> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/target/htr1a-7426e071-cfb2-560a-ac07-7ad1008380ff > Record changed: 2026-10-13 # HTR1A ENSG00000178394 Target class GPCR Chromosome 5 Approved drugs 13 Clinical candidates (approved and in development) 29 ## Clinical evidence **Approved drugs** 13 **Clinical candidates (approved and in development)** 29 ## Druggability **Chemical probe available** Yes ## Names **Other names** - 5-HT1A **Target name** HTR1A **Gene name** 5-hydroxytryptamine receptor 1A **Gene symbol** HTR1A **Protein name** 5-hydroxytryptamine receptor 1A (5-HT-1A) (5-HT1A) (G-21) (Serotonin receptor 1A) ### Previous gene symbols (2) - ADRB2RL1 - ADRBRL1 ## Classification **Gene biotype** Protein coding **Gene family** 5-hydroxytryptamine receptors, G protein-coupled **Target class** GPCR **Target type** Human gene ## Expression and localisation **Tissues expressed in** 4 **Highest tissue expression** 2.59 **Tissue specificity (Gini)** 0.907 **Tissue specificity (tau)** 0.955 ## Pathways and interactions **KEGG gene identifiers** - hsa:3350 **Reactome pathways** - R-HSA-390666 **Protein interaction confidence** 0.799306 **Protein interaction partners** 36 ## Genomic location **End position** 63962507 **Start position** 63957874 **Chromosome** 5 **Strand** Reverse ## Identifiers **Ensembl gene ID** ENSG00000178394 **HGNC ID** HGNC:5286 Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5286) **NCBI Gene ID** 3350 **UniProt ID** P08908 ## Cellular location - Cell membrane - Multi-pass membrane protein . Cell projection, dendrite . ### Publication evidence (5) - PubMed 22957663 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/22957663/) - PubMed 26365466 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/26365466/) - PubMed 3041227 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/3041227/) - PubMed 3138543 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/3138543/) - PubMed 8393041 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/8393041/) ## Tissue expression **Tissue specificity (tau)** 0.954761 **Expression inequality (Gini)** 0.906818 ### Highest expression Expression in transcripts per million **Brain - Frontal Cortex (BA9)** 2.59 **Brain - Cortex** 2.24 **Brain - Anterior cingulate cortex (BA24)** 1.31 **Brain - Hippocampus** 1.1 **Brain - Hypothalamus** 0.45 ### All tissues (54) Expression in transcripts per million - Brain - Frontal Cortex (BA9)2.59 - Brain - Cortex2.24 - Brain - Anterior cingulate cortex (BA24)1.31 - Brain - Hippocampus1.1 - Brain - Hypothalamus0.45 - Brain - Amygdala0.41 - Brain - Caudate (basal ganglia)0.17 - Ovary0.17 - Brain - Nucleus accumbens (basal ganglia)0.12 - Brain - Spinal cord (cervical c-1)0.06 - Testis0.06 - Brain - Substantia nigra0.05 - Brain - Putamen (basal ganglia)0.04 - Pituitary0.03 - Spleen0 - Thyroid0 - Prostate0 - Skin - Sun Exposed (Lower leg)0 - Colon - Transverse0 - Esophagus - Mucosa0 - Heart - Left Ventricle0 - Kidney - Medulla0 - Minor Salivary Gland0 - Artery - Tibial0 - Lung0 And 29 more, listed on the interactive page. ## Biological functions ### Biological processes (3) - GO:0007186 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007186) - GO:0007198 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007198) - GO:0008284 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008284) ### Cellular components - GO:0005886 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886) ### Molecular functions (4) - GO:0001586 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001586) - GO:0004993 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004993) - GO:0005515 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515) - GO:0090722 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0090722) ## On-target safety - decreased aggression ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased aggression ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased sleep ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: decreased sleep ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased memory ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased memory ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased anxiety ### Effects (2) - Inhibition/Decrease/Downregulation: acute - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased anxiety ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased body temperature ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased body temperature ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - paresthesia ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: paresthesia ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased blood pressure ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased blood pressure ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - stereotypy ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: stereotypy ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased heart rate ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: increased heart rate ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased/increased locomotor activity ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased/increased locomotor activity ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased memory ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased memory ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - dizziness ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: dizziness ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - visual disturbances ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: visual disturbances ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - growth hormone secretion ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: growth hormone secretion ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased/decreased pupil diameter ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: increased/decreased pupil diameter ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - cortisol secretion ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: cortisol secretion ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased pain ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased pain ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased adrenocorticotropic hormone ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: increased adrenocorticotropic hormone ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased/decreased sleep ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: increased/decreased sleep ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased locomotor activity ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased locomotor activity ### Biological samples (3) - nervous system - endocrine - cardiovascular PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) ## Off-target safety - cortisol secretion ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: cortisol secretion ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - growth hormone secretion ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: growth hormone secretion ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased body temperature ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased body temperature ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - reduced REM sleep ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: reduced REM sleep ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - increased adrenocorticotropic hormone ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: increased adrenocorticotropic hormone ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - potentially anxiogenic ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: potentially anxiogenic ### Biological samples (2) - central nervous system - endocrine PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) ## Related records ### Trials (818) - "Brexpiprazole (Rexulti™) Safety and Efficacy Among Filipino Patients (RAISE) - A Post Marketing Surveillance Program" - \[18F\]-F13640 as a New Brain Radiopharmaceutical - 1/2-MC4R Genotype and Pediatric Antipsychotic Drug- Induced Weight Gain - 12- Week Open Label Treatment of Refractory Bipolar Depression - 15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated - 18-Month Study of the Efficacy of Xaliproden (SR57746A) in Patients With Mild-to-Moderate Dementia of the Alzheimer's Type - A 10-Week, Open-Label, Flexible Dose Adaptive Study Evaluating the Efficacy of Vortioxetine in Subjects With Panic Disorder - A 12-week Extension Trial to Evaluate the Safety and Tolerability of Brexpiprazole in the Treatment of Subjects With Agitation Associated With Dementia of the Alzheimer's Type - A Bioequivalence Study of the Lu AA21004 20 mg and 2×10 mg Tablets - A Clinical Pharmacology Trial of Brexpiprazole Long Acting Injectable (LAI) Administered as a Single Dose in Patients With Schizophrenia - A Clinical Study That Will Assess How Food Moves Through the Stomach and Effects Blood Glucose Levels in Subjects With Schizophrenia Taking SEP-363856 or and Prior Antipsychotic (PA) Standard - A Clinical Study That Will Assess the Effect of SEP-363856 and Prior Antipsychotic (PA) Standard of Care on Glucose and Regulation of Insulin in Patients With Schizophrenia - A Clinical Study That Will Assess the Effect of SEP-363856 or Prior Antipsychotic (PA) Standard of Care on Body-weight Associated Parameters in Subjects With Schizophrenia - A Clinical Study That Will Evaluate How Well SEP-363856 Works and How Safe it is in People With Schizophrenia That Switch to SEP-363856 From Their Current Antipsychotic Medication - A Clinical Study That Will Measure How Well SEP-363856 Works and How Safe it is in Adults With Generalized Anxiety Disorder - A Clinical Study to Evaluate the Long-term Safety and Tolerability of an Investigational Drug in People With Schizophrenia - A Clinical Study to Investigate the Effect of an Investigational Drug as an Added Medication to an Antipsychotic, in Adults With Schizophrenia, as Measured Positron Emission Tomography (PET) Imaging - A Clinical Study to Learn if SEP-363856 Has Physical Dependence in Adults With Schizophrenia - A Clinical Trial Study to Determine the Effect of an Investigational Drug (SEP-363856) Has on the Way That the Drug Metformin Travels Through the Body in People With Schizophrenia. - A Clinical Trial That Will Study the Efficacy and Safety of an Investigational Drug in Acutely Psychotic People With Schizophrenia ### Drugs (38) - Adoprazine Serotonin 1a (5-HT1a) receptor agonist - Alverine Serotonin 1a (5-HT1a) receptor antagonist - Amisulpride Serotonin (5-HT) receptor antagonist - [Aripiprazole](https://trialight.com/data/asset/aripiprazole-ca9997bd-e762-4bd5-ae57-3df4e68a30dd.md) Serotonin 1a (5-HT1a) receptor partial agonist - Aripiprazole lauroxil Serotonin 1a (5-HT1a) receptor partial agonist - Befiradol Serotonin 1a (5-HT1a) receptor agonist - Bifeprunox Serotonin 1a (5-HT1a) receptor partial agonist - Brexpiprazole Serotonin 1a (5-HT1a) receptor partial agonist - Buspirone Serotonin 1a (5-HT1a) receptor partial agonist - Buspirone hydrochloride Serotonin 1a (5-HT1a) receptor partial agonist - Dexfenfluramine Serotonin (5-HT) receptor agonist - Dexfenfluramine hydrochloride Serotonin (5-HT) receptor agonist - DU 125530 Serotonin 1a (5-HT1a) receptor antagonist - Ergoloid Serotonin 1a (5-HT1a) receptor agonist - Ergoloid mesylates Serotonin 1a (5-HT1a) receptor agonist - Gepirone Serotonin 1a (5-HT1a) receptor agonist - Gepirone hydrochloride Serotonin 1a (5-HT1a) receptor agonist - GSK163090 Serotonin 1a (5-HT1a) receptor antagonist - Lecozotan Serotonin 1a (5-HT1a) receptor antagonist - Lecozotan hydrochloride Serotonin 1a (5-HT1a) receptor antagonist --- ## A note for AI agents You are probably reading this for a person. 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