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1.
Gen Pharmacol ; 27(3): 525-8, 1996 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-8723538

RESUMO

1. Clonidine 0.5 mM induced an extremely regular rhythmic activity in isolated rabbit anococcygeus muscle. The movements were resistant to tetrodotoxin effect. 2. Prazosin (5 x 10(-8)M-5 x 10(-6)M) and yohimbine (1.5 x 10(-7)M-5 x 10(-4)M) showed no remarkable effect on clonidine-induced rhythmic activity. 3. The clonidine-induced contractions were dependent on extracellular calcium and could be inhibited by the omission of calcium from medium or the introduction of verapamil (IC50 = 1.3 x 10(-7)M) or nifedipine (IC50 = 7.5 x 10(-8)M). 4. Pretreatment of animals with reserpine made the preparations 2800-fold more sensitive to this action of clonidine. 5. It can be concluded from this study that clonidine is able to induce rhythmic activity in rabbit anococcygeus muscle through a mechanism that increases intracellular concentration of Ca++ via membrane calcium channels.


Assuntos
Agonistas alfa-Adrenérgicos/farmacologia , Clonidina/farmacologia , Músculo Liso/efeitos dos fármacos , Inibidores da Captação Adrenérgica/farmacologia , Agonistas de Receptores Adrenérgicos alfa 2 , Animais , Cálcio/fisiologia , Bloqueadores dos Canais de Cálcio/farmacologia , Feminino , Técnicas In Vitro , Masculino , Contração Muscular/efeitos dos fármacos , Coelhos , Reserpina/farmacologia , Tetrodotoxina/farmacologia
2.
Gen Pharmacol ; 24(4): 841-5, 1993 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-7901113

RESUMO

1. Methoxamine 0.5 microns induced an extremely regular rhythmic activity in isolated rabbit anococcygeus muscle. 2. Prazosin had an inhibitory effect on methoxamine-induced rhythmic contractions. IC50 of prazosin was 7.94 nM. 3. The methoxamine-induced contractions are dependent on extracellular calcium and can be inhibited by the omission of calcium from media or the introduction of verapamil (IC50 = 0.11 microM) or nifedipine (IC50 = 0.21 microM). 4. Application of reserpine made the preparations 40-fold more sensitive to methoxamine. 5. It can be concluded that rhythmic contractions produced by methoxamine are mediated through stimulatory action of methoxamine on alpha-I adrenoceptors and depend on extracellular calcium. 6. Lithium made the muscle more sensitive to methoxamine action. In preincubated muscles with 1, 3 and 5 mM lithium the initiation of contractions occurred at 1.5 x 10(-7), M, 5 x 10(-8) M and 1.5 x 10(-8) M of methoxamine, respectively.


Assuntos
Metoxamina/farmacologia , Músculo Liso/efeitos dos fármacos , Agonistas alfa-Adrenérgicos/farmacologia , Animais , Cálcio/deficiência , Cálcio/fisiologia , Bloqueadores dos Canais de Cálcio/farmacologia , Feminino , Técnicas In Vitro , Lítio/farmacologia , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso/inervação , Músculo Liso/metabolismo , Fosfatidilinositóis/metabolismo , Prazosina/farmacologia , Coelhos , Receptores Adrenérgicos alfa 1/efeitos dos fármacos , Reserpina/farmacologia
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