Coleman R A, Kennedy I
Prostaglandins. 1985 Mar;29(3):363-75. doi: 10.1016/0090-6980(85)90096-6.
The receptors mediating prostanoid-induced contraction of guinea-pig isolated trachea have been characterised in terms of a recently proposed general classification of prostanoid receptors. Results obtained on the trachea were compared with those obtained on guinea-pig fundus, which contains a sub-type of PGE2-sensitive (EP-) receptor termed the EP1-receptor, and guinea-pig lung strip, which contains a thromboxane-sensitive or TP-receptor. The following agonists were studied, PGE2, PGF2 alpha and the thromboxane-like agonists U-46619 and Wy17186. The antagonists studied were SC-19220 which selectively blocks EP1-receptors, and AH19437 which selectively blocks TP-receptors. On guinea-pig fundus the rank order of agonist potency was PGE2 greater than PGF2 alpha greater than Wy-17186 approximately equal to U-46619, and responses to all agonists were antagonised by SC-19220 but not by AH19437. On guinea-pig lung strip the rank order of potency was U-46619 greater than Wy17186 much greater than PGF2 alpha greater than PGE2 and responses to all agonists tested were blocked by AH19437 but not by SC-19220. On the trachea, the rank order was PGE2 = U-46619 greater than Wy17186 = PGF2 alpha. SC-19220 antagonised responses to PGE2 and PGF2 alpha, but not those to U-46619 or Wy17186. Conversely, AH19437 antagonised responses to U-46619 and Wy17186 but not those to PGE2 or PGF2 alpha. It is concluded that prostanoid-induced contractions of guinea-pig trachea can be mediated by both EP1- and TP-receptors.
根据最近提出的前列腺素受体通用分类法,对介导豚鼠离体气管前列腺素诱导收缩的受体进行了表征。将在气管上获得的结果与在豚鼠胃底(其中含有一种对PGE2敏感的亚型受体,称为EP1受体)和豚鼠肺条(其中含有对血栓素敏感的受体或TP受体)上获得的结果进行了比较。研究了以下激动剂:PGE2、PGF2α以及血栓素样激动剂U-46619和Wy17186。研究的拮抗剂为选择性阻断EP1受体的SC-19220和选择性阻断TP受体的AH19437。在豚鼠胃底,激动剂效力的排序为:PGE2>PGF2α>Wy-17186≈U-46619,对所有激动剂的反应均被SC-19220拮抗,但不被AH19437拮抗。在豚鼠肺条上,效力排序为:U-46619>Wy17186>>PGF2α>PGE2,对所有测试激动剂的反应均被AH19437阻断,但不被SC-19220阻断。在气管上,排序为:PGE2 = U-46619>Wy17186 = PGF2α。SC-19220拮抗对PGE2和PGF2α的反应,但不拮抗对U-46619或Wy17186的反应。相反,AH19437拮抗对U-46619和Wy17186的反应,但不拮抗对PGE2或PGF2α的反应。结论是,豚鼠气管中前列腺素诱导的收缩可由EP1受体和TP受体介导。