential of - 90 mv.5 In cell-attached configuration, open probability of unitary voltage-dependent Ba2+ channels (27 pS, 90 mM Ba2+) was inhibited by 100 muM ZD6169 andby 10 muM nifedipine.6 Reverse transcriptase-polymerase chain reaction (RT-PCR) analysis revealed the presence of the transcript of the alpha (1C) subunit of L-type Ca2+ channels in pig urethra.7 These results demonstrate that ZD6169 causes urethral relaxation throughtwo distinct mechanisms, activation of KATP channels at lower concentrations and inhibition of voltage-dependent Ca2+ channels at higher concentrations (about 10 muM).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 02:04:13