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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Benzodiazepine receptor affinities, behavioral, and anticonvulsant activity of 2-aryl-2,5-dihydropyridazino(4,3-b)indol- 3(3H)-ones in mice.
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Benzodiazepine receptor affinities, behavioral, and anticonvulsant activity of 2-aryl-2,5-dihydropyridazino(4,3-b)indol- 3(3H)-ones in mice.

机译：苯二氮卓受体亲和力，行为和抗惊厥活性的2-芳基-2,5-二氢吡啶并（4,3-b）吲哚-3（3H）-在小鼠中。

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摘要

The anticonvulsant properties of 1,4-benzodiazepines (BDZs), pyrazoloquinolones (CGS), 2-aryl-2,5-dihydropyridazino[4, 3-b]indol-3(3H)-ones (PIs) 1 1i 1d 1f 1e 1b 1c 1h, and 1a, the latter being inactive against audiogenic seizures. Some PIs 1 and abecarnil showed anticonvulsant properties against seizures induced by PTZ with a potency lower than that observed in audiogenic seizures. The pharmacological actions of 1d, 1f, and 1i were significantly reduced by a treatment with flumazenil (8.24 micromol/kg IP), suggesting a clear involvement of benzodiazepine mechanisms in the anticonvulsant activity of these compounds or their metabolites. The anticonvulsant activity of 1d, 1f, and 1i was also evaluated against seizures induced by two beta-carbolines namely methyl-beta-carboline-3-carboxylate (beta-CCM) and methyl-6, 7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM), in DBA/2 mice: they gave better protection against seizures induced by beta-CCM than the ones by DMCM. The potency of various BDZs and PIs as inhibitors of specific [3H]flumazenil binding to neuronal membranes, was also evaluated. The radioligand binding study, carried out on stable cell lines expressing definite combinations of benzodiazepine receptor subunits, demonstrated that 1b, 1e, 1d, and 1h have preferential interaction with alpha(1), beta(3), gamma(2), receptor subtypes.
机译：1,4-苯并二氮杂卓（BDZs），吡唑并喹诺酮类（CGS），2-芳基-2,5-二氢吡啶并[4，3-b]吲哚-3（3H）-ones（PIs）1的抗惊厥特性1 1i 1d 1f 1e 1b 1c 1h和1a，后者对音源性癫痫发作无效。一些PIs 1和阿贝卡尼对PTZ诱发的癫痫发作表现出抗惊厥作用，其效力低于音源性癫痫发作。氟马西尼（8.24 micromol / kg IP）处理可显着降低1d，1f和1i的药理作用，表明苯二氮卓机制明显参与了这些化合物或其代谢产物的抗惊厥活性。还评估了1d，1f和1i的抗惊厥活性，以对抗由两种β-咔啉（甲基-β-咔啉-3-羧酸盐（β-CCM）和甲基-6、7-二甲氧基-4-乙基-β）诱发的癫痫发作-DBA / 2小鼠体内的-carboline-3-羧酸盐（DMCM）：与DMCM相比，它们对β-CCM引起的癫痫发作具有更好的保护作用。还评估了各种BDZ和PI作为特异性[3H]氟马西尼与神经元膜结合的抑制剂的效力。在表达苯并二氮杂receptor受体亚基明确组合的稳定细胞系上进行的放射性配体结合研究表明1b，1e，1d和1h与α（1），β（3），γ（2）受体亚型具有优先相互作用。

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