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

Several alpha 2-adrenoceptor compounds have been reported to recognize 5-HT1A receptors. The interaction of the alpha 2A/D- and alpha 2B/C-adrenoceptor antagonists BRL 44408 (2-[2H-(1-methyl-1,3-dihydroisoindole) methyl]-4,5-dihydroimidazole) and ARC 239 (2-[2-[4-(o-methoxyphenyl)piperazin-1-yl] ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolinedione) with 5-HT1A receptors was evaluated in rat brain. Competition experiments in cortex with both compounds against the specific binding of the 5-HT1A receptor radioligand [3H]8-OH-DPAT (8-hydroxy-2-(n-dipropyl-amine)-tetralin) yielded Ki values in the nanomolar range, fairly close to their previously reported affinities for alpha 2-adrenoceptors. Similar Ki values were obtained under alpha 2-adrenoceptor masking conditions by competition assays of these compounds against the alpha 2-adrenoceptor and 5-HT1A receptor radioligand [3H]RX 821002 (2-methoxy idazoxan) specific binding in hippocampus. The results indicate that BRL 44408 and ARC 239 recognize 5-HT1A receptors in addition to alpha 2-adrenoceptors. The fact should be considered when using these compounds to study alpha 2-adrenoceptor subtypes.
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PMID:The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. 889 22

Using in vivo extracellular recordings, we have examined the effect of the application of the prototypical 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), on the firing rate of locus coeruleus neurons. 8-OH-DPAT (1 microgram/kg, i.v.) did not modify the basal activity of the locus coeruleus but shifted to the left the dose-response curve for the clonidine induced inhibition of firing rate and reduced the corresponding ED50 by 77%. 2-[2-[4-(o-methoxyphenyl)piperazin-1-yl]ethyl]-4,4-dimethyl-1,3(2H ,4H)-isoquinolinedione (ARC 239; 75 micrograms/kg, i.v.), and chlorpromazine (75 micrograms/kg, i.v.) also shifted to the left the dose-response curve for clonidine and reduced by 38 and 46%, respectively, the ED50, while slightly increasing the basal firing rate. The results indicated that 5-HT1A receptors may modulate the responses mediated by alpha 2A-adrenoceptors in the locus coeruleus.
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PMID:Activation of 5-HT1A receptors potentiates the clonidine inhibitory effect in the locus coeruleus. 931 29

This study examined the influence of pretreatment with N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexane carboxamide maleate (WAY100635, full 5-HT1A receptor antagonist, 37 nmol) on feeding effects evoked by local injections of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT, 5-HT(1A) and 5-HT(7) receptor agonist, 6 nmol) into the LH and into the ARC of female rats adapted to a wet mash diet (enriched with 10% sucrose), during diestrus or estrus. The results showed that the LH-pretreatment with WAY100635 suppressed the hypophagic effects evoked by 8-OH-DPAT during estrus as well as diestrus. The ARC pretreatment with WAY100635 blockaded the hypophagia evoked by 8-OH-DPAT in estrus rats. The previous treatment with WAY100635 in the ARC also suppressed the feeding duration decrease evoked by 8-OH-DPAT in estrus. The latency to start feeding, the drinking behavior and the durations of other non-ingestive behaviors were not affected by the different treatments, hypothalamic regions (LH or ARC), and/or estrous cycle stages (diestrus and estrus), except for the locomotion duration increase after 8-OH-DAPT in LH-pretreated rats in diestrus. The present findings confirm our previous suggestion that ARC- and the LH-5-HT(1A) receptors participate in the serotonergic control of feeding and that these feeding-related serotonergic circuits in LH are affected by ovarian hormones, since the treatment with WAY100635 evoked a hypophagia response during the diestrus phases.
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PMID:WAY100635 blocks the hypophagia induced by 8-OH-DPAT in the hypothalamic nuclei. 2013 4