Fedan J S, Hogaboom G K, O'Donnell J P, Colby J, Westfall D P
Eur J Pharmacol. 1981 Jan 5;69(1):41-53. doi: 10.1016/0014-2999(81)90600-2.
The specific purine-receptor antagonist, arylazido aminopropionyl ATP (ANAPP3), was used to determine if purines released from nerves of the guinea-pig was deferens contribute to the neurogenic response. ANAPP3, which is a photoaffinity label, antagonized contractile responses of the in vitro vas deferens to transmural stimulation, reversibly in the presence of the compound and irreversibly after its photoactivation in the presence of the tissues. The antagonism by ANAPP3 was augmented by depletion of norepinephrine produced by reserpine pretreatment. Responses of untreated tissues were only slightly antagonized by the alpha-adrenoceptor blocker prazosin. However, neurogenic responses were markedly reduced in the combined presence of ANAPP3 and prazosin. ANAPP3 did not affect the release of tritium from tissues prelabeled with [3H]norepinephrine. The initial phasic component of the neurogenic response was preferentially antagonized by ANAPP3 whereas the secondary more tonic component of the response was preferentially antagonized by prazosin and reserpine pretreatment. Small, residual responses remaining after chemical sympathectomy produced by 6-hydroxydopamine pretreatment were potentiated, rather than inhibited, by ANAPP3 and were, unlike untreated tissues, sensitive to atropine. These and previous findings indicate that ATP or a related purine, originating from adrenergic neurons, acts as a co-transmitter with norepinephrine in this tissue.
使用特异性嘌呤受体拮抗剂芳基叠氮氨基丙酰ATP（ANAPP3）来确定豚鼠输精管神经释放的嘌呤是否有助于神经源性反应。ANAPP3是一种光亲和标记物，它能拮抗离体输精管对跨壁刺激的收缩反应，在化合物存在时这种拮抗作用是可逆的，而在组织存在时经光激活后则是不可逆的。利血平预处理导致去甲肾上腺素耗竭会增强ANAPP3的拮抗作用。未处理组织的反应仅被α-肾上腺素能受体阻滞剂哌唑嗪轻微拮抗。然而，在ANAPP3和哌唑嗪同时存在时，神经源性反应会显著降低。ANAPP3不影响预先用[3H]去甲肾上腺素标记的组织中氚的释放。ANAPP3优先拮抗神经源性反应的初始相成分，而反应的继发性更强的紧张性成分则优先被哌唑嗪和利血平预处理所拮抗。6-羟基多巴胺预处理导致化学性交感神经切除后残留的小反应，被ANAPP3增强而非抑制，并且与未处理组织不同，对阿托品敏感。这些以及先前的研究结果表明，源自肾上腺素能神经元的ATP或相关嘌呤在该组织中作为去甲肾上腺素的共递质发挥作用。
