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Htr1a  -  5-hydroxytryptamine (serotonin) receptor...

Rattus norvegicus

Synonyms: 5-HT-1A, 5-HT1A, 5-hydroxytryptamine receptor 1A, 5HT1A, 5ht1a, ...
 
 
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Disease relevance of Htr1a

  • Antisense oligodeoxynucleotide knockdown of spinal 5-HT1A receptor attenuated spontaneous pain and reversed heat hyperalgesia in rats injected with bee venom [1].
  • 5-HT1A receptor immunoreactivity in hypothalamic neurons involved in body weight control [2].
  • We have investigated the effect of 5-HT2 receptor agonist or antagonist administration on postsynaptic 5-HT1A receptor sensitivity assessed by two behavioral measures, reciprocal forepaw treading or hypothermia induced by acute injection of the 5-HT1A receptor agonist 8-OH-DPAT [3].
  • 3. When superfused before tetanus, the 5-HT1A receptor agonist 8-hydroxydipropylamino-tetralin (8-OH-DPAT, 5 microM) prevented the expression of LTP without affecting PTP [4].
  • Evidence for the involvement of central 5-HT1A receptors in the mediation of lordosis behavior in the female rat [5].
 

Psychiatry related information on Htr1a

  • Stress sensitization of ethanol withdrawal-induced reduction in social interaction: inhibition by CRF-1 and benzodiazepine receptor antagonists and a 5-HT1A-receptor agonist [6].
  • Initial clinical trials and animal behavior studies that predict clinical activity of antidepressant drugs have reported evidence favoring the antidepressant-like activity of 5-HT1A receptor partial agonists [7].
  • Consistent with these results, stimulus generalization occurs with 5 both in rats trained to discriminate 8-OH-DPAT from saline and in rats trained to discriminate the 5-HT2 agonist DOM from saline [8].
  • Other groups of rats treated subchronically with each of the 5-HT1A agonists or antidepressants showed no increase in locomotor activity, so that general changes in activity could not account for the reduction of immobility time in the forced swim test [9].
  • NAN-190, a 5-HT 1A receptor antagonist, (-)-pindolol, a 5-HT 1A/1B receptor antagonist, and tropisetron, a 5-HT(3/4) receptor antagonist, did not affect the pain threshold in the hyperalgesic hind limb to the same extent as in the normal hind limb [10].
 

High impact information on Htr1a

  • Using acutely isolated, patch-clamped dorsal raphe neurons, we found that low concentrations of 5-HT and the 5-HT1A-selective agonist 8-OH-DPAT reversibly decrease whole-cell calcium current [11].
  • This effect is antagonized by the putative 5-HT1A-selective antagonist NAN 190 [11].
  • Since 5-HT1A receptors inhibit cAMP formation, their down-regulation argues against a negative feedback control in this system, consistent with observations in vivo [12].
  • Current through the channel could be activated by acetylcholine or, if RNA encoding a neuronal 5HT1A receptor was coinjected with atrial RNA, by serotonin (5HT) [13].
  • A 5HT-evoked current (I5HT) was observed in oocytes injected with ventricle RNA fractions (of 2.5-5.5 kb) and 5HT1A receptor RNA [13].
 

Chemical compound and disease context of Htr1a

  • In addition, some of these rats also received intraventricular pertussis toxin (PTX) injections 2 to 3 days before experimentation to abolish the postsynaptic 5-HT1A receptor-mediated membrane hyperpolarization and to unmask a 5-HT-induced depolarization [14].
  • Rats were pretreated with the 5-HT1A agonists buspirone (0, 0.5, 2.0 mg/kg, i.p.), 8-OH-DPAT (0, 0.05, 0.2 mg/kg, s.c.) or ipsapirone (0, 1.0, 2.5 mg/kg, i.p.), 45 min before decapitation [15].
  • The EB- or EB plus P-activated lordosis was also suppressed by administration of the selective 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) [5].
  • On the other hand, the 5-HT1A, 5-HT1B and beta adrenoceptor antagonists pindolol (2 mg/kg) and cyanopindolol (2 mg/kg), the 5-HT1A receptor agonist/antagonist ipsapirone (10 and 35 mg/kg) and haloperidol (0.25 and 0.5 mg/kg) showed a tendency towards enhancing the TFMPP- or m-CPP-induced hyperthermia [16].
  • Nevertheless, (+)-flesinoxan and LY 165,163 mimicked 8-OH-DPAT and WY 48,723 in eliciting a pronounced rise in plasma corticosterone and a marked hypothermia: these actions were blocked by the 5-HT1A receptor antagonist, (-)-alprenolol, but they were not affected by the alpha 1-antagonist prazosin [17].
 

Biological context of Htr1a

 

Anatomical context of Htr1a

  • Serotonergic 5-HT1A and 5-HT2A receptors are abundantly expressed in prefrontal cortex (PFC) and are targets of atypical antipsychotic drugs [23].
  • Here we showed that 1 or 4 h after a subcutaneous bee venom challenge, expression of 5-HT1A receptor mRNA in the ipsilateral lumbar spinal cord increased significantly by 80.94 or 37.86%, respectively [1].
  • Expression of 5-HT1A receptor mRNA in rat lumbar spinal dorsal horn neurons after peripheral inflammation [24].
  • The effect of blockade of 5-HT1A receptors was investigated on (1). retention in a mildly aversive passive-avoidance task, and (2). spontaneous single-unit activity of central nucleus of the amygdala (CeA) neurons, a brain site implicated in modulation of retention [25].
  • They showed a significant (P < 0.05, Mann-Whitney test) serotonin 1A (5-HT1A) mRNA expression increase in the dentate gyrus and CA3 areas of isolated animals [19].
 

Associations of Htr1a with chemical compounds

  • Serotonin 5-HT1A receptors regulate AMPA receptor channels through inhibiting Ca2+/calmodulin-dependent kinase II in prefrontal cortical pyramidal neurons [26].
  • Systemic administration of the selective 5-HT1A antagonist NAN-190 immediately after training markedly-and dose-dependently-facilitated retention in the passive-avoidance task; enhanced retention was time-dependent and was not attributable to variations in wattages of shock received by animals [25].
  • In experiment 2, six groups (N = 10) were given either saline, the 5-HT1A antagonist, WAY 100635 (0.05 mg/kg) or 8-OHDPAT (0.05 mg/kg) plus WAY 100635 (0.05 mg/kg) 20 min before a saline or cocaine (10.0 mg/kg) treatment on 9 consecutive days [27].
  • Acute and chronic administration of the selective 5-HT1A receptor antagonist WAY-405 significantly alters the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study [28].
  • Corticosterone increases 5-HT1A autoreceptor agonist affinity (+90%, p<0.001) in adrenalectomized rats [29].
 

Physical interactions of Htr1a

  • In the lateral septum, 5-HT1A receptor immunoreactivity was colocalized with the calcium-binding protein calbindin D-28k, a marker for septal GABAergic somatospiny neurons [22].
  • 5-HT1A receptor-immunoreactive GABAergic cells in the MSDB were also demonstrated to contain the calcium-binding protein parvalbumin, a marker for septohippocampal projecting GABAergic neurons [22].
  • Repeated treatment with ECS produced an increase in the density of 5-HT1A and tended to increase the specific binding of 5-HT2 serotonin receptors [30].
  • The selective degeneration of serotoninergic neurons produced by an intracerebral injection of 5,7-dihydroxytryptamine was associated only with a significant loss of 5-HT1A binding to the dorsal raphe nucleus (-60%) and of 5-HT1B binding to the substantia nigra (-37%) [31].
  • We investigated the effects of chronic systemic injections of salmon calcitonin on the [3H]-8-OHDPAT binding to 5-HT1A receptors in the frontal cortex and hippocampus in adrenalectomized and intact (non adrenalectomized) rats [32].
 

Regulatory relationships of Htr1a

  • Selective heterologous regulation of 5-HT1A receptor-stimulated 35S GTPgammaS binding in the anterior cingulate cortex as a result of 5-HT2 receptor activation [33].
  • These results suggest that both hypothalamic and extrahypothalamic CRF neurons are influenced by activation of 5-HT1A receptors [34].
  • 5-HT1B/1D receptor agonists stimulated binding in substantia nigra and in areas containing 5-HT1A receptors [35].
  • None of the three 5-HT1A agonists influenced the basal levels of renin, ACTH and prolactin but 8-OH-DPAT and buspirone increased the basal level of corticosterone in plasma [15].
  • NPY and PYY inhibited both the slow 5-HT1A receptor-mediated IPSP and the alpha 1-adrenoceptor-mediated slow EPSP while not affecting the fast, amino acid-mediated synaptic responses [36].
 

Other interactions of Htr1a

  • 5-HT1A, 5-HT2, and GABAB receptors interact to modulate neurotransmitter release probability in layer 2/3 somatosensory rat cortex as evaluated by the paired pulse protocol [37].
  • Galanin (10 nM) increases dorsal raphe 5-HT1A autoreceptor density (+65%, p<0.05) and its Kd value (+248%, p<0.05) only in adrenalectomized rats treated with corticosterone [29].
  • Dorsal raphe glucocorticoid receptors activation by corticosterone may therefore lead to an increased signalling of 5-HT1A autoreceptors that may become counteracted by galanin receptor activation [29].
  • 5-HT1A receptor immunoreactivity was also detected in a subpopulation of VAChT-containing cholinergic neurons of the MSDB [22].
  • Effects of 5-HT1A receptor agonists on hypothalamo-pituitary-adrenal axis activity and corticotropin-releasing factor containing neurons in the rat brain [34].
 

Analytical, diagnostic and therapeutic context of Htr1a

  • Adrenalectomy diminishes 5-HT1A autoreceptors affinity [29].
  • After this period they were sacrificed and their brains removed for 'in situ' hybridization study using 32P-labeled oligonucleotide probes complementary to 5-HT1A or M1 muscarinic receptor mRNA [19].
  • Systemic administration of agents that (1) increase synaptic levels of serotonin (5-HT) or dopamine (DA); (2) activate 5-HT1A, 5-HT2, D2, D3, or GABA(A) receptors; or (3) block opioid and 5-HT3 receptors decrease ethanol intake in most animal models [38].
  • 1. We have previously found that the putative 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) decreases hippocampal 5-hydroxytryptamine (5-HT) release in the anaesthetized rat, as measured by brain microdialysis [39].
  • Experimental lesions followed by binding of [3H]8-hydroxy-2-(n-dipropylamino)tetralin (8-OH-DPAT) and [3H]ketanserin to cryostat sections and quantitative autoradiography were used to investigate the cellular localization of 5-hydroxytryptamine1A (5-HT1A) and 5-hydroxytryptamine2 (5-HT2) receptors in the neocortex of the rat [40].

References

  1. 5-hydroxytryptamine1A receptor is involved in the bee venom induced inflammatory pain. Wang, W., Wu, S.X., Wang, Y.Y., Liu, X.Y., Li, Y.Q. Pain (2003) [Pubmed]
  2. 5-HT1A receptor immunoreactivity in hypothalamic neurons involved in body weight control. Collin, M., Bäckberg, M., Onnestam, K., Meister, B. Neuroreport (2002) [Pubmed]
  3. Effect of chronic serotonin-2 receptor agonist or antagonist administration on serotonin-1A receptor sensitivity. Hensler, J.G., Truett, K.A. Neuropsychopharmacology (1998) [Pubmed]
  4. Induction and maintenance of ganglionic long-term potentiation require activation of 5-hydroxytryptamine (5-HT3) receptors. Alkadhi, K.A., Salgado-Commissariat, D., Hogan, Y.H., Akpaudo, S.B. J. Physiol. (Lond.) (1996) [Pubmed]
  5. Evidence for the involvement of central 5-HT1A receptors in the mediation of lordosis behavior in the female rat. Ahlenius, S., Larsson, K., Fernandez-Guasti, A. Psychopharmacology (Berl.) (1989) [Pubmed]
  6. Stress sensitization of ethanol withdrawal-induced reduction in social interaction: inhibition by CRF-1 and benzodiazepine receptor antagonists and a 5-HT1A-receptor agonist. Breese, G.R., Knapp, D.J., Overstreet, D.H. Neuropsychopharmacology (2004) [Pubmed]
  7. Behavioral studies of serotonin receptor agonists as antidepressant drugs. Lucki, I. The Journal of clinical psychiatry. (1991) [Pubmed]
  8. N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. Glennon, R.A., Titeler, M., Lyon, R.A., Slusher, R.M. J. Med. Chem. (1988) [Pubmed]
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  10. Contribution of the peripheral 5-HT 2A receptor to mechanical hyperalgesia in a rat model of neuropathic pain. Nitanda, A., Yasunami, N., Tokumo, K., Fujii, H., Hirai, T., Nishio, H. Neurochem. Int. (2005) [Pubmed]
  11. Serotonin receptor activation reduces calcium current in an acutely dissociated adult central neuron. Penington, N.J., Kelly, J.S. Neuron (1990) [Pubmed]
  12. Long-term regulation of serotonergic activity in the rat brain via activation of protein kinase A. Foguet, M., Hartikka, J.A., Schmuck, K., Lübbert, H. EMBO J. (1993) [Pubmed]
  13. Expression of an atrial G-protein-activated potassium channel in Xenopus oocytes. Dascal, N., Lim, N.F., Schreibmayer, W., Wang, W., Davidson, N., Lester, H.A. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  14. Modification of serotonin responses in rat dorsolateral septal nucleus neurons by acute and chronic cocaine. Simms, D., Gallagher, J.P. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  15. Neuroendocrine responses to the serotonin2 agonist DOI are differentially modified by three 5-HT1A agonists. Li, Q., Rittenhouse, P.A., Levy, A.D., Alvarez Sanz, M.C., Van de Kar, L.D. Neuropharmacology (1992) [Pubmed]
  16. Hyperthermia induced by m-trifluoromethylphenylpiperazine (TFMPP) or m-chlorophenylpiperazine (m-CPP) in heat-adapted rats. Kłodzińska, A., Chojnacka-Wójcik, E. Psychopharmacology (Berl.) (1992) [Pubmed]
  17. 5-HT1A receptors and the tail-flick response. VI. Intrinsic alpha 1A-adrenoceptor antagonist properties can mask the actions of 5-HT1A receptor agonists in the spontaneous tail-flick paradigm. Millan, M.J., Rivet, J.M., Gobert, A., Canton, H., Veiga, S., Bervoets, K. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  18. Cloning, functional expression, and mRNA tissue distribution of the rat 5-hydroxytryptamine1A receptor gene. Albert, P.R., Zhou, Q.Y., Van Tol, H.H., Bunzow, J.R., Civelli, O. J. Biol. Chem. (1990) [Pubmed]
  19. Effects of isolation-rearing on serotonin-1A and M1-muscarinic receptor messenger RNA expression in the hipocampal formation of rats. Del-Bel, E.A., Joca, S.R., Padovan, C.M., Guimarães, F.S. Neurosci. Lett. (2002) [Pubmed]
  20. Activation of 5-HT1A receptors in raphe pallidus inhibits leptin-evoked increases in brown adipose tissue thermogenesis. Morrison, S.F. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2004) [Pubmed]
  21. Decreased 5-HT1A receptor gene expression and 5-HT1A receptor protein in the cerebral cortex and brain stem during pancreatic regeneration in rats. Mohanan, V., Kaimal, S.B., Paulose, C.S. Neurochem. Res. (2005) [Pubmed]
  22. 5-HT1A receptor mRNA and immunoreactivity in the rat medial septum/diagonal band of Broca-relationships to GABAergic and cholinergic neurons. Lüttgen, M., Ogren, S.O., Meister, B. J. Chem. Neuroanat. (2005) [Pubmed]
  23. Expression of serotonin1A and serotonin2A receptors in pyramidal and GABAergic neurons of the rat prefrontal cortex. Santana, N., Bortolozzi, A., Serrats, J., Mengod, G., Artigas, F. Cereb. Cortex (2004) [Pubmed]
  24. Expression of 5-HT1A receptor mRNA in rat lumbar spinal dorsal horn neurons after peripheral inflammation. Zhang, Y.Q., Gao, X., Ji, G.C., Huang, Y.L., Wu, G.C., Zhao, Z.Q. Pain (2002) [Pubmed]
  25. Enhanced retention in the passive-avoidance task by 5-HT(1A) receptor blockade is not associated with increased activity of the central nucleus of the amygdala. Schneider, A.M., Wilkins, E., Firestone, A., Everbach, E.C., Naylor, J.C., Simson, P.E. Learn. Mem. (2003) [Pubmed]
  26. Serotonin 5-HT1A receptors regulate AMPA receptor channels through inhibiting Ca2+/calmodulin-dependent kinase II in prefrontal cortical pyramidal neurons. Cai, X., Gu, Z., Zhong, P., Ren, Y., Yan, Z. J. Biol. Chem. (2002) [Pubmed]
  27. Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects. Carey, R.J., DePalma, G., Damianopoulos, E., Shanahan, A., Müller, C.P., Huston, J.P. Brain Res. (2005) [Pubmed]
  28. Acute and chronic administration of the selective 5-HT1A receptor antagonist WAY-405 significantly alters the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study. Minabe, Y., Schechter, L., Hashimoto, K., Shirayama, Y., Ashby, C.R. Synapse (2003) [Pubmed]
  29. Corticosterone strongly increases the affinity of dorsal raphe 5-HT1A receptors. Bellido, I., Hansson, A.C., Gómez-Luque, A.J., Andbjer, B., Agnati, L.F., Fuxe, K. Neuroreport (2004) [Pubmed]
  30. Effect of repeated treatment with electroconvulsive shock (ECS) on serotonin receptor density and turnover in the rat cerebral cortex. Nowak, G., Dulinski, J. Pharmacol. Biochem. Behav. (1991) [Pubmed]
  31. Quantitative autoradiography of multiple 5-HT1 receptor subtypes in the brain of control or 5,7-dihydroxytryptamine-treated rats. Vergé, D., Daval, G., Marcinkiewicz, M., Patey, A., el Mestikawy, S., Gozlan, H., Hamon, M. J. Neurosci. (1986) [Pubmed]
  32. Calcitonin increases 5-HT1A binding site densities in the brain of adrenalectomized rats. Boujrad, F., Dauphin, F., de Beaurepaire, R. Brain Res. (1998) [Pubmed]
  33. Selective heterologous regulation of 5-HT1A receptor-stimulated 35S GTPgammaS binding in the anterior cingulate cortex as a result of 5-HT2 receptor activation. Valdez, M., Burke, T.F., Hensler, J.G. Brain Res. (2002) [Pubmed]
  34. Effects of 5-HT1A receptor agonists on hypothalamo-pituitary-adrenal axis activity and corticotropin-releasing factor containing neurons in the rat brain. Owens, M.J., Edwards, E., Nemeroff, C.B. Eur. J. Pharmacol. (1990) [Pubmed]
  35. 5-Hydroxytryptamine1A and 5-hydroxytryptamine1B receptors stimulate [35S]guanosine-5'-O-(3-thio)triphosphate binding to rodent brain sections as visualized by in vitro autoradiography. Waeber, C., Moskowitz, M.A. Mol. Pharmacol. (1997) [Pubmed]
  36. Neuropeptide Y selectively inhibits slow synaptic potentials in rat dorsal raphe nucleus in vitro by a presynaptic action. Kombian, S.B., Colmers, W.F. J. Neurosci. (1992) [Pubmed]
  37. 5-HT1A, 5-HT2, and GABAB receptors interact to modulate neurotransmitter release probability in layer 2/3 somatosensory rat cortex as evaluated by the paired pulse protocol. Torres-Escalante, J.L., Barral, J.A., Ibarra-Villa, M.D., Pérez-Burgos, A., Góngora-Alfaro, J.L., Pineda, J.C. J. Neurosci. Res. (2004) [Pubmed]
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  39. Pharmacological characterization of 8-OH-DPAT-induced inhibition of rat hippocampal 5-HT release in vivo as measured by microdialysis. Sharp, T., Bramwell, S.R., Hjorth, S., Grahame-Smith, D.G. Br. J. Pharmacol. (1989) [Pubmed]
  40. 5-Hydroxytryptamine1A but not 5-hydroxytryptamine2 receptors are enriched on neocortical pyramidal neurones destroyed by intrastriatal volkensin. Francis, P.T., Pangalos, M.N., Pearson, R.C., Middlemiss, D.N., Stratmann, G.C., Bowen, D.M. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
 
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