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γ-氨基丁酸模拟剂对猫脊髓的作用。

Effects of GABA-mimetic agents on the cat spinal cord.

作者信息

Polc P

机构信息

Pharma Research Department F. Hoffman-La Roche & Co. Ltd., Basle, Switzerland.

出版信息

Prog Neuropsychopharmacol. 1979;3(4):345-52. doi: 10.1016/0364-7722(79)90045-6.

Abstract

Muscimol, ibotenic acid, isoguvacine, 4,5,6,7-tetrahydroisoxazolo [5,4-c]pyridin-3-ol (THIP) and gamma-aminobutyric acid (GABA) injected intravenously exerted the following dose-dependent effects on the lumbosacral spinal cord of spinal cats: 1. The excitability of primary afferents and the amplitude of dorsal root reflexes were enhanced; segmental monosynaptic ventral root reflexes and dorsal root potentials as well as the spontaneous gamma-fibre activity and, to a smaller extent, the excitability of motoneurons and polysynaptic reflexes, were depressed. 2. Muscimol was the most potent compound (0.3-1 mg/kg produced significant effects), followed by ibotenic acid (3-10 mg/kg), isoguvacine and THIP (10-30 mg/kg) and GABA (100 mg/kg). 3. Most effects were reversibly antagonized by bicuculline, but not by strychnine, indicating that they were due to a specific interaction with GABA-receptors. 4. These results suggest that the systemic injection of GABA-mimetic agents affects spinal cord activities by actions related to GABA-receptors located on primary afferent endings, intrinsic spinal neurons, and motoneurons.

摘要

静脉注射蝇蕈醇、鹅膏蕈氨酸、异鹅膏蕈氨酸、4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇(THIP)和γ-氨基丁酸(GABA)对脊髓猫的腰骶脊髓产生了以下剂量依赖性效应:1. 初级传入神经的兴奋性和背根反射的幅度增强;节段性单突触腹根反射和背根电位以及自发γ纤维活动,以及在较小程度上运动神经元的兴奋性和多突触反射受到抑制。2. 蝇蕈醇是最有效的化合物(0.3 - 1 mg/kg产生显著效应),其次是鹅膏蕈氨酸(3 - 10 mg/kg)、异鹅膏蕈氨酸和THIP(10 - 30 mg/kg)以及GABA(100 mg/kg)。3. 大多数效应可被荷包牡丹碱可逆性拮抗,但不能被士的宁拮抗,表明它们是由于与GABA受体的特异性相互作用所致。4. 这些结果表明,全身性注射GABA模拟剂通过与位于初级传入神经末梢、脊髓固有神经元和运动神经元上的GABA受体相关的作用来影响脊髓活动。

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