Hicks Alissa R, Varner Kurt J
Department of Cardiopulmonary Science, Louisiana State University Health Sciences Center, New Orleans, Louisiana, USA.
J Recept Signal Transduct Res. 2008;28(4):429-36. doi: 10.1080/10799890802244572.
Gamma-hydroxybutyrate (GHB) and its metabolic precursor, 1,4-butanediol (BDL), are widely used recreational drugs. Although most commonly described as CNS depressants, GHB and BDL elicit significant sympathomimetic cardiovascular responses [increases in mean arterial pressure (MAP) and heart rate] when administered parenterally. Given that humans most commonly ingest both drugs orally, we examined the dose-response relationships for intragastrically administered GHB and BDL on MAP and heart rate in conscious rats using radiotelemetry. The intragastric administration of GHB increased MAP. BDL increased both MAP and heart rate and was approximately 10-fold more potent as a cardiovascular stimulant than GHB when administered intragastrically. Pretreatment with ethanol prevented the lethality of BDL. These data indicate that 1) both GHB and BDL produce cardiovascular responses when administered intragastrically and 2) BDL is more potent and potentially more dangerous than GHB when administered via this route.
γ-羟基丁酸(GHB)及其代谢前体1,4-丁二醇(BDL)是广泛使用的消遣性药物。尽管GHB和BDL最常被描述为中枢神经系统抑制剂,但经肠胃外给药时,它们会引发显著的拟交感神经心血管反应[平均动脉压(MAP)和心率升高]。鉴于人类最常口服这两种药物,我们使用无线电遥测技术研究了在清醒大鼠中胃内给予GHB和BDL对MAP和心率的剂量反应关系。胃内给予GHB可升高MAP。BDL可同时升高MAP和心率,且胃内给药时作为心血管兴奋剂的效力约为GHB的10倍。乙醇预处理可预防BDL的致死性。这些数据表明:1)胃内给予GHB和BDL均可产生心血管反应;2)通过该途径给药时,BDL比GHB效力更强且潜在危险性更高。