CHARACTERIZATION OF KININ RECEPTORS MODULATING NEUROGENIC CONTRACTIONS OF THE MOUSE ISOLATED VAS-DEFERENS

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dc.contributor.authorMAAS, J
dc.contributor.authorRAE, GA
dc.contributor.authorHUIDOBROTORO, JP
dc.contributor.authorCALIXTO, JB
dc.date.accessioned2025-01-21T01:34:54Z
dc.date.available2025-01-21T01:34:54Z
dc.date.issued1995
dc.description.abstract1 This study analyses the receptors mediating the effects of bradykinin (BK) and analogues on neurogenic twitch contractions of the mouse isolated vas deferens evoked, in the presence of captopril (3 mu M), by electrical field stimulation with trains of 4 rectangular 0.5 ms pulses of supramaximal strength, delivered at a frequency of 10 Hz every 20 s.
dc.description.abstract2 BK (0.1 - 300 nM) induced a graded potentiation of twitches, with an EC(50) (geometric mean and 95% confidence limits) of 4.5 nM (1.7-11.6) and an E(max) of 315 +/- 19 mg per 10 mg of wet tissue (n = 6). Similar results were obtained in tissues challenged with Lys-BK, [Hyp(3)]-BK, Met,Lys-BK and the selective Bz receptor agonist [Tyr(Me)8]-BK (0.1-300 nM).
dc.description.abstract3 The selective B-2 receptor antagonists, Hoe 140 (1-10 nM) and NPC 17731 (3-30 nM), caused graded rightward shifts df the curve to BK-induced twitch potentiation, yielding apparent pA(2) values of 9.65 +/- 0.09 and 9.08 +/- 0.13, respectively, and Schild plot slopes not different from 1. Both antagonists (100 nM) failed to modify similar twitch potentiations induced by substance P (3 nM) or endothelin-1 (1 nM). Preincubation with the selective B-1 receptor antagonist, [Leu(8),des-Arg(9)]-BK (1 mu M), increased the potentiating effect of BK on twitches at 30-300 nM.
dc.description.abstract4 In contrast to BK, the selective B-1 receptor agonist, [des-Arg(9)]-BK (0.3-1000 nM) reduced the amplitude of twitches in a graded fashion, with an IC50 of 13.7 nM (10.4-16.1) and an I-max of 175 +/- 11 mg (n = 4). The twitch depression induced by [des-Arg(9)]-BK (300 nM) was not affected by Hoe 140 (30 nM) or NPC 17731 (100 nM), but was abolished by the selective B-1 receptor antagonist, [Leu(8),des-Arg(9)]-BK (1 mu M), which did not modify the twitch inhibitory effect of clonidine (1 nM) or morphine (300 nM).
dc.description.abstract5 In non-stimulated preparations, BK (100 nM) also potentiated, in a Hoe 140-sensitive (10 nM) manner, the contractions induced by ATP (100 mu M), but not by noradrenaline (10 mu M), whereas [des-Arg(9)]-BK (300 nM) did not modify the contractions induced by either agonist.
dc.description.abstract6 It is concluded that the mouse vas deferens expresses both B-1 and B-2 receptors, which modulate sympathetic neurotransmission in opposing ways. Neurogenic contractions are inhibited by stimulation of possibly prejunctional B-1 receptors, whereas activation of B-2 receptors increases twitch contractions, in part by amplifying the responsiveness of the smooth muscle cells to the sympathetic co-transmitter ATP.
dc.fuente.origenWOS
dc.identifier.issn0007-1188
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/97617
dc.identifier.wosidWOS:A1995QR09900022
dc.issue.numero7
dc.language.isoen
dc.pagina.final1477
dc.pagina.inicio1471
dc.revistaBritish journal of pharmacology
dc.rightsacceso restringido
dc.subjectBRADYKININ
dc.subjectB-1 RECEPTORS
dc.subjectB-2 RECEPTORS
dc.subjectMOUSE VAS DEFERENS
dc.subjectNEUROTRANSMISSION
dc.subjectBRADYKININ ANTAGONIST
dc.subjectHOE 140
dc.subjectNPC 17731
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleCHARACTERIZATION OF KININ RECEPTORS MODULATING NEUROGENIC CONTRACTIONS OF THE MOUSE ISOLATED VAS-DEFERENS
dc.typeartículo
dc.volumen114
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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