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)

The effects of tandospirone, a novel 5-HT1A receptor-related anxiolytic, on pressor responses elicited by activation of the posterior hypothalamus were examined in alpha-chloralose-anesthetized cats and compared with those of diazepam and tofisopam. Intravenous administration of tandospirone (0.1-1 mg/kg) and diazepam (1 mg/kg) markedly inhibited the pressor responses to stimulation of the posterior hypothalamus, but did not inhibit the pressor responses to intravenous norepinephrine. The inhibition of the posterior hypothalamus-induced pressor response by tandospirone was significantly antagonized by pindolol (a 5-HT1A receptor antagonist) but not by CGS-8216 (a benzodiazepine receptor antagonist), while the latter reduced the inhibitory effects of diazepam. Tofisopam (a 2,3-benzodiazepine which lacks affinity for benzodiazepine receptors) only attenuated the posterior hypothalamus-induced pressor responses at a high dose (10 mg/kg), which was sufficient to suppress the norepinephrine-induced pressor responses. These results indicate that tandospirone, diazepam and tofisopam all inhibit the pressor response to the posterior hypothalamus activation. In addition, tandospirone and diazepam exert this effect through different mechanisms, the former probably through 5-HT1A receptors and the latter through benzodiazepine receptors.
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PMID:Effects of tandospirone, a 5-HT1A receptor-related anxiolytic, on the pressor response elicited by stimulation of the posterior hypothalamus in cats. 168 89

The activity of anxiolytic and other drugs in a light-dark test situation was studied in rats treated with the anxiogenic compound m-chlorophenyl-piperazine (mCPP). mCPP 0.5 mg/kg significantly diminished the exploratory activity of the animals in the light compartment of the apparatus. Drugs to be tested against mCPP-induced anxiety when studied alone (not in combination with mCPP) did not significantly alter the activity of rats in the light-dark apparatus, except yohimbine, which reduced the movement time values in the lit area. 1,4-Benzodiazepines [diazepam (0.1-4mg/kg) and chlordiazepoxide (2-8mg/kg)], 5-HT2A/2C antagonists [ritanserin (0.25-8 mg/kg) and deramciclane (0.5-8 g/kg)], the 5-HT3 antagonist MDL-72222 (3 mg/kg) and ethanol (2-4 mg/kg) significantly reduced the effect of mCPP. A dose-dependent increase in the exploratory activity of mCPP-treated animals was found in the 2,3-benzodiazepine girisopam (2.5-5 mg/kg)-treated groups. Tofisopam, another 2,3-benzodiazepine molecule, also showed activity against mCPP, although its effect was not statistically significant. The 5-HT1A partial agonist buspirone was also active in the dose range of 0.25-0.5 mg/kg, while the 5-HT1A full agonist 8-OH-DPAT was the only drug with presumed anxiolytic activity that clearly lacked any effect in this model. Imipramine, amitriptyline, morphine, naloxone, haloperidol, clozapine, amphetamine, yohimbine, carbamazepine and diphenylhydantoin were not effective. We conclude that mCPP-induced anxiety in the light-dark box is a potent and useful method for screening and detecting anxiolytic activity of a wide range of compounds with various modes of action.
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PMID:mCPP-induced anxiety in the light-dark box in rats--a new method for screening anxiolytic activity. 956 15