Shannon H E, Cone E J, Yousefnejad D
J Pharmacol Exp Ther. 1982 Oct;223(1):190-6.
Single i.v. doses of beta-phenylethylamine (PEA) and its N-methyl homolog (NMPEA) were administered to separate groups of five dogs. The dose- and time-related effects of these compounds were determined on pupil diameter, heart rate and body temperature. Blood samples were obtained concurrently with the physiologic measures and plasma levels of PEA and NMPEA were determined by gas chromatography. Both compounds dilated pupils, tended to produce an initial tachycardia followed by a bradycardia and elevated body temperature. The plasma pharmacokinetics of both PEA and NMPEA could be described by first-order kinetics which estimated half-lives of approximately 5 to 10 min. Plasma levels for both amines correlated significantly only with increases in pupil diameter. The present findings demonstrate that the endogenous trace amine PEA and NMPEA, which may be produced enzymatically by nonspecific N-methyl transferases, produce prominent physiologic effects of short duration when administered i.v. in the dog, suggesting that alterations in the metabolism of these amines which result in elevated plasma levels can produce pronounced effects on mammalian nervous system function.
给五组不同的狗分别静脉注射单剂量的β-苯乙胺（PEA）及其N-甲基同系物（NMPEA）。测定了这些化合物对瞳孔直径、心率和体温的剂量及时间相关效应。在进行生理指标测量的同时采集血样，并用气相色谱法测定血浆中PEA和NMPEA的水平。两种化合物均使瞳孔扩张，往往会先引起心动过速，随后出现心动过缓，并使体温升高。PEA和NMPEA的血浆药代动力学可用一级动力学描述，估计半衰期约为5至10分钟。两种胺类的血浆水平仅与瞳孔直径的增加显著相关。目前的研究结果表明，内源性痕量胺PEA和NMPEA可能由非特异性N-甲基转移酶酶促产生，静脉注射给狗时会产生持续时间短的显著生理效应，这表明这些胺类代谢的改变导致血浆水平升高，可对哺乳动物神经系统功能产生明显影响。
