Karobath M, Lippitsch M
Eur J Pharmacol. 1979 Oct 15;58(4):485-8. doi: 10.1016/0014-2999(79)90321-2.
The effects of THIP and isoguvacine on 3H-flunitrazepam binding to washed membranes prepared from the cerebral cortex of adult rats have been examined. THIP, which has only minimal stimulatory effects on benzodiazepine (BZ) receptor binding, has been found to inhibit the stimulation induced by small concentrations (2 microM) of exogenous GABA. While isoguvacine stimulates BZ receptor binding, although to a smaller extent than GABA, it also antagonizes the stimulation of BZ receptor binding induced by GABA. Thus THIP and isoguvacine exhibit the properties of a partial agonist of GABA-stimulated BZ receptor binding.
已研究了 THIP 和异谷氨酰胺对 3H-氟硝西泮与成年大鼠大脑皮质制备的洗涤膜结合的影响。THIP 对苯二氮䓬（BZ）受体结合仅有极小的刺激作用，已发现它能抑制低浓度（2 microM）外源性 GABA 诱导的刺激。而异谷氨酰胺虽刺激 BZ 受体结合，但其程度小于 GABA，它也拮抗 GABA 诱导的 BZ 受体结合刺激。因此，THIP 和异谷氨酰胺表现出 GABA 刺激的 BZ 受体结合的部分激动剂特性。
