Shen R, Tillekeratne L M, Kirchhoff J R, Hudson R A
Department of Medicinal and Biological Chemistry College of Pharmacy, Toledo, Ohio 43606, USA.
Biochem Biophys Res Commun. 1996 Nov 1;228(1):187-92. doi: 10.1006/bbrc.1996.1637.
The synthesis and properties of 6-hydroxy-N,N-dimethylepinephrine (6-hydroxy-catecholine) are reported. This agent is intended for use as a selective presynaptic cholinotoxin and is based on previously reported neurotoxins of the same type. 6-hydroxycatecholine is a close structural analogue of the catecholaminergic neurotoxin 6-hydroxydopamine, and is expected both to be selectively reactive at cholinergic sites and to undergo less vigorous and potentially more selective inactivating reactions. It is also possible that in specific dementia-inducing pathologies, 6-hydroxycatecholine could be formed endogenously.
报道了6-羟基-N,N-二甲基肾上腺素(6-羟基儿茶酚)的合成及性质。该药剂旨在用作选择性突触前胆碱能毒素,它基于先前报道的同类神经毒素。6-羟基儿茶酚是儿茶酚胺能神经毒素6-羟基多巴胺的紧密结构类似物,预计它既能在胆碱能位点发生选择性反应,又能经历不那么剧烈且可能更具选择性的失活反应。在特定的致痴呆病理过程中,6-羟基儿茶酚也有可能内源性形成。