Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T75984
|
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| Former ID |
TTDI01743
|
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| Target Name |
5-HT 2 receptor
|
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| Target Type |
Successful
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| Disease | Arthritis [ICD9: 710-719; ICD10: M00-M25] | ||||
| Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
| Alcohol use disorders [ICD9: 303; ICD10: F10.2] | |||||
| Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | |||||
| Depression [ICD9: 311; ICD10: F30-F39] | |||||
| Generalized anxiety disorder; Social phobia [ICD9: 300, 300.02, 300.23; ICD10: F40-F42, F40.1, F41.1, F93.2] | |||||
| Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
| Migraine [ICD9: 346; ICD10: G43] | |||||
| Psychotic disorders [ICD9: 290-299; ICD10: F20-F29] | |||||
| Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | |||||
| Schizophrenia [ICD9: 295; ICD10: F20] | |||||
| Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
| Function |
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5- dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.
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| Drugs and Mode of Action | |||||
| Drug(s) | Perospirone | Drug Info | Approved | Psychotic disorders | [1], [2] |
| Bis(olanzapine) pamoate monohydrate | Drug Info | Phase 3 | Psychotic disorders | [2] | |
| FK949E | Drug Info | Phase 3 | Alcohol use disorders | [3] | |
| Nexopamil | Drug Info | Phase 2 | Hypertension | [4] | |
| TGOF02N | Drug Info | Phase 2 | Schizophrenia | [5] | |
| TGWOOAA | Drug Info | Phase 2 | Generalized anxiety disorder; Social phobia | [6] | |
| AMAP-102 | Drug Info | Phase 1 | Arthritis | [7] | |
| ICI-170809 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [8] | |
| SUN-C5174 | Drug Info | Discontinued in Phase 2 | Peripheral vascular disease | [9] | |
| Beloxepin | Drug Info | Discontinued in Phase 1 | Depression | [10] | |
| SUN-9221 | Drug Info | Discontinued in Phase 1 | Hypertension | [11] | |
| AHR-16303B | Drug Info | Terminated | Hypertension | [12] | |
| Dotarizine | Drug Info | Terminated | Migraine | [13] | |
| E-2040 | Drug Info | Terminated | Schizophrenia | [14] | |
| Emopamil | Drug Info | Terminated | Cerebrovascular ischaemia | [15] | |
| MDL-28133A | Drug Info | Terminated | Thromboembolism | [16] | |
| NPC-18166 | Drug Info | Terminated | Psychotic disorders | [17] | |
| Modulator | AHR-16303B | Drug Info | [12] | ||
| Beloxepin | Drug Info | [18] | |||
| Bis(olanzapine) pamoate monohydrate | Drug Info | [2] | |||
| Dotarizine | Drug Info | [13] | |||
| E-2040 | Drug Info | [19] | |||
| Emopamil | Drug Info | [15] | |||
| FK949E | Drug Info | [20], [21] | |||
| ICI-170809 | Drug Info | [22] | |||
| MDL-28133A | Drug Info | [23] | |||
| Nexopamil | Drug Info | [4] | |||
| NPC-18166 | Drug Info | [24] | |||
| Perospirone | Drug Info | [25], [2] | |||
| SUN-9221 | Drug Info | [26] | |||
| TGOF02N | Drug Info | [27] | |||
| Antagonist | AMAP-102 | Drug Info | [28] | ||
| SUN-C5174 | Drug Info | [29] | |||
| TGWOOAA | Drug Info | [30] | |||
| Pathways | |||||
| KEGG Pathway | Calcium signaling pathway | ||||
| Neuroactive ligand-receptor interaction | |||||
| Gap junction | |||||
| Serotonergic synapse | |||||
| Inflammatory mediator regulation of TRP channels | |||||
| References | |||||
| REF 1 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7556). | ||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 3 | ClinicalTrials.gov (NCT02362412) Study to Evaluate the Effects of Switching Different Strength Forms of FK949E in Bipolar Disorder Patients With Major Depressive Episodes. U.S. National Institutes ofHealth. | ||||
| REF 4 | Inhibition by the combined Ca2+ and 5-HT2 receptor antagonist nexopamil (LU 49938) of intracoronary thrombus formation in a canine model of arterial stenosis and intimal damage. J Cardiovasc Pharmacol. 1993 Nov;22(5):687-94. | ||||
| REF 5 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | ||||
| REF 6 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | ||||
| REF 7 | ClinicalTrials.gov (NCT00995605) AMAP102 - Safety, Tolerability and Pharmacokinetics in Healthy Subjects. U.S. National Institutes of Health. | ||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001766) | ||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012828) | ||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001334) | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006767) | ||||
| REF 12 | AHR-16303B, a novel antagonist of 5-HT2 receptors and voltage-sensitive calcium channels. J Cardiovasc Pharmacol. 1991 Jan;17(1):41-53. | ||||
| REF 13 | Vasostabilizing effect of Dotarizine (Ca(2+)-channel blocker) on cerebrovascular reactivity in rabbits. Neurol Res. 2000 Mar;22(2):229-32. | ||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126) | ||||
| REF 15 | Calcium entry and 5-HT2 receptor blockade in oliguric ischaemic acute renal failure: effects of levemopamil in conscious rats. Br J Pharmacol. 1996 Mar;117(6):1348-54. | ||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002814) | ||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004563) | ||||
| REF 18 | WO patent application no. 2009,1055,07, Beloxepin, its enantiomers, and analogs thereof for the treatment of pain. | ||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126) | ||||
| REF 20 | D(2) and 5HT(2A) receptor occupancy of different doses of quetiapine in schizophrenia: a PET study. Eur Neuropsychopharmacol. 2001 Apr;11(2):105-10. | ||||
| REF 21 | Time course of central nervous dopamine-D2 and 5-HT2 receptor blockade and plasma drug concentrations after discontinuation of quetiapine (Seroquel) in patients with schizophrenia. Psychopharmacology(Berl). 1998 Jan;135(2):119-26. | ||||
| REF 22 | 5-HT2 receptor blockade by ICI 170,809 does not affect the inhibitory effect of the 5-HT1A receptor ligand gepirone on neuroleptic-induced catalepsy. Braz J Med Biol Res. 1994 Oct;27(10):2437-41. | ||||
| REF 23 | Effects of MDL 28,133A, a 5-HT2 receptor antagonist, on platelet aggregation and coronary thrombosis in dogs. J Cardiovasc Pharmacol. 1994 Nov;24(5):761-72. | ||||
| REF 24 | WO patent application no. 2004,0825,84, 5ht2c receptor antagonists in the treatment of schizophrenia. | ||||
| REF 25 | Pharmacological effects of zotepine and other antipsychotics on the central 5-HT2 receptors. Pharmacopsychiatry. 1993 Mar;26(2):53-8. | ||||
| REF 26 | Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56. | ||||
| REF 27 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | ||||
| REF 28 | Clinical pipeline report, company report or official report of Anamar. | ||||
| REF 29 | Synthesis and serotonin 2 (5-HT2) receptor antagonist activity of 5-aminoalkyl-substituted pyrrolo[3,2-c]azepines and related compounds. Chem Pharm Bull (Tokyo). 2000 May;48(5):623-35. | ||||
| REF 30 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | ||||
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