Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P08908 (5-HT1A)
 5,574 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We studied the effect of repeated treatment with imipramine, amitriptyline (10 mg/kg po, twice daily for 14 days) or electroconvulsive shock (ECS, once daily for 10 days) on the 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT)-induced increase in food intake in free feeding rats. The response to 8-OH-DPAT, measured 24 h after the last administration of the antidepressant drugs or ECS, was not modified. These results, together with literature data, indicate that the presynaptic 5-HT1A receptors involved in the 8-OH-DPAT-induced feeding are not affected by long-term antidepressant administration.
Pol J Pharmacol Pharm
PMID:Repeated treatment with imipramine, amitriptyline or electroconvulsive shock does not affect the 8-OH-DPAT-induced increase in food intake in free feeding rats. 215 67

1-[3-(trifluoromethyl) phenyl] piperazine (TFMPP), a putative 5-HT1B, 5-HT1C and 5-HT2 agonist decreased dose-dependently food intake over 4 h in freely feeding rats. The TFMPP-induced anorexia was blocked by mesulergine (a 5-HT1C and 5-HT2 antagonist), metergoline (a 5-HT1A, 5-HT1B, 5-HT1C and 5-HT2 antagonist), mianserin (a 5-HT1C and 5-HT2 antagonist) and attenuated by ketanserin and ritanserin (5-HT2 antagonists). The examined anorexia was not antagonized by cyanopindolol and compound 21009 (5-HT1A and 5-HT1B antagonists). These results indicate that the TFMPP-induced anorexia in freely feeding rats is probably mediated by 5-HT2--and, may be also by 5-HT1C receptors.
Pol J Pharmacol Pharm
PMID:Anorexia induced by M-trifluoromethylphenylpiperazine (TFMPP) in rats. 228 Oct 17

Ipsapirone (TVX Q 7821), a compound with a high affinity for the 5-HT1A receptor-subtype, decreased by itself 5-HIAA level and reduced 5-HIAA accumulation after probenecid administration in the rat hypothalamus. The reduced 5-HIAA level and 5-HIAA/5-HT ratio after the 5-HT1A selective agonist 8-OH-DPAT was not antagonized by pretreatment with ipsapirone.
Pol J Pharmacol Pharm
PMID:Effects of ipsapirone on the level of 5-hydroxytryptamine and 5-hydroxyindoleacetic acid in some regions of the rat brain. 247 37

We studied the effect of repeated treatment (twice daily for 14 consecutive days) with the antidepressant drugs imipramine, citalopram and mianserin (all the drugs administered in a dose of 10 mg/kg po) on the 8-OH-DPAT-induced increase in the serum corticosterone concentration. We found that all those drugs affected neither basal nor 8-OH-DPAT-induced increase in the corticosterone concentration. These results suggest that long-term administration of the investigated antidepressant drugs does not modify the functional sensitivity of central 5-HT1A receptors.
Pol J Pharmacol Pharm
PMID:The lack of effect of repeated treatment with antidepressant drugs on the 8-OH-DPAT-induced increase in the serum corticosterone concentration. 253 82

The study examined the effect of both oxaprotiline (OXA) enantiomers on the serotonin system in rats and mice. (+)-OXA and (-)-OXA partly inhibit the behavioral syndrome induced by 8-OH-DPAT and 5-methoxy-dimethyltryptamine (5-MeODMT) in normal and reserpinized rats. Imipramine and desipramine produced a similar but less potent effect. (+)-OXA and, to a lesser extent, (-)-OXA antagonized the m-chlorophenylpiperazine (m-CPP)-induced hypothermia in mice. Imipramine and desipramine produced no such effect. (+)-OXA attenuated the head-twitch response to L-5-HTP in mice, but (-)-OXA has no such action. Neither enantiomer inhibited the fenfluramine-induced hyperthermia in rats nor antagonized m-CPP-induced stimulation of hind limb flexor reflex of spinal rat. The obtained results indicate that both enantiomers may have a 5-HT1B-antagonistic action and a less potent 5-HT1A-antagonistic one; on the other hand, they shown no 5-HT2-antagonistic activity.
Pol J Pharmacol Pharm
PMID:Pharmacological effects of oxaprotiline enantiomers on the central serotonin system. 253 22

Intrastriatal administration of ipsapirone (IPSA, 0.5 and 1 mM), an agonist of 5-HT1A serotonergic receptors, enhanced in a dose-dependent manner DA release in the rat striatum, without affecting levels of the DA metabolites DOPAC and HVA. The IPSA evoked-enhancement of DA release was followed by a decrease in 5-HIAA concentration. The effects of intrastriatal administration of IPSA were mimicked by 8-OH-DPAT (0.5 mM), another agonist of 5-HT1A receptors, and were antagonized by the peripheral administration of metergoline (5 mg/kg ip) and intrastriatal administration of NAN-190 (0.5 mM). IPSA given peripherally (10 mg/kg ip) also enhanced DA release; that effect was accompanied by an increase in DOPAC and HVA levels. It is postulated that IPSA increases the release of DA from nigrostriatal terminals via activation of striatal 5-HT1A receptors in a manner independent of the activation of 5-HT1A receptors in the dorsal raphe nuclei.
Pol J Pharmacol
PMID:Enhancement by ipsapirone of dopamine release in the rat striatum. 769 36

Effects of the non-selective 5-hydroxytryptamine (5-HT) receptor agonist m-chlorophenylpiperazine (m-CPP) on the nociceptive responsiveness in a hot plate and tail flick tests were examined in mice. Intraperitoneal administration of m-CPP (1-10 mg/kg) produced a dose-dependent antinociception in both those tests; the effect of m-CPP in the hot plate test was stronger. The antinociceptive effect of m-CPP in either test was abolished by pretreatment with mesulergine (2 mg/kg), ritanserin (1-2 mg/kg), 5-HT2A/5-HT2C receptor antagonists, and metergoline (0.5-2 mg/kg), a non-selective 5-HT receptor antagonist. On the other hand, spiperone (0.25-0.5 mg/kg), a dopamine, 5-HT1A and 5-HT2A receptor antagonist; pindolol (4-8 mg/kg), a beta-adrenoceptor, 5-HT1A and 5-HT1B receptor antagonist and zacopride (0.1-1 mg/kg) a 5-HT3 receptor antagonist, did not affect the analgesia induced by m-CPP. Neither of the drugs used as putative receptor antagonists changed the nociceptive responsiveness in mice. The obtained results suggest that the analgesia induced by m-CPP is mediated by 5-HT2C receptors.
Pol J Pharmacol
PMID:Involvement of 5-HT2C receptors in the m-CPP-induced antinociception in mice. 789 29

The preparation of several derivatives of bicyclo[2.2.2]oct-7-ene- 2,3,5,6-tetracarboxydiimide on two routes has been described. Some of them display an expected anxiolytic activity. The 5-HT1A receptor affinities of tested compounds are comparable with that of buspirone.
Pol J Pharmacol
PMID:Synthesis and pharmacological screening of some N,N'-bis-[4-(4-aryl-1-piperazinyl)butyl]-substituted derivatives of 1,8-dimethylbicyclo-[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide. 789 33

The role of brain serotonergic system innervating hippocampus and nucleus accumbens in the anxiolytic-like action of the 5-HT1A receptor agonists and 5-HT3 receptor antagonists, is discussed. The data on the effects of intrastructural microinjections of selective serotonergic agonists and antagonists in the Vogel and open field (neophobic reaction) tests are described and critically reviewed. It is concluded that both postsynaptic inhibition of the temporal lobe function (the hippocampus), and attenuation of the cell body firing of the raphe neurons appears to be important elements of anti-anxiety action of benzodiazepines and 5-HT1A receptor antagonists. Thus, it is hypothesized that this dual mechanism of the 5-HT1A receptor agonists and the 5-HT3 receptor antagonists action cooperates synergistically in the processing of emotional functions.
Pol J Pharmacol
PMID:Limbic mechanisms of anxiolytics acting on 5-HT receptors. 789 37

The 5-HT1A antagonistic properties of (+)-N-tert-butyl-3-[4-(2-methoxyphenyl)piperazin-1-yl]-2-phenyl pro panamide ((+)WAY 100135) were studied. Its effect on the 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT)-induced behavioral syndrome (flat body posture and reciprocal forepaw treading) in reserpine-pretreated rats, the stimulus effect in a drug discrimination model in rats, the lower lip retraction in rats, the hypothermia in mice and secretion of corticosterone in rats, i.e. responses mediated by 5-HT1A receptors, were examined. (+)WAY 100135 administered in doses up to 10 mg/kg dose-dependently antagonized all the above responses to 8-OH-DPAT, the lowest effective doses ranging from 1.25 to 2.5 mg/kg. At the same time, (+)WAY 100135 alone given in doses of 1.25-10 mg/kg did not mimic the activity of 8-OH-DPAT in the tests used. Our results indicate that (+)WAY 100135 is an antagonist of pre- and postsynaptic 5-HT1A receptors devoid of agonist properties.
Pol J Pharmacol
PMID:Antagonism of (+)WAY 100135 to behavioral, hypothermic and corticosterone effects induced by 8-OH-DPAT. 798 67


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