DIFFERENTIAL REGULATION OF CENTRAL AND PERIPHERAL BENZODIAZEPINE BINDING-SITES IN THE RAT OLFACTORY-BULB

DIFFERENTIAL REGULATION OF CENTRAL AND PERIPHERAL BENZODIAZEPINE BINDING-SITES IN THE RAT OLFACTORY-BULB
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DOI:
10.1016/0014-2999(84)90658-7
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发表时间:
1984-01-01
影响因子:
5
通讯作者:
SKOLNICK, P
SKOLNICK, P
中科院分区:
医学2区
文献类型:
--
作者:
BOLGER, GT;MEZEY, E;SKOLNICK, P

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在嗅球手术分离后19-21天和27-31天检查[3 H]氟硝西泮和[3 H]Ro 5-4864 [4“-氯地西泮]结合位点的密度。虽然在两个时间间隔在嗅球中观察到[3 H]氟硝珠结合的统计学显著性降低,但仅在术后27-31天观察到[3 H]Ro 5-4864结合的显著性降低。在小脑中未观察到任何放射性配体结合的一致变化。 嗅球摘除导致Ro 5-4864的惊厥效力(但不是效力)显著降低,而戊四唑的效力和效力均不受该程序的影响。苯二氮卓受体和苯二氮卓类的外周型结合位点显然是独立调节的,并且外周型结合位点的至少一个亚群与嗅球中的神经元元素相关。嗅球中苯二氮卓类药物的外周型结合位点可能影响Ro 5-4864的诱导作用。
The density of [3H]flunitrazepam and [3H]Ro 5-4864 [4''-chlorodiazepam] binding sites was examined 19-21 and 27-31 days after surgical isolation of the olfactory bulbs. While statistically significant reductions in [3H]flunitrazpeam binding were observed in the olfactory bulbs at both intervals, a significant reduction in [3H]Ro 5-4864 binding was observed only at 27-31 days after surgery. No consistent changes in the binding of either radioligand were observed in cerebella. Extirpation of the olfactory bulbs resulted in a significant reduction in the convulsant potency (but not efficacy) of Ro 5-4864, while neither the potency nor efficacy of pentylenetetrazole was affected by this procedure. Benzodiazepine receptors and peripheral-type binding sites for benzodiazepines are apparently regulated independently, and at least a subpopulation of peripheral-type binding sites are associated with neuronal elements in the olfactory bulb. Peripheral-type binding sites for benzodiazepines in the olfactory bulbs may influence the consulvant actions of Ro 5-4864.