Cohen M L, Kurz K D, Fuller R W
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285.
Clin Exp Hypertens A. 1987;9(10):1549-65. doi: 10.3109/10641968709159002.
mCPP (meta-chlorophenylpiperazine) has agonist activity at some central serotonin receptors and antagonist activity at peripheral vascular 5HT2 receptors, both effects that have been postulated to lower blood pressure. mCPP (10 and 30 mg/kg, i.p. 1 hr after administration) increased serotonin and decreased 5-hydroxy-indolacetic acid (5-HIAA) brain concentrations and elevated serum corticosterone and prolactin, indications of central serotonergic agonist activities. The same doses of mCPP also antagonized vascular 5HT2 receptors as measured by blockade of pressor responses to serotonin in pithed rats. Although mCPP could be demonstrated to activate central serotonergic receptors and block peripheral vascular 5HT2 receptors, mCPP (10 and 30 mg/kg, i.p.) produced little effect on blood pressure in either the anesthetized or conscious spontaneously hypertensive rat (SHR) up to 1 hr after intraperitoneal administration. The findings are consistent with initial studies in normotensive humans that have not demonstrated a reduction in blood pressure clinically after mCPP in doses that produce elevations in serum cortisol and prolactin levels.
间氯苯哌嗪（mCPP）对某些中枢5-羟色胺受体具有激动剂活性，而对外周血管5HT2受体具有拮抗剂活性，这两种作用均被认为可降低血压。mCPP（10毫克/千克和30毫克/千克，腹腔注射，给药后1小时）可增加5-羟色胺并降低脑内5-羟吲哚乙酸（5-HIAA）浓度，还可提高血清皮质酮和催乳素水平，这些都是中枢5-羟色胺能激动剂活性的指标。同样剂量的mCPP还可通过阻断脊髓麻醉大鼠对5-羟色胺的升压反应来拮抗血管5HT2受体。尽管已证明mCPP可激活中枢5-羟色胺能受体并阻断外周血管5HT2受体，但在腹腔注射后长达1小时的时间内，mCPP（10毫克/千克和30毫克/千克，腹腔注射）对麻醉或清醒的自发性高血压大鼠（SHR）的血压几乎没有影响。这些发现与在血压正常的人类中进行的初步研究一致，在这些研究中，给予能使血清皮质醇和催乳素水平升高的剂量的mCPP后，临床上并未显示出血压降低。
