Asano M, Hidaka H
Br J Pharmacol. 1977 Oct;61(2):263-9. doi: 10.1111/j.1476-5381.1977.tb08414.x.
1 When the isolated thoracic aorta of the rabbit was contracted with prostaglandin F2alpha, 5-alkylpicolinic acids produced dose-dependent relaxations. 2 Picolinic acid, 2,5-pyridinedicarboxylic acid and 5-acetylpicolinic acid which do not have the 5-alkyl residue failed to relax blood vessels. 3 The vascular relaxation was dependent on the number of carbon atoms in the 5-alkyl compounds. 4 Relaxations which occurred with 5-alkylpicolinic acids were not affected by pretreatment with either propranolol or atropine. 5 It is concluded that the 5-alkyl residue is necessary for the vascular relaxation with 5-alkylpicolinic acid and that it was not produced by stimulation of beta-adrenoceptors or cholinoceptors but rather through an activation of the basic process.
当用前列腺素F2α使兔离体胸主动脉收缩时,5 - 烷基吡啶甲酸产生剂量依赖性舒张作用。
没有5 - 烷基残基的吡啶甲酸、2,5 - 吡啶二甲酸和5 - 乙酰基吡啶甲酸不能使血管舒张。
血管舒张作用取决于5 - 烷基化合物中的碳原子数。
5 - 烷基吡啶甲酸引起的舒张作用不受普萘洛尔或阿托品预处理的影响。
得出结论:5 - 烷基残基是5 - 烷基吡啶甲酸血管舒张所必需的,其舒张作用不是由β - 肾上腺素能受体或胆碱能受体的刺激产生的,而是通过基本过程的激活产生的。