Kuboia M, Atobe M, Nakagawara M, Kariya T
Department of Neuropsychiatry, Yamanashi Medical University, Japan.
Neuropsychobiology. 1996;33(3):132-7. doi: 10.1159/000119263.
This study examines the in vivo effects of 2,3-dichloro-alpha-methylbenzylamine (DCMB), a centrally active phenylethanolamine-N-methyltransferase (PNMT) inhibitor, on alpha 2-adrenoceptors. Sixty-six rats received either DCMB, SKF29661, the peripheral PNMT inhibitor, at a dose of 50 mg/kg or saline intraperitoneally. To examine the functional responses of the alpha 2-adrenoceptors to these drugs, changes in spontaneous locomotor activity, concentration of 3-methoxy-4-hydroxyphenylglycol (MHPG) in dialysates from the hypothalamus, and the influence of clonidine on growth hormone (GH) secretion were investigated. (1) DCMB increased spontaneous motion of the rat. (2) DCMB increased extracellular MHPG concentration in the hypothalamus verified by micro-brain dialysis. (3) Clonidine failed to stimulate GH secretion in DCMB-treated rats. These results suggest that DCMB has an inhibitory action on the alpha 2-adrenoceptor function in vivo.
本研究考察了中枢活性苯乙醇胺 -N-甲基转移酶（PNMT）抑制剂2,3 - 二氯 -α-甲基苄胺（DCMB）对α2 - 肾上腺素能受体的体内作用。66只大鼠腹腔注射剂量为50 mg/kg的DCMB、外周PNMT抑制剂SKF29661或生理盐水。为了考察α2 - 肾上腺素能受体对这些药物的功能反应，研究了自发运动活性的变化、下丘脑透析液中3 - 甲氧基 - 4 - 羟基苯乙二醇（MHPG）的浓度以及可乐定对生长激素（GH）分泌的影响。（1）DCMB增加了大鼠的自发运动。（2）通过微量脑透析证实，DCMB增加了下丘脑细胞外MHPG浓度。（3）在经DCMB处理的大鼠中，可乐定未能刺激GH分泌。这些结果表明，DCMB在体内对α2 - 肾上腺素能受体功能具有抑制作用。
