Grunewald G L, McLeish M J, Criscione K R
Department of Medicinal Chemistry, University of Kansas, 4060 Malott Hall, 1251 Wescoe Hall Drive, Lawrence, KS 66045-7582, USA.
Bioorg Med Chem Lett. 2001 Jun 18;11(12):1579-82. doi: 10.1016/s0960-894x(01)00245-1.
Epinephrine (Epi) acts as a neurotransmitter in the brain, but its function therein is not well understood. Phenylethanolamine N-methyltransferase (PNMT) catalyzes the final step in the biosynthesis of Epi and is thus a pharmacological target to investigate the function of Epi in the central nervous system. The kinetic differences between bovine adrenal PNMT and human brain PNMT for a number of substrates and inhibitors are examined and the results reported.
肾上腺素(Epi)在大脑中作为神经递质发挥作用,但其在大脑中的功能尚未得到充分了解。苯乙醇胺N-甲基转移酶(PNMT)催化Epi生物合成的最后一步,因此是研究Epi在中枢神经系统中功能的药理学靶点。本文研究了牛肾上腺PNMT和人脑PNMT对多种底物和抑制剂的动力学差异,并报告了结果。