Das S, Bhargava H N
Gen Pharmacol. 1987;18(1):99-102. doi: 10.1016/0306-3623(87)90178-9.
The effect of TRH and its analogs, MK771 and RX-77368 on the binding of [3H]D-serine-6-threonine-leucine enkephalin (delta opiate receptors), [3H]ethylketocyclazocine (kappa receptors) and [3H]naltrexone (mu receptors) to the rat brain membranes was determined. Neither TRH nor its analogs affected the binding of ligands for mu, delta, and kappa opiate receptors at either 35 or 0 degrees C. Since previous studies from this laboratory indicate that the drugs acting at the kappa, and delta opiate receptors inhibit the binding of 3H TRH to brain TRH receptors, the present studies suggest a unidirectional interaction between opiates and TRH in the brain at the level of their receptors.
测定了促甲状腺激素释放激素(TRH)及其类似物MK771和RX - 77368对[3H]D - 丝氨酸 - 6 - 苏氨酸 - 亮氨酸脑啡肽(δ阿片受体)、[3H]乙基酮环唑辛(κ受体)和[3H]纳曲酮(μ受体)与大鼠脑膜结合的影响。在35℃或0℃时,TRH及其类似物均不影响μ、δ和κ阿片受体配体的结合。由于本实验室先前的研究表明,作用于κ和δ阿片受体的药物会抑制[3H](3 - MeHis2)TRH与脑TRH受体的结合,因此本研究提示,在脑内受体水平上,阿片类药物与TRH之间存在单向相互作用。