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 general purpose of the present study was to analyze the possible interactions between the GABA benzodiazepine and the serotonin systems in the mediation of the antianxiety actions of 5-HT1A compounds. The anxiolytic effect of buspirone (5 mg/kg), ipsapirone (5 mg/kg), indorenate (5 mg/kg), and 8-OH-DPAT (0.5 mg/kg) was established in the rat burying behavior test. Flumazenil (5 mg/kg), but not bicuculline (2.5 mg/kg), effectively counteracted the reduction in burying behavior produced by buspirone, ipsapirone, and 8-OH-DPAT. These same 5-HT1A compounds, at subthreshold doses, produced an important reduction in burying behavior when combined with diazepam (0.25 mg/kg). The effect of indorenate was not altered by any of the antagonists and, when combined with diazepam it produced large increases in burying behavior latency. Only buspirone alone and in combination with bicuculline or flumazenil impaired motor coordination as tested in the rota rod. Data are discussed on the bases of the interaction between the GABAergic and serotonergic systems, stressing species differences and variations due to the animal model of anxiety.
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PMID:Modification of the anxiolytic action of 5-HT1A compounds by GABA-benzodiazepine agents in rats. 961 Sep 20

Various clinical studies suggest that many features of OCD are influenced by sex, age and fluctuations in hormonal levels. Animal models have confirmed these differences, and suggest they are mediated by the serotonergic system. We compared the perseveration behavior in a T-maze after the administration of the 5-HT1A agonist, 8-OH-DPAT (2.0 mg/kg) and the preventive action of subchronic fluoxetine (10 mg/kg, 3 times) in middle-aged (11-14 months) males and female rats in two endocrine states: irregular cycles (tested in diestrus) or persistent diestrus. After 8-OH-DPAT, females with persistent diestrus presented higher perseveration scores than males and females with irregular cycles. Fluoxetine produced an anticompulsive-like effect only in females with persistent diestrus. Females in persistent diestrus showed higher estradiol levels than those in irregular cycles or males. In all groups 8-OH-DPAT increased ambulation and fluoxetine did not modify this action. In males, the combined administration of fluoxetine and 8-OH-DPAT impaired motor coordination. Data are discussed on the basis of estradiol levels and sex differences.
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PMID:Sex- and endocrine-stage-differences in middle-aged rats in an animal model of OCD. 2339 68

Since serotonin (5-HT) is strongly involved in the etiology and pathophysiology of depression, the development of new antidepressants is still based on the serotonergic system. The complexity of serotonergic system provides an opportunity for the development of compounds with multiple and complementary mechanism of action. This study describes serotonin receptor profile, functional characterization, and pharmacological in vivo evaluation of new aroxyalkyl derivatives of 2-methoxyphenylpiperazine. The obtained results allowed for the identification of compound 3, (1-[3-(2,6-dimethylphenoxy)propyl]-4-(2-methoxyphenyl)piperazine hydrochloride), a partial 5-HT1A receptor agonist, and 5-HT2A receptor antagonist, with high affinity toward 5-HT7 receptors, showing antidepressant- and anxiolytic-like properties. Moreover, 5-HT1A receptor activation is crucial for the antidepressant-like activity of compound 3. The rest of the compounds (except compounds 1 and 9) showed antidepressant but not anxiolytic-like properties, which did not result from 5-HT1A receptors activation. Furthermore, the compounds are 5-HT1A and weak 5-HT3 receptors antagonists, and some of them 5-HT2A antagonists. Moreover, none of the studied compounds impaired motor coordination at antidepressant-like doses. Since the studied compounds exhibited activity in behavioral assays and interacted with various receptors, the results of our experiments are very promising and require further studies.
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PMID:Antidepressant-like activity of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and evidence for the involvement of serotonin receptor subtypes in their mechanism of action. 2664 62