Bourreau J P, Tricoche R
Laboratoire de physiologie animale, CNRS UA 290, Biomembranes, Université de Poitiers, France.
Can J Physiol Pharmacol. 1987 Dec;65(12):2496-9. doi: 10.1139/y87-397.
The prejunctional activities of S-3341 and clonidine have been studied in the transmural field-stimulated epididymal part of the rat vas deferens. Both S-3341 and clonidine inhibited these neuronally induced contractions. At high concentrations, these agonists induced spontaneous contractions in the preparation, which were abolished by 10(-7) M prazosin. The inhibitory effects of S-3341 and clonidine were antagonized in a competitive manner by rauwolscine and were found not to be modified in a statistically significant manner by 10(-7) M prazosin. The pA2 values of rauwolscine against S-3341 and clonidine were the same, indicating the receptors influenced by these drugs were the same also. However, the efficacy of S-3341 is lower than that of clonidine (by a factor of approximately 100). This lower efficacy of S-3341 at the prejunctional level could be linked to the lack of a sedative effect of this compound at therapeutic concentrations.
在大鼠输精管经壁场刺激的附睾部分，对S-3341和可乐定的接头前活性进行了研究。S-3341和可乐定都抑制这些神经诱导的收缩。在高浓度时，这些激动剂在制备物中诱导自发收缩，10(-7)M哌唑嗪可消除这些收缩。S-3341和可乐定的抑制作用被萝芙辛以竞争性方式拮抗，并且发现10(-7)M哌唑嗪对其无统计学显著影响。萝芙辛对S-3341和可乐定的pA2值相同，表明受这些药物影响的受体也是相同的。然而，S-3341的效能低于可乐定（约为100倍）。S-3341在接头前水平的这种较低效能可能与该化合物在治疗浓度下缺乏镇静作用有关。
