Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020672 (hypothermia)
 17,327 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The novel, naphthylpiperazine 5-HT1A agonist, S 14671 (4-[(thenoyl-2)aminoethyl]-1-(7-methoxynaphtylpiperazine], displayed very high affinity for 5-HT1A binding sites (pKi = 9.3) as compared to the serotonin (5-HT)1A agonists, 8-OH-DPAT (9.2) and (+)-flesinoxan (8.7) and the 5-HT1A partial agonists, buspirone (7.9) and BMY 7378 (8.8). In vivo, S 14671 induced the typical 5-HT1A agonist-induced responses of hypothermia and spontaneous tail-flicks at doses as low as greater than or equal to 5 micrograms/kg s.c. and greater than or equal to 40 micrograms/kg s.c., respectively. In each test, it was about 10-fold more potent than 8-OH-DPAT and 100-fold more potent than (+)-flesinoxan and buspirone. The actions of S 14671 could be blocked by BMY 7378 and the 5-HT1A receptor antagonist, (-)-alprenolol, but not by the 5-HT1C/2 receptor antagonist, ritanserin, nor the 5-HT3 receptor antagonist, ICS 205930. Thus, S 14671 is a novel 5-HT1A ligand of high efficacy and exceptional in vivo potency.
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PMID:S 14671: a novel naphthylpiperazine 5-HT1A agonist of high efficacy and exceptional in vivo potency. 183 84

The effects of peripherally administered serotonin (5-HT) on the rectal temperature were investigated. 5-HT i.p. induced a dose-dependent hypothermia in mice. The hypothermic effects of 5-HT were strongly antagonized by the 5-HT1 and 5-HT2 receptor antagonist methysergide and the 5-HT2 receptor antagonist ketanserin. However, the 5-HT1 receptor antagonist pindolol and the 5-HT3 receptor antagonist ICS 205-930 were without effect. In addition, the peripheral 5-HT2 receptor antagonist xylamidine strongly reduced 5-HT-induced hypothermia. These results indicate that the activation of the peripheral 5-HT2 receptors induces hypothermia, although the central 5-HT2 receptors have been suggested to relate to hyperthermia.
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PMID:Activation of peripheral serotonin2 receptors induces hypothermia in mice. 199 84

1. The current classification of receptors for 5-hydroxytryptamine (5-HT) is based on functional studies, and encompasses three main receptor types. 2. 5-HT1-like receptors mediate inhibition of release of various neurotransmitters from central and peripheral sites, smooth muscle contraction and relaxation (and release of endothelium-derived relaxing factor), tachycardia, a variety of behavioural actions (for example, forepaw treading, hypothermia, hyperphagia, drug discriminative stimulus properties, nociceptive pathway modulation, and anxiolytic, anti-aggressive and prosexual effects), and central neuronal excitatory and inhibitory activity. Selective antagonists for this receptor are not yet available, but the 5-HT2 receptor antagonists methysergide and methiothepin have appreciable affinity for 5-HT1-like receptors, and 5-carboxamidotryptamine is a selective agonist. 3. 5-HT2 receptors mediate smooth muscle contraction, platelet aggregation, increased capillary permeability, some behavioural syndromes (for example, head twitch and wet-dog shakes) and drug discriminative stimulus properties, central neuroexcitatory effects, and some neuroendocrine functions. Ketanserin and cyproheptadine are selective antagonists. 4. 5-HT3 receptors mediate peripheral afferent and efferent neuroexcitatory actions, anxiogenic effects, and modulation of cytotoxic drug-induced emesis, gastric emptying, and dopamine-related mesolimbic hyperactivity. Selective antagonists include cocaine, MDL 72222 and ICS 205-930; 2-methyl-5-HT is a selective agonist.
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PMID:The classification of 5-hydroxytryptamine receptors. 267 Mar 59

In the present study we examined the effect of different drugs on the m-trifluoromethylphenylpiperazine (TFMPP)- and m-chlorophenylpiperazine (m-CPP)-induced hypothermia in mice. Both the hypothermias studied are blocked or reversed by pindolol, cyanopindolol and compound 21-009, but not by atenolol. Neither hypothermia is antagonized by 5-HT1A antagonists (ipsapirone, spiperone), a 5-HT1C antagonist (mesulergine), 5-HT2 antagonists (cyproheptadine, mianserin, methysergide), 5-HT3 antagonists (ICS 205930, metoclopramide). The examined hypothermias are not antagonized by other antihypothermic agents (pimozide, idazoxan, atropine). The 8-OH-DPAT-induced hypothermia is not affected by cyanopindolol or compound 21009. The obtained results indicate that the TFMPP- and m-CPP-induced hypothermias in mice are mediated by 5-HT1B. These hypothermias may be a good screening test for evaluation of the 5-HT1B-agonistic and 5-HT1B-antagonistic activity.
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PMID:Hypothermia induced by m-trifluoromethylphenylpiperazine or m-chlorophenylpiperazine: an effect mediated by 5-HT1B receptors? 296 49

This study determined the effects of the 5-hydroxytryptamine (5-HT) serotonin antagonists ondansetron and (3 alpha-tropanyl]-1H-indole-3-carboxylic acid ester HCl (ICS 205-930) on hypothermia induced in rats by irradiation and by administration of a 5-HT3 receptor agonist, 2-methyl-5-hydroxytryptamine (2-Me-5-HT). Intraperitoneal (i.p.) administration of 50-200 micrograms/kg of ondansetron and intraventricular administration of 5-20 micrograms of ondansetron attenuated hypothermia induced by 20 Gy gamma rays. However, the same doses of ondansetron administered i.p. or intraventricularly did not antagonize the hypothermia induced by 10 micrograms 2-Me-5-HT. In contrast, i.p. administration of 50-200 micrograms/kg of ICS 205-930 and intraventricular administration of 5-20 micrograms of ICS 205-930 attenuated hypothermia induced by radiation and 2-Me-5-HT. These results indicate that ICS 205-930 attenuates hypothermia induced by radiation and 2-Me-5-HT. However, the doses of ondansetron that attenuated radiation-induced hypothermia did not attenuate hypothermia induced by 2-Me-5-HT.
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PMID:Effect of ondansetron and ICS 205-930 on radiation-induced hypothermia in rats. 918 74