Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effect of six 5-HT3 receptor antagonists: ondansetron (0.01-3 mg/kg ip), granisetron (0.01-1 mg/kg ip), zacopride (0.01-3 mg/kg ip), tropisetron (0.001-0.1 mg/kg ip), MDL 72222 (0.01-3 mg/kg ip) and DAU 6215 (0.01-3 mg/kg sc) were examined in the conflict drinking test (Vogel test) and in the elevated plus-maze test in rats. Ondansetron (0.1-0.3 or 1 mg/kg), zacopride (0.1-1 mg/kg) and tropisetron (0.01 mg/kg) increased the punished responding in the Vogel test and showed anxiolytic effects in the elevated plus-maze test. Their effects were limited to a narrow dose range and were not dose-dependent. Granisetron (0.1 mg/kg) exhibited an anti-conflict activity, but was ineffective in the elevated plus-maze test. MDL 72222 and DAU 6215 were ineffective in both those tests. On the other hand, diazepam (2.5-10 mg/kg), used as a reference drug, was active in either procedure and its effects were dose-dependent. These results indicate that an anxiolytic-like activity is not a common characteristic of 5-HT3 receptor antagonists. Moreover, even the anxiolytic action of drugs which were active in the experimental models used should be accepted with caution.
Pol J Pharmacol Pharm
PMID:The anxiolytic-like effects of 5-hydroxytryptamine3 (5-HT3) receptor antagonists. 147 May 64

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 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 effect of 5HT3 and 5HT4 active compounds on the motivational properties of morphine has been examined in the place conditioning (PC) paradigm using unbiased procedure. Place conditioning with morphine produced significant place preference. Pretreatment with the DAU 6285 (mixed 5HT3 antagonist--5HT4 antagonist) abolished morphine-induced PC. Ondansetron (selective 5HT3 antagonist) attenuated morphine place preference at the dose of 0.1 mg/kg. BIMU 8 (mixed 5HT3 antagonist--5HT4 agonist) failed to modify morphine PC in the 0.001-0.1 mg/kg dose range. While ondansetron given alone failed to produce place conditioning, pairing of BIMU 8 (0.001 mg/kg) induced significant place preference. On the other hand, animals were frequently avoiding compartment paired with the injection of DAU 6285. These findings suggest that 5-hydroxytryptamine by means of 5HT4 receptors mediates appetitive properties of morphine induced-stimuli and suggest that 5HT4 receptor may be involved in the brain reward and reinforcement processes.
Pol J Pharmacol
PMID:The effect of drugs interacting with serotonergic 5HT3 and 5HT4 receptors on morphine place conditioning. 801 74

We tested how 5-HT3 receptor antagonists, tropisetron (TR) and ondansetron (ON) affect the hyperlocomotion induced by single dose of ethanol EtOH) in mice. EtOH in a dose-dependent manner (0.5-2.0 g/kg ip) increased locomotion of mice. The effect of 2.0 g/kg of EtOH was reduced by ON (0.1 mg/kg and 1.0 mg/kg sc) and, to the lesser extent and only in limited dose range (0.01 mg/kg) by TR. Tropisetron (but not ON) increased concentrations of EtOH in the blood. The data suggest that 5-HT3 receptor is involved in EtOH-induced hyperlocomotion.
Pol J Pharmacol
PMID:Effects of 5-HT3 receptor antagonists on ethanol-induced hyperlocomotion in mice. 861 7

The effects of drugs selectively effecting central serotonergic systems on immobilization-induced analgesia (SIA) were tested in the rat. The drugs were used in dose ranges previously shown to effect emotional processes. SIA was tested using the tail withdrawal method. It was found that pretreatment of rats with para-chlorophenylalanine (p-CPA), an inhibitor of serotonin synthesis, significantly attenuated SIA, measured immediately after stress session. Ritanserin, a 5-HT2A/2C receptor antagonist, ondansetron, a 5-HT3 receptor antagonist and citalopram, a selective serotonin re-uptake blocker increased the baseline pain threshold, whereas 8-OH-DPAT, a full 5-HT1A receptor agonist and buspirone, a partial 5-HT1A receptor agonist expressing also high affinity towards dopaminergic D2 receptors, were without effect on pain perception and stress induced analgesia. It has been concluded, that modification of SIA by serotonergic drugs probably merely reflects changes in the activity of the 5-HT system on the spinal cord level, with minor, if any, contribution of supraspinal emotional centers.
Pol J Pharmacol
PMID:Influence of serotonergic drugs on restraint stress induced analgesia. 886 28

To date, more than two thousand experiments have investigated the behavioral effect of 5-HT-interacting drugs in animal models of anxiety disorders. Most of them have focused on the involvement of drugs interacting with 5-HT1A, 5-HT2A/2C and 5-HT3 receptors. Although numerous results are in line with the classic 5-HT hypothesis of anxiety, suggesting that decreased anxiety is related to decreased activity in central 5-HT neurons and vice versa, paradoxical drug effects have often been found. To explain this variability, several authors point to a determining role of the experimental paradigms used. In fact, an overview of the behavioral data arising from the vast literature indicates that conditioned procedures as well as more ethological-based tests are equal in revealing anxiolytic-like effects of drugs targetting 5-HT1A, 5-HT2A or 5-HT2C receptor subtypes. Furthermore, results obtained in ethologically-based animal models of anxiety with drugs stimulating 5-HT transmission are most consistent with the classic 5-HT hypothesis of anxiety in that they showed an increase in animals' emotional reactivity. Finally, anxiolytic-like effects of 5-HT3 receptor antagonists are in great part revealed by models based on spontaneous behaviors. Taken together, these observations lead to the conclusion that different 5-HT mechanisms, mediated by different receptor subtypes, are involved in the genesis of anxiety.
Pol J Pharmacol
PMID:Variability in the effects of 5-HT-related compounds in experimental models of anxiety: evidence for multiple mechanisms of 5-HT in anxiety or never ending story? 911 42