Reactome | HTR1A binds HTR1A agonists

HTR1A binds HTR1A agonists

Stable Identifier

R-HSA-9693478

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 agonists (Homo sapiens)

General

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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.

HTR1A is seen to be a promising target for HTR1A agonist drugs to alleviate anxiety and depression in schizophrenia (Newman-Tancredi et al. 1998). The prototype HTR1A agonist drug buspirone was originally developed as an antipsychotic drug for the treatment of schizophrenia. It was found to be ineffective for the treatment of schizophrenia but clinically it showed significant anxiolytic actions (Jann 1988).

Literature References

PubMed ID	Title	Journal	Year
9760039	Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study Verrièle, L, Conte, C, Touzard, M, Gavaudan, S, Millan, MJ, Audinot, V, Chaput, C, Newman-Tancredi, A	Eur. J. Pharmacol.	1998
9205951	Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy Lavielle, G, Lochon, S, Verrièle, L, Audinot-Bouchez, V, Conte, C, Millan, MJ, Chaput, C, Newman-Tancredi, A	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 Lavielle, G, Nicolas, JP, Gobert, A, Rivet, JM, Audinot, V, Millan, MJ, Muller, O, Lejeune, F, Cussac, D, Newman-Tancredi, A	J. Pharmacol. Exp. Ther.	1998
3041384	Buspirone: an update on a unique anxiolytic agent Jann, MW	Pharmacotherapy	1988
12784105	Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology Roth, BL, Mailman, R, Renock, S, Shapiro, DA, Arrington, E, Liu, LX, Chiodo, LA, Sibley, DR	Neuropsychopharmacology	2003
15341484	Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors Van Amsterdam, C, Bartoszyk, GD, Böttcher, H, Gericke, R, Anzali, S, Heinrich, T, Greiner, HE, Seyfried, CA	J. Med. Chem.	2004
8935801	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding Leysen, JE, Lesage, AS, Gommeren, W, Janssen, PF, De Loore, K, Van Gompel, P, Luyten, WH, Schotte, A	Psychopharmacology (Berl.)	1996
12388666	Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes Millan, MJ, Cussac, D, Maiofiss, L, Newman-Tancredi, A, Boutin, JA, Audinot, V	J. Pharmacol. Exp. Ther.	2002
12177684	Pharmacology of flibanserin Jason, K, Pollentier, S, Alexander, B, Evans, K, Rohde, F, Borsini, F	CNS Drug Rev	2002
1386736	High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells Wootton, R, Strange, PG, Newman-Tancredi, A	Biochem. J.	1992
10193663	Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors Wallis, R, McHarg, A, Napier, C, Stewart, M, Hopkins, B, Melrose, H	Eur. J. Pharmacol.	1999
9986723	N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist Zgombick, JM, Audia, JE, Adham, N, Walker, C, Krushinski, J, Kohlman, DT, Liang, SX, Schaus, JM, Xu, YC	J. Med. Chem.	1999
19499624	Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders Dawson, LA, Watson, JM	CNS Neurosci Ther	2009
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 Verrièle, L, Millan, MJ, Chaput, C, Newman-Tancredi, A	Naunyn Schmiedebergs Arch. Pharmacol.	1998
21486038	Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder Nielsen, SM, Jørgensen, M, Mørk, A, Frederiksen, K, Hogg, S, Zhong, H, Jensen, KG, Ruhland, T, Bang-Andersen, B, Smith, G, Stensbøl, TB	J. Med. Chem.	2011