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McN - A - 343和二甲基苯基哌嗪对豚鼠心房摄取和释放3H - 去甲肾上腺素的影响。

Effects of McN-A-343 and DMPP on the uptake and release of 3 H-noradrenaline by guinea-pig atria.

作者信息

Allen G S, Rand M J, Story D F

出版信息

Br J Pharmacol. 1972 Jul;45(3):480-9. doi: 10.1111/j.1476-5381.1972.tb08105.x.

Abstract
  1. McN-A-343 4-(m-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium chloride and DMPP (N,N-dimethyl-N'-phenylpiperazinium iodide) inhibit the uptake of (+/-)-(3)H-noradrenaline by guinea-pig atria, being approximately as potent as cocaine in this respect.2. The inhibition of uptake produced by McN-A-343 or DMPP was not affected by atropine or hexamethonium in concentrations which antagonized actions on muscarinic and nicotinic receptors respectively.3. McN-A-343 in the presence of atropine had a positive inotropic action on atria, but this was not accompanied by efflux of radioactivity from atria previously incubated with (-)-(3)H-noradrenaline.4. In the presence of McN-A-343, responses of atria to noradrenaline were increased and those to tyramine were decreased.5. DMPP had positive inotropic and chronotropic actions on atria, and these effects were accompanied by an increase in efflux of radioactivity from atria previously incubated with (-)-(3)H-noradrenaline.
摘要
  1. McN - A - 343(4 - (间氯苯基氨甲酰氧基)- 2 - 丁炔基三甲基氯化铵)和DMPP(N,N - 二甲基 - N'- 苯基哌嗪碘化物)抑制豚鼠心房对(±)-(3)H - 去甲肾上腺素的摄取,在这方面其效力与可卡因大致相当。

  2. McN - A - 343或DMPP产生的摄取抑制作用不受阿托品或六甲铵的影响,这两种药物的浓度分别拮抗对毒蕈碱和烟碱受体的作用。

  3. 在阿托品存在的情况下,McN - A - 343对心房有正性变力作用,但这并未伴随着放射性从先前用(-)-(3)H - 去甲肾上腺素孵育的心房中流出。

  4. 在McN - A - 343存在的情况下,心房对去甲肾上腺素的反应增强,而对酪胺的反应减弱。

  5. DMPP对心房有正性变力和变时作用,这些作用伴随着放射性从先前用(-)-(3)H - 去甲肾上腺素孵育的心房中流出增加。

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Analysis of the cardiovascular responses to McN-A-343 and DMPP in pithed guinea-pigs.
Neuropharmacology. 1980 Nov;19(11):1113-8. doi: 10.1016/0028-3908(80)90110-0.

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1
THE UPTAKE AND RELEASE OF H3-NOREPINEPHRINE BY THE GUINEA-PIG HEART IN VIVO.豚鼠心脏在体对H3-去甲肾上腺素的摄取与释放
Naunyn Schmiedebergs Arch Exp Pathol Pharmakol. 1964 Apr 21;248:85-98. doi: 10.1007/BF00247061.
2
THE UPTAKE OF NORADRENALINE BY THE ISOLATED PERFUSED RAT HEART.去甲肾上腺素在离体灌注大鼠心脏中的摄取
Br J Pharmacol Chemother. 1963 Dec;21(3):523-37. doi: 10.1111/j.1476-5381.1963.tb02020.x.
6
Inhibition of orphenadrine of 3H-dl-noradrenaline and 14C-tyramine uptake in atria.
Eur J Pharmacol. 1969 Feb;5(3):296-8. doi: 10.1016/0014-2999(69)90152-6.

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