Kennedy C, Burnstock G
Eur J Pharmacol. 1985 Apr 23;111(1):49-56. doi: 10.1016/0014-2999(85)90112-8.
The actions of ATP, 2-methylthioATP, alpha, beta-methyleneATP, beta, gamma-methyleneATP, adenosine and non-adrenergic, non-cholinergic inhibitory nerve stimulation were compared on the ergotamine-contracted longitudinal muscle of the isolated rabbit portal vein with the vessel endothelium either intact or removed by mechanical rubbing. Non-adrenergic, non-cholinergic inhibitory nerve stimulation produced frequency-dependent relaxations. The purines (except alpha, beta-methyleneATP) also caused relaxation with the following potency order: 2-methylthioATP greater than ATP greater than beta, gamma-methyleneATP = adenosine. 8-Phenyltheophylline, a potent P1-purinoceptor antagonist, antagonised relaxations to adenosine but not those to ATP indicating that ATP and its analogues act directly via a P2-purinoceptor and not via a P1-purinoceptor after breakdown to adenosine. alpha, beta-MethyleneATP produced contractions which were not maintained and was tachyphylactic. The contractions were unaffected by tetrodotoxin and therefore unlikely to be due to release of a contractile substance from a neuronal source following initiation of an action potential. Removal of the endothelium did not affect the actions of non-adrenergic, non-cholinergic inhibitory nerve stimulation, ATP, alpha, beta-methyleneATP, beta, gamma-methyleneATP or adenosine. Thus purine action does not have an endothelium-dependent component in the rabbit portal vein longitudinal muscle. The results indicate the possibility that there may be more than one type of P2-purinoceptor in this tissue.
在分离的兔门静脉麦角胺收缩的纵行肌上,比较了ATP、2-甲硫基ATP、α,β-亚甲基ATP、β,γ-亚甲基ATP、腺苷以及非肾上腺素能、非胆碱能抑制性神经刺激的作用,该血管内皮完整或通过机械摩擦去除。非肾上腺素能、非胆碱能抑制性神经刺激产生频率依赖性舒张。嘌呤(α,β-亚甲基ATP除外)也引起舒张,其效力顺序如下:2-甲硫基ATP>ATP>β,γ-亚甲基ATP = 腺苷。8-苯基茶碱是一种强效P1嘌呤受体拮抗剂,可拮抗对腺苷的舒张作用,但不拮抗对ATP的舒张作用,这表明ATP及其类似物在分解为腺苷后直接通过P2嘌呤受体而非P1嘌呤受体起作用。α,β-亚甲基ATP产生的收缩不能持续且有快速耐受性。这些收缩不受河豚毒素影响,因此不太可能是由于动作电位引发后从神经源释放收缩物质所致。去除内皮不影响非肾上腺素能、非胆碱能抑制性神经刺激、ATP、α,β-亚甲基ATP、β,γ-亚甲基ATP或腺苷的作用。因此,在兔门静脉纵行肌中,嘌呤作用不存在内皮依赖性成分。结果表明,该组织中可能存在不止一种类型的P2嘌呤受体。