Bültmann R, von Kügelgen I, Starke K
Pharmakologisches Institut, Freiburg, Federal Republic of Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1991 Aug;344(2):174-82. doi: 10.1007/BF00167215.
The possible involvement of ATP, in addition to noradrenaline, in nicotine-evoked vasoconstriction was studied in branches of the ileocolic artery of the rabbit. For measurement of vasoconstrictor responses, the arteries were simultaneously incubated and perfused. For measurement of the release of [3H]-noradrenaline, they were preincubated with [3H]-noradrenaline and then superfused. Prazosin (0.1 mumol/l) antagonized the constrictor effect of exogenous noradrenaline but not that of exogenous ATP. Desensitization of P2X-receptors by alpha, beta-methylene ATP markedly attenuated the effect of exogenous ATP but not that of noradrenaline. The presumed P2-purinoceptor antagonist suramin (100 mumol/l) reduced the maximal contraction obtainable with noradrenaline and shifted the concentration-response curve for the constrictor effect of alpha, beta-methylene ATP to the right, but did not change the effect of ATP. Nicotine elicited monophasic vasoconstrictions which faded while nicotine was still in the medium. The concentration-response curve was bell-shaped with an EC50 of 50 mumol/l and a maximal effect at 180 mumol/l, and the exposure time-response curve indicated that responses were maximal after 5 s of contact of nicotine (180 mumol/l) with the tissue. Neither prazosin 0.1 mumol/l nor desensitization by alpha,beta-methylene ATP changed the time course of the response to nicotine, but both depressed the magnitude of the responses over the whole concentration- and exposure time-response curves. The depression was greater with prazosin than with alpha,beta-methylene ATP. Desensitization by alpha,beta-methylene ATP or addition of suramin 100 mumol/l practically abolished the prazosin-resistant part of the response. The effect of nicotine was blocked by hexamethonium as well as by sympathetic denervation by 6-hydroxydopamine.(ABSTRACT TRUNCATED AT 250 WORDS)
除去甲肾上腺素外,还研究了ATP在尼古丁诱发的家兔回结肠动脉分支血管收缩中的可能作用。为测定血管收缩反应,动脉同时进行孵育和灌注。为测定[3H] - 去甲肾上腺素的释放,先将动脉与[3H] - 去甲肾上腺素预孵育,然后进行灌流。哌唑嗪(0.1 μmol/L)可拮抗外源性去甲肾上腺素的收缩作用,但不能拮抗外源性ATP的收缩作用。α,β - 亚甲基ATP对P2X受体的脱敏作用显著减弱了外源性ATP的作用,但不影响去甲肾上腺素的作用。推测的P2 - 嘌呤受体拮抗剂苏拉明(100 μmol/L)降低了去甲肾上腺素可获得的最大收缩幅度,并使α,β - 亚甲基ATP收缩作用的浓度 - 反应曲线右移,但不改变ATP的作用。尼古丁引起单相血管收缩,在尼古丁仍存在于介质中时收缩作用逐渐减弱。浓度 - 反应曲线呈钟形,EC50为50 μmol/L,在180 μmol/L时达到最大效应,暴露时间 - 反应曲线表明,尼古丁(180 μmol/L)与组织接触5秒后反应达到最大。0.1 μmol/L的哌唑嗪或α,β - 亚甲基ATP的脱敏作用均未改变对尼古丁反应的时间进程,但两者均降低了整个浓度 - 暴露时间反应曲线上反应的幅度。哌唑嗪引起的抑制作用比α,β - 亚甲基ATP更大。α,β - 亚甲基ATP的脱敏作用或添加100 μmol/L的苏拉明实际上消除了对哌唑嗪耐药的反应部分。尼古丁的作用被六甲铵以及6 - 羟基多巴胺交感神经去支配所阻断。(摘要截短至250字)