盐酸哈尔满(Harmane hydrochloride)是多靶点活性分子,对多种受体具有抑制作用并介导多重生物效应。它抑制苯二氮卓类受体(IC50=7μM)、I1咪唑啉受体(IC50=30nM),对mACh、阿片受体、MAO-A/B、α2-肾上腺素受体的IC50分别为24μM、2.8μM、0.5μM、5μM、18μM;通过抑制I1咪唑啉受体降低血压,还具有抗抑郁、抗焦虑、抗惊厥、镇痛作用。此外,它能降低酪氨酸羟化酶(TH)活性、增强左旋多巴(L-DOPA)诱导的PC12细胞毒性以抑制多巴胺生物合成,同时提高2-乙酰氨基芴(AAF)诱导的致突变作用。
[1] Müller WE, Fehske KJ, Borbe HO, Wollert U, Nanz C, Rommelspacher H. On the neuropharmacology of harmane and other beta-carbolines. Pharmacol Biochem Behav. 1981 May;14(5):693-9. doi: 10.1016/0091-3057(81)90133-7. PMID: 6264501.[2]Musgrave IF, Badoer E. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9. doi: 10.1038/sj.bjp.0703142. PMID: 10725251; PMCID: PMC1571934.[3]Umezawa K, Shirai A, Matsushima T, Sugimura T. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30. doi: 10.1073/pnas.75.2.928. PMID: 345280; PMCID: PMC411371.[4]Yang YJ, Lee JJ, Jin CM, Lim SC, Lee MK. Effects of harman and norharman on dopamine biosynthesis and L-DOPA-induced cytotoxicity in PC12 cells. Eur J Pharmacol. 2008 Jun 10;587(1-3):57-64. doi: 10.1016/j.ejphar.2008.03.050. Epub 2008 Apr 4. PMID: 18457825.[5]Aricioglu F, Altunbas H. Harmane induces anxiolysis and antidepressant-like effects in rats. Ann N Y Acad Sci. 2003 Dec;1009:196-201. doi: 10.1196/annals.1304.024. PMID: 15028588.





