Reactome | HTR1A binds HTR1A antagonists

HTR1A binds HTR1A antagonists

Stable Identifier

R-HSA-9648268

Type

Reaction [binding]

Species

Homo sapiens

Compartment

plasma membrane, extracellular region

ReviewStatus

5/5

Locations in the PathwayBrowser

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Signal Transduction (Homo sapiens)

- Signaling by GPCR (Homo sapiens)
  - GPCR ligand binding (Homo sapiens)
    - Class A/1 (Rhodopsin-like receptors) (Homo sapiens)
      - Amine ligand-binding receptors (Homo sapiens)
        
        Serotonin receptors (Homo sapiens)
        
        HTR1A binds HTR1A antagonists (Homo sapiens)

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The serotonin 1A receptor (HTR1A), encoded by the HTR1A gene, binds the neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, that mediates inhibitory neurotransmission. HTR1A is the most widespread of all the HTR1 receptors, mainly throughout the central nervous system. Dysfunctions associated with abnormal HTR1A neurotransmission are linked to several psychiatric disorders, including anxiety, depression, and movement disorders.

Literature References

PubMed ID	Title	Journal	Year
9760039	Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study Newman-Tancredi, A, Gavaudan, S, Conte, C, Chaput, C, Touzard, M, Verrièle, L, Audinot, V, Millan, MJ	Eur. J. Pharmacol.	1998
20518729	New insight into the therapeutic role of 5-HT1A receptors in central nervous system disorders Ohno, Y	Cent Nerv Syst Agents Med Chem	2010
9205951	Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy Newman-Tancredi, A, Conte, C, Chaput, C, Verrièle, L, Audinot-Bouchez, V, Lochon, S, Lavielle, G, Millan, MJ	Naunyn Schmiedebergs Arch. Pharmacol.	1997
9732398	S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol Millan, MJ, Gobert, A, Newman-Tancredi, A, Audinot, V, Lejeune, F, Rivet, JM, Cussac, D, Nicolas, JP, Muller, O, Lavielle, G	J. Pharmacol. Exp. Ther.	1998
9067310	Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats Lejeune, F, Newman-Tancredi, A, Audinot, V, Millan, MJ	J. Pharmacol. Exp. Ther.	1997
15689356	[11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS Turner, MR, Rabiner, EA, Hammers, A, Al-Chalabi, A, Grasby, PM, Shaw, CE, Brooks, DJ, Leigh, PN	Brain	2005
10715164	2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors Glennon, RA, Lee, M, Rangisetty, JB, Dukat, M, Roth, BL, Savage, JE, McBride, A, Rauser, L, Hufeisen, S, Lee, DK	J. Med. Chem.	2000
15628665	Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells Kalipatnapu, S, Pucadyil, TJ, Harikumar, KG, Chattopadhyay, A	Biosci. Rep.	2004
9495870	Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist De Vry, J, Schohe-Loop, R, Heine, HG, Greuel, JM, Mauler, F, Schmidt, B, Sommermeyer, H, Glaser, T	J. Pharmacol. Exp. Ther.	1998
8935801	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding Schotte, A, Janssen, PF, Gommeren, W, Luyten, WH, Van Gompel, P, Lesage, AS, De Loore, K, Leysen, JE	Psychopharmacology (Berl.)	1996
16330560	A 18F-MPPF PET normative database of 5-HT1A receptor binding in men and women over aging Costes, N, Merlet, I, Ostrowsky, K, Faillenot, I, Lavenne, F, Zimmer, L, Ryvlin, P, Le Bars, D	J. Nucl. Med.	2005
9048968	Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635 Khawaja, X, Ennis, C, Minchin, MC	Life Sci.	1997
15357957	Synthesis, receptor binding and functional studies of mesoridazine stereoisomers Choi, S, Haggart, D, Toll, L, Cuny, GD	Bioorg. Med. Chem. Lett.	2004
1386736	High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells Newman-Tancredi, A, Wootton, R, Strange, PG	Biochem. J.	1992
11512051	The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor Roth, BL, Ernsberger, P, Steinberg, SA, Rao, S, Rauser, L, Savage, J, Hufeisen, S, Berridge, MS, Muzic, RF	Psychopharmacology (Berl.)	2001
11454652	SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue Watson, J, Roberts, C, Scott, C, Kendall, I, Collin, L, Day, NC, Harries, MH, Soffin, E, Davies, CH, Randall, AD, Heightman, T, Gaster, L, Wyman, P, Parker, C, Price, GW, Middlemiss, DN	Br. J. Pharmacol.	2001
15887956	Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist Ward, SE, Harrington, FP, Gordon, LJ, Hopley, SC, Scott, CM, Watson, JM	J. Med. Chem.	2005
9851589	Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist Jerning, E, Svantesson, GT, Mohell, N	Eur. J. Pharmacol.	1998
9336327	The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299 Johansson, L, Sohn, D, Thorberg, SO, Jackson, DM, Kelder, D, Larsson, LG, Rényi, L, Ross, SB, Wallsten, C, Eriksson, H, Hu, PS, Jerning, E, Mohell, N, Westlind-Danielsson, A	J. Pharmacol. Exp. Ther.	1997
11750183	Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders Kalkman, HO, Subramanian, N, Hoyer, D	Neuropsychopharmacology	2001
11714892	N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract Leonardi, A, Guarneri, L, Poggesi, E, Angelico, P, Velasco, C, Cilia, A, Testa, R	J. Pharmacol. Exp. Ther.	2001
9550290	Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists Newman-Tancredi, A, Verrièle, L, Chaput, C, Millan, MJ	Naunyn Schmiedebergs Arch. Pharmacol.	1998
12527336	Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes Hameg, A, Bayle, F, Nuss, P, Dupuis, P, Garay, RP, Dib, M	Biochem. Pharmacol.	2003
10611634	Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states Millan, MJ, Newman-Tancredi, A, Audinot, V, Cussac, D, Lejeune, F, Nicolas, JP, Cogé, F, Galizzi, JP, Boutin, JA, Rivet, JM, Dekeyne, A, Gobert, A	Synapse	2000