RH-3421是一种有效的二氢吡唑杀虫剂，可抑制哺乳动物突触体中游离[Ca2+]和45Ca2+摄取的去极化刺激的上升。

Comparative biochemistry and physiology. Part C, Pharmacology, toxicology & endocrinology Pub Date : 1994-07-01

A Zhang, R A Nicholson

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引用次数: 0

摘要

二氢吡唑RH-3421抑制veratridine-和K(+)-诱导的突触体游离Ca2+升高，ic50分别为0.2和1微米。K(+)诱导的游离突触体Ca2+的升高需要外部Ca2+，在河豚毒素存在下也被RH-3421阻断。K(+)刺激的突触体对45Ca2+的摄取不受河豚毒素的影响，被钴离子阻断，被RH-3421单独(IC50 = 11微米)和存在河豚毒素时抑制。RH-3421不影响非去极化突触体中游离Ca2+或基础45Ca2+摄取的水平。结果表明RH-3421抑制神经末梢电压敏感钙通道。

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RH-3421, a potent dihydropyrazole insecticide, inhibits depolarization-stimulated rises in free [Ca2+] and 45Ca2+ uptake in mammalian synaptosomes.

The dihydropyrazole RH-3421 inhibits veratridine- and K(+)-induced rises in synaptosomal free Ca2+ with IC50s of 0.2 and 1 microM, respectively. The K(+)-induced rise in free synaptosomal Ca2+, which requires external Ca2+, is also blocked by RH-3421 in the presence of tetrodotoxin. The K(+)-stimulated 45Ca2+ uptake by synaptosomes is unaffected by tetrodotoxin, blocked by cobalt ions and inhibited by RH-3421 both alone (IC50 = 11 microM) and in the presence of tetrodotoxin. RH-3421 does not influence the level of free Ca2+ or basal 45Ca2+ uptake in non-depolarized synaptosomes. The results suggest RH-3421 inhibits voltage-sensitive calcium channels in nerve endings.

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Comparative biochemistry and physiology. Part C, Pharmacology, toxicology & endocrinology

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