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HTR1A  -  5-hydroxytryptamine (serotonin) receptor...

Canis lupus familiaris

 
 
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Disease relevance of HTR1A

  • These findings further confirm the involvement of 5-HT1A and 5-HT2 receptor in cytotoxic drug induced emesis, though the species difference in their antiemetic action can not be ruled out [1].
  • 4. Stimulation of 5-HT1A receptors alone, which is assumed to occur with flesinoxan, exerted antihypertensive activity only at low doses, without inducing reflex tachycardia at rest [2].
  • 1. Antihypertensive effects resulting from alpha 1-adrenoceptor blockade and stimulation of central nervous 5-HT1A receptors were compared with the effects arising from stimulation of 5-HT1A receptors alone during arterial hypertension [2].
 

Psychiatry related information on HTR1A

  • We report the discovery of a novel, potent, and selective amidosulfonamide nonazapirone 5-HT1A agonist for the treatment of anxiety and depression, which is now in Phase III clinical trials for generalized anxiety disorder (GAD) [3].
 

High impact information on HTR1A

  • The 5-HT1A receptor agonist flesinoxan (10, 50, 100 and 150 microg kg-1) induced a dose-dependent relaxation of the canine proximal stomach (50+/-10, 230+/-51, 290+/-38 and 275+/-33 ml, respectively; n=9-11) [4].
  • Differential addressing of 5-HT1A and 5-HT1B receptors in transfected LLC-PK1 epithelial cells: a model of receptor targeting in neurons [5].
  • 5-HT1A and 5-HT3 receptor antagonists, NAN-190 and metoclopramide, inhibited the 5-HT-stimulated increase in [Ca2+]i with pKB values of 6.3 and 6.2, respectively, indicating that the 5-HT receptors mediating Ca2+ signal had low affinity for these receptor antagonists [6].
  • 3. The contractile effects of 5-HT, sumatriptan and 8-OH-DPAT in the dog isolated saphenous vein were resistant to antagonism by the 5-HT1A receptor antagonists spiperone, spiroxatrine and pindolol (all 1 microM) [7].
  • 1. There is controversy about whether 5-HT1A receptors mediate contraction of isolated cerebral blood vessels [7].
 

Chemical compound and disease context of HTR1A

 

Biological context of HTR1A

 

Anatomical context of HTR1A

 

Associations of HTR1A with chemical compounds

  • Serotonin evoked an endothelium-dependent relaxation of prostaglandin F2 alpha-contracted rings which was inhibited by antagonists with affinity for 5-hydroxytryptamine (5-HT)1 and 5-HT2 receptors, methiothepin and metergoline, but was not mimicked or antagonized by the 5-HT1A-selective ligand, 8-hydroxy-2-di-n-propylamino tetralin [10].
  • In contrast, the dose-response curves of 5-HT-induced IPs accumulation were not shifted until the concentrations of NAN-190 and metoclopramide (5-HT1A and 5-HT3 receptor antagonists, respectively) were increased up to 10 microM [11].
  • We investigated the hypotensive activity of flesinoxan (0.1 + 0.2 + 0.7 mumol/kg), a 5-HT1A-receptor agonist, in dogs anaesthetized with either morphine and pentobarbital or enflurane and also in the conscious state [9].
  • The concentration-response curve for 5-carboxamidotryptamine (5-CT, a 5-HT1-like receptor agonist) was unaffected by propranolol (10 microM), which is reported to have affinity for 5-HT1A, 5-HT1B and 5-HT1C recognition sites [12].
  • The most potent compound, N-(endo-8-methyl-8-azabicyclo[3.2.1 oct-3-yl)-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c, ED50 = 36.3 nMi), was seven times as active as cisapride, while 8c had no affinity for 5-HT1A, 5-HT1D, D2, muscarinic M2 or muscarinic M3 receptors even at 10 microM [13].
 

Other interactions of HTR1A

References

  1. Involvement of 5-HT1A and 5-HT2 receptor in cisplatin induced emesis in dogs. Gupta, Y.K., Sharma, S.S. Indian J. Physiol. Pharmacol. (2002) [Pubmed]
  2. Influence of alpha 1-adrenoceptor blockade and/or 5-HT1A agonism on blood pressure and heart rate at rest and during exercise in hypertensive dogs. Grohs, J.G., Huber, S., Fischer, G., Raberger, G. Journal of autonomic pharmacology. (1992) [Pubmed]
  3. An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. Becker, O.M., Dhanoa, D.S., Marantz, Y., Chen, D., Shacham, S., Cheruku, S., Heifetz, A., Mohanty, P., Fichman, M., Sharadendu, A., Nudelman, R., Kauffman, M., Noiman, S. J. Med. Chem. (2006) [Pubmed]
  4. In vivo characterization of 5-HT1A receptor-mediated gastric relaxation in conscious dogs. Janssen, P., Prins, N.H., Moreaux, B., Meulemans, A.L., Lefebvre, R.A. Br. J. Pharmacol. (2003) [Pubmed]
  5. Differential addressing of 5-HT1A and 5-HT1B receptors in transfected LLC-PK1 epithelial cells: a model of receptor targeting in neurons. Langlois, X., el Mestikawy, S., Arpin, M., Triller, A., Hamon, M., Darmon, M. Neuroscience (1996) [Pubmed]
  6. 5-Hydroxytryptamine-stimulated calcium mobilization in cultured canine tracheal smooth muscle cells. Yang, C.M., Hsieh, J.T., Yo, Y.L., Ong, R., Tsao, H.L. Cell Calcium (1994) [Pubmed]
  7. Vascular 5-HT1-like receptors that mediate contraction of the dog isolated saphenous vein and carotid arterial vasoconstriction in anaesthetized dogs are not of the 5-HT1A or 5-HT1D subtype. Perren, M.J., Feniuk, W., Humphrey, P.P. Br. J. Pharmacol. (1991) [Pubmed]
  8. Alpha 1-adrenoceptor blockade and/or 5-HT1A agonism during treadmill exercise in dogs. Grohs, J.G., Fischer, G., Huber, S., Raberger, G. Journal of autonomic pharmacology. (1991) [Pubmed]
  9. Cardiovascular effects of flesinoxan in anaesthetized and conscious dogs. Grohs, J.G., Fischer, G., Raberger, G. Naunyn Schmiedebergs Arch. Pharmacol. (1990) [Pubmed]
  10. Comparison of serotonergic receptor subtypes on the smooth muscle and endothelium of the canine coronary artery. Houston, D.S., Vanhoutte, P.M. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  11. 5-Hydroxytryptamine receptor-mediated phosphoinositide hydrolysis in canine cultured tracheal smooth muscle cells. Yang, C.M., Yo, Y.L., Hsieh, J.T., Ong, R. Br. J. Pharmacol. (1994) [Pubmed]
  12. Further characterization of the 5-hydroxytryptamine 5-HT1-like receptor mediating contraction of guinea-pig iliac artery. Schoeffter, P., Sahin-Erdemli, I. Eur. J. Pharmacol. (1992) [Pubmed]
  13. Synthesis and evaluation of novel 2-oxo-1,2-dihydro-3-quinolinecarboxamide derivatives as serotonin 5-HT4 receptor agonists. Suzuki, M., Ohuchi, Y., Asanuma, H., Kaneko, T., Yokomori, S., Ito, C., Isobe, Y., Muramatsu, M. Chem. Pharm. Bull. (2000) [Pubmed]
  14. 5-HT-induced colonic contractions: enteric locus of action and receptor subtypes. Graf, S., Sarna, S.K. Am. J. Physiol. (1997) [Pubmed]
 
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