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甲氧那明可抑制麻醉大鼠的基础和组胺诱导的鼻充血。

Methoxyphenamine inhibits basal and histamine-induced nasal congestion in anaesthetized rats.

作者信息

Lau W A, King R G, Boura A L

机构信息

Department of Pharmacology, Monash University, Clayton, Victoria, Australia.

出版信息

Br J Pharmacol. 1990 Oct;101(2):394-8. doi: 10.1111/j.1476-5381.1990.tb12720.x.

DOI:10.1111/j.1476-5381.1990.tb12720.x
PMID:1701679
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1917682/
Abstract
  1. Nasal resistance in anaesthetized rats was assessed by measuring air overflow during ventilation of the nasal passages at constant pressure. Nasal basal resistance was reduced in a dose-dependent manner by methoxyphenamine hydrochloride (0.01-30 mg kg-1, i.v.), pseudoephedrine hydrochloride (0.03-3 mg kg-1, i.v.) and adrenaline bitartrate (0.01-3 micrograms kg-1, i.v.). Both methoxyphenamine and pseudoephedrine were less potent and less efficacious than adrenaline but caused longer-lasting responses. 2. Nasal congestion induced by histamine (0.2% nebulised solution passed into the nasal passages for 15 s) was inhibited by i.v. administration of methoxyphenamine, pseudoephedrine, adrenaline, methoxamine or tyramine: the ID50s against 0.2% histamine-induced nasal congestion were 1.16 (95% confidence limits; 0.5, 1.8) mg kg-1, 0.25 (0.19, 0.33) mg kg-1, 0.037 (0.018, 0.06) micrograms kg-1, 8.12 (6.74, 9.65) micrograms kg-1 and 30.6 (26.1, 35.8) micrograms kg-1 respectively. 3. The inhibitory effects of both methoxyphenamine and tyramine on histamine-induced nasal congestion were reduced after administration of desmethylimipramine (0.1 and 1 mg kg-1, i.v.) or prazosin (0.1 and 0.3 mg kg-1, i.v.). Similarly, the inhibitory effects of methoxamine were reduced after prazosin (0.1 and 0.3 mg kg-1). 4. These results indicate that methoxyphenamine (1 mg kg-1, i.v.) inhibits histamine-induced nasal congestion in the rat. This action, at least in part, is probably indirect being mediated by release of neuronal noradrenaline which then acts on alpha 1-adrenoceptors.
摘要
  1. 通过在恒定压力下测量鼻道通气期间的空气溢出量来评估麻醉大鼠的鼻阻力。盐酸甲氧那明(0.01 - 30 mg·kg⁻¹,静脉注射)、盐酸伪麻黄碱(0.03 - 3 mg·kg⁻¹,静脉注射)和重酒石酸肾上腺素(0.01 - 3 μg·kg⁻¹,静脉注射)均以剂量依赖性方式降低鼻基础阻力。甲氧那明和伪麻黄碱的效力和效能均低于肾上腺素,但引起的反应持续时间更长。2. 组胺(0.2%雾化溶液通入鼻道15秒)诱导的鼻充血可通过静脉注射甲氧那明、伪麻黄碱、肾上腺素、甲氧明或酪胺来抑制:针对0.2%组胺诱导的鼻充血的半数抑制剂量(ID50)分别为1.16(95%置信限;0.5,1.8)mg·kg⁻¹、0.25(0.19,0.33)mg·kg⁻¹、0.037(0.018,0.06)μg·kg⁻¹、8.12(6.74,9.65)μg·kg⁻¹和30.6(26.1,35.8)μg·kg⁻¹。3. 静脉注射去甲丙咪嗪(0.1和1 mg·kg⁻¹)或哌唑嗪(0.1和0.3 mg·kg⁻¹)后,甲氧那明和酪胺对组胺诱导的鼻充血的抑制作用均减弱。同样,哌唑嗪(0.1和0.3 mg·kg⁻¹)给药后,甲氧明的抑制作用也减弱。4. 这些结果表明,静脉注射1 mg·kg⁻¹的甲氧那明可抑制大鼠组胺诱导的鼻充血。这种作用至少部分可能是间接的,由神经元去甲肾上腺素的释放介导,然后作用于α1肾上腺素能受体。

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