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)

To elucidate the mechanism of antinociceptive effects of calcitonin, we investigated whether receptor antagonists for various neurotransmitter receptors alter the inhibitory effect of calcitonin on intrathecally injected N-methyl-D-aspartate-induced aversive behavior in mice. Neither naloxone, an opioid receptor antagonist, phentolamine and benextramine, alpha-adrenoceptor antagonists, nor ritanserin, a 5-HT2A receptor antagonist, inhibited the calcitonin-induced anti-aversive effects. Pindolol and (--)-propranolol, non-selective antagonists of beta-adrenoceptors and 5-HT1 receptors, 1-(2-methoxyphenyl)-4-[4-(2-phethalimido) butyl]-piperazine hydrobromide (NAN-190), a 5-HT1A receptor antagonist, 3-tropanyl-3,5-dichlorobenzoate (MDL72222) and metoclopramide, 5-HT3 receptor antagonists, significantly inhibited the calcitonin-induced anti-aversive effects. (--)-Bicuculline, a GABAA receptor antagonist, phaclofen and 5-aminovaleric acid, GABAB receptor antagonists, also attenuated the calcitonin-induced anti-aversive effects. These results suggest that beta-adrenoceptor, 5-HT1A, 5-HT3, GABAA and GABAB receptors, but not alpha-adrenoceptor, opioid nor 5-HT2A receptors, are involved in the inhibitory effect of calcitonin on intrathecally injected N-methyl-D-aspartate-induced aversive behavior in mice.
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PMID:Neuronal mechanism of the inhibitory effect of calcitonin on N-methyl-D-aspartate-induced aversive behavior. 779 51

Using in vivo microdialysis either alone or in combination with extracellular unit recordings, we have examined the effect of serotonergic and nonserotonergic drugs applied to the dorsal raphe nucleus (DRN) on behavioural states in the cat. We found that 8-hydroxy-2-(n-dipropylamino)tetralin hydrobromide (8-OH-DPAT), a selective 5-HT1A receptor agonist, induced a dose-dependent increase in wakefulness (W) and decrease in deep slow-wave sleep (SWS), but had no significant effect on the generation of paradoxical sleep (PS) at concentrations of 5-500 microM. At the highest concentration tested, however, PS occurred directly after W, as in narcolepsy. N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-cyclohex anecarboxamide maleate (WAY-100635), a selective 5-HT1A receptor antagonist, had no effect on overall behavioural states at concentrations of 50 or 500 microM. Muscimol, a potent GABAA receptor agonist, had little or no effect at concentrations of 10, 50 or 100 microM, but concentrations of 500 or 1000 microM caused a pronounced increase in W and decrease in SWS without inducing any changes in the amount of PS, although PS episodes occurred as in narcolepsy. Bicuculline, a GABAA receptor antagonist, or kainate, an excitatory amino acid agonist, produced a dose-dependent increase in W and decrease in deep SWS and PS. Extracellular unit recordings combined with microdialysis infusion into the DRN demonstrated that only high concentrations of 8-OH-DPAT or muscimol significantly affect a large population of DRN neurons. Taken together, these findings indicate that DRN serotonergic activity does not play any crucial role in PS generation, but is involved in the regulation of W and SWS as well as in narcolepsy.
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PMID:Role of dorsal raphe neurons in paradoxical sleep generation in the cat: no evidence for a serotonergic mechanism. 1113 8

A wealth of evidence suggests a role for brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) in the aetiology of depression and in the mode of action of antidepressant drugs. Less clear is the involvement of this neurotrophin in other stress-related pathologies such as anxiety disorders. The dorsal periaqueductal grey matter (DPAG), a midbrain area rich in BDNF and TrkB receptor mRNAs and proteins, has been considered a key structure in the pathophysiology of panic disorder. In this study we investigated the effect of intra-DPAG injection of BDNF in a proposed animal model of panic: the escape response evoked by the electrical stimulation of the same midbrain area. To this end, the intensity of electrical current that needed to be applied to DPAG to evoke escape behaviour was measured before and after microinjection of BDNF. We also assessed whether 5-HT- or GABA-related mechanisms may account for the putative behavioural/autonomic effects of the neurotrophin. BDNF (0.05, 0.1, 0.2 ng) dose-dependently inhibited escape performance, suggesting a panicolytic-like effect. Local microinjection of K252a, an antagonist of TrkB receptors, or bicuculline, a GABAA receptor antagonist, blocked this effect. Intra-DPAG administration of WAY-100635 or ketanserin, respectively 5-HT1A and 5-HT2A/2C receptor antagonists, did not alter BDNF's effects on escape. Bicuculline also blocked the inhibitory effect of BDNF on mean arterial pressure increase caused by electrical stimulation of DPAG. Therefore, in the DPAG, BDNF-TrkB signalling interacts with the GABAergic system to cause a panicolytic-like effect.
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PMID:Panicolytic-like effect of BDNF in the rat dorsal periaqueductal grey matter: the role of 5-HT and GABA. 2004 14