Decker M W, Curzon P, Holladay M W, Nikkel A L, Bitner R S, Bannon A W, Donnelly-Roberts D L, Puttfarcken P S, Kuntzweiler T A, Briggs C A, Williams M, Arneric S P
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
J Physiol Paris. 1998 Jun-Aug;92(3-4):221-4. doi: 10.1016/s0928-4257(98)80014-4.
ABT-594, a nicotinic acetylcholine receptor agonist, has antinociceptive effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Direct injection of ABT-594 into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and destruction of serotonergic neurons in the NRM attenuates the effect of systemic ABT-594. However, lidocaine-inactivation of the NRM prevents the antinociceptive effect of systemic (-)-nicotine but not that of systemic ABT-594.
ABT-594是一种烟碱型乙酰胆碱受体激动剂,在急性热痛、持续性化学性疼痛和神经性疼痛的大鼠模型中具有镇痛作用。在热阈值试验中,将ABT-594直接注射到中缝大核(NRM)具有镇痛作用,而破坏NRM中的5-羟色胺能神经元会减弱全身性ABT-594的作用。然而,NRM的利多卡因失活可阻止全身性(-)-尼古丁的镇痛作用,但不能阻止全身性ABT-594的镇痛作用。