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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Paton D M, Olsson R A

Department of Oral Biology, Faculty of Dentistry, University of Alberta, Edmonton, Canada.

J Auton Pharmacol. 1991 Apr;11(2):85-91. doi: 10.1111/j.1474-8673.1991.tb00247.x.

The potencies of a series of N6-substituted secondary and tertiary alkyladenosine analogues as inhibitors of the twitch responses of isolated guinea-pig ileum stimulated at 0.2 Hz have been determined. 2. All the analogues tested were full agonists. 3. Since their inhibitory effects were antagonized by theophylline and they had no significant effect on responses of ileum to carbachol, it was concluded that they acted predominantly by causing presynaptic inhibition of transmitter release. 4. Their structure-activity relationships indicated that the S4 subregion of the adenosine receptor in this tissue is capacious enough to accommodate a methyl group while the nature of the secondary alkyl moiety appears to determine the degree to which the tertiary methyl group reduces activity.

已测定了一系列N6-取代的仲烷基和叔烷基腺苷类似物作为0.2Hz刺激的离体豚鼠回肠抽搐反应抑制剂的效力。2. 所有测试的类似物都是完全激动剂。3. 由于它们的抑制作用被茶碱拮抗，且对回肠对卡巴胆碱的反应无显著影响，因此得出结论，它们主要通过引起递质释放的突触前抑制起作用。4. 它们的构效关系表明，该组织中腺苷受体的S4亚区域足够宽敞以容纳一个甲基，而仲烷基部分的性质似乎决定了叔甲基降低活性的程度。

Paton D M, Olsson R A

Department of Oral Biology, Faculty of Dentistry, University of Alberta, Edmonton, Canada.

J Auton Pharmacol. 1991 Apr;11(2):85-91. doi: 10.1111/j.1474-8673.1991.tb00247.x.

The potencies of a series of N6-substituted secondary and tertiary alkyladenosine analogues as inhibitors of the twitch responses of isolated guinea-pig ileum stimulated at 0.2 Hz have been determined. 2. All the analogues tested were full agonists. 3. Since their inhibitory effects were antagonized by theophylline and they had no significant effect on responses of ileum to carbachol, it was concluded that they acted predominantly by causing presynaptic inhibition of transmitter release. 4. Their structure-activity relationships indicated that the S4 subregion of the adenosine receptor in this tissue is capacious enough to accommodate a methyl group while the nature of the secondary alkyl moiety appears to determine the degree to which the tertiary methyl group reduces activity.

已测定了一系列N6-取代的仲烷基和叔烷基腺苷类似物作为0.2Hz刺激的离体豚鼠回肠抽搐反应抑制剂的效力。2. 所有测试的类似物都是完全激动剂。3. 由于它们的抑制作用被茶碱拮抗，且对回肠对卡巴胆碱的反应无显著影响，因此得出结论，它们主要通过引起递质释放的突触前抑制起作用。4. 它们的构效关系表明，该组织中腺苷受体的S4亚区域足够宽敞以容纳一个甲基，而仲烷基部分的性质似乎决定了叔甲基降低活性的程度。