Kłodzińska A, Chojnacka-Wójcik E
Institute of Pharmacology, Polish Academy of Sciences, Kraków.
Psychopharmacology (Berl). 1992;109(4):466-72. doi: 10.1007/BF02247725.
TFMPP and m-CPP, non-selective 5-HT agonists, administered in doses of 1-20 mg/kg evoked hyperthermia in rats at a high ambient temperature (28 degrees C). The hyperthermic effect of TFMPP (10 mg/kg) or m-CPP (10 mg/kg) was dose-dependently antagonized by the 5-HT1c and 5-HT2 receptor antagonists mesulergine (0.5-4 mg/kg), ketanserin (0.6-2.5 mg/kg) and ritanserin (0.5-2 mg/kg) and by the non-selective 5-HT antagonist metergoline (0.5-1 mg/kg), or was attenuated by the 5-HT1A, 5-HT2 and dopamine receptor antagonist spiperone (3 mg/kg, but not 0.3 or 1 mg/kg). On the other hand, the 5-HT1A, 5-HT1B and beta adrenoceptor antagonists pindolol (2 mg/kg) and cyanopindolol (2 mg/kg), the 5-HT1A receptor agonist/antagonist ipsapirone (10 and 35 mg/kg) and haloperidol (0.25 and 0.5 mg/kg) showed a tendency towards enhancing the TFMPP- or m-CPP-induced hyperthermia. The 5-HT1A and alpha 1-adrenoceptor antagonist NAN-190 (1-4 mg/kg), the 5-HT3 antagonists tropisetron (0.01-1 mg/kg) and zacopride (0.5 and 1 mg/kg), the beta-blockers betaxolol (8 mg/kg) and ICI 118, 551 (8 mg/kg), which have no affinity for 5-HT receptors and prazosin (1 mg/kg), did not affect the hyperthermic effect of TFMPP or m-CPP. The hyperthermias studied were not modified, in animals with 5-HT lesion produced by p-chloroamphetamine (PCA) either. All the drugs used as putative receptor antagonists, as well as PCA, did not change or decreased (ipsapirone) the body temperature in heat-adapted rats.(ABSTRACT TRUNCATED AT 250 WORDS)
非选择性5-羟色胺(5-HT)激动剂TFMPP和间氯苯哌嗪,以1-20毫克/千克的剂量给药,在高环境温度(28摄氏度)下可引起大鼠体温过高。TFMPP(10毫克/千克)或间氯苯哌嗪(10毫克/千克)的体温过高效应,可被5-HT1c和5-HT2受体拮抗剂美舒麦角(0.5-4毫克/千克)、酮色林(0.6-2.5毫克/千克)和利坦色林(0.5-2毫克/千克)以及非选择性5-HT拮抗剂麦角乙脲(0.5-1毫克/千克)剂量依赖性地拮抗,或者被5-HT1A、5-HT2和多巴胺受体拮抗剂螺哌隆(3毫克/千克,但不是0.3或1毫克/千克)减弱。另一方面,5-HT1A、5-HT1B和β肾上腺素能受体拮抗剂吲哚洛尔(2毫克/千克)和氰吲哚洛尔(2毫克/千克)、5-HT1A受体激动剂/拮抗剂伊沙匹隆(10和35毫克/千克)以及氟哌啶醇(0.25和0.5毫克/千克)显示出增强TFMPP或间氯苯哌嗪诱导的体温过高的趋势。5-HT1A和α1肾上腺素能受体拮抗剂NAN-190(1-4毫克/千克)、5-HT3拮抗剂托烷司琼(0.01-1毫克/千克)和扎考必利(0.5和1毫克/千克)、对5-HT受体无亲和力的β阻滞剂倍他洛尔(8毫克/千克)和ICI 118,551(8毫克/千克)以及哌唑嗪(1毫克/千克),均不影响TFMPP或间氯苯哌嗪的体温过高效应。在对氯苯丙胺(PCA)造成5-HT损伤的动物中,所研究的体温过高情况也未改变。所有用作假定受体拮抗剂的药物以及PCA,均未改变热适应大鼠的体温或使其体温降低(伊沙匹隆)。(摘要截短至250字)