Target Information
| Target General Information | Top | |||||
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| Target ID |
T59679
(Former ID: TTDS00107)
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| Target Name |
5-HT 4 receptor (HTR4)
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| Synonyms |
Serotonin receptor 4; 5-hydroxytryptamine receptor 4; 5-HT4 receptor; 5-HT4; 5-HT-4
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| Gene Name |
HTR4
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Gastro-oesophageal reflux disease [ICD-11: DA22] | |||||
| 2 | Irritable bowel syndrome [ICD-11: DD91] | |||||
| Function |
The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MDKLDANVSSEEGFGSVEKVVLLTFLSTVILMAILGNLLVMVAVCWDRQLRKIKTNYFIV
SLAFADLLVSVLVMPFGAIELVQDIWIYGEVFCLVRTSLDVLLTTASIFHLCCISLDRYY AICCQPLVYRNKMTPLRIALMLGGCWVIPTFISFLPIMQGWNNIGIIDLIEKRKFNQNSN STYCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAHQIQMLQRAGASSESRP QSADQHSTHRMRTETKAAKTLCIIMGCFCLCWAPFFVTNIVDPFIDYTVPGQVWTAFLWL GYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYRRPSILGQTVPCSTTTINGSTHVLRD AVECGGQWESQCHPPATSPLVAAQPSDT Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Cisapride | Drug Info | Approved | Gastroesophageal reflux disease | [2], [3] | |
| 2 | HTF 919 | Drug Info | Approved | Constipation | [4], [5] | |
| 3 | R0-93877 | Drug Info | Approved | Irritable bowel syndrome | [6] | |
| 4 | Tegaserod | Drug Info | Approved | Irritable bowel syndrome | [4] | |
| Clinical Trial Drug(s) | [+] 17 Clinical Trial Drugs | + | ||||
| 1 | Renzapride | Drug Info | Phase 3 | Irritable bowel syndrome | [7], [8] | |
| 2 | DSP-6952 | Drug Info | Phase 2 | Constipation | [9] | |
| 3 | Lintopride | Drug Info | Phase 2 | Nausea | [10] | |
| 4 | PF-885706 | Drug Info | Phase 2 | Gastroesophageal reflux disease | [11] | |
| 5 | Piboserod | Drug Info | Phase 2 | Atrial fibrillation | [12], [13] | |
| 6 | PRX-3140 | Drug Info | Phase 2 | Post-traumatic stress disorder | [14] | |
| 7 | SB-207266A | Drug Info | Phase 2 | Irritable bowel syndrome | [15] | |
| 8 | SPD-557 | Drug Info | Phase 2 | Diabetic gastroparesis | [16] | |
| 9 | TD-5108 | Drug Info | Phase 2 | Gastroparesis | [17], [18] | |
| 10 | TD-8954 | Drug Info | Phase 2 | Gastrointestinal disease | [19] | |
| 11 | YKP-GI | Drug Info | Phase 2 | Constipation | [20], [21] | |
| 12 | BIMU-1 | Drug Info | Phase 1 | Cognitive impairment | [22], [23] | |
| 13 | DA-6886 | Drug Info | Phase 1 | Irritable bowel syndrome | [24] | |
| 14 | M-0004 | Drug Info | Phase 1 | Gastroesophageal reflux disease | [25] | |
| 15 | PF-04995274 | Drug Info | Phase 1 | Alzheimer disease | [26] | |
| 16 | SER-101 | Drug Info | Phase 1 | Congestive heart failure | [27] | |
| 17 | SUVN-D4010 | Drug Info | Phase 1 | Alzheimer disease | [28], [29] | |
| Discontinued Drug(s) | [+] 10 Discontinued Drugs | + | ||||
| 1 | E-3620 | Drug Info | Discontinued in Phase 2 | Gastric motility disorder | [30] | |
| 2 | Fabesetron | Drug Info | Discontinued in Phase 2 | Irritable bowel syndrome | [31] | |
| 3 | Naronapride | Drug Info | Discontinued in Phase 2 | Gastroesophageal reflux disease | [32] | |
| 4 | Norcisapride | Drug Info | Discontinued in Phase 2 | Gastroesophageal reflux disease | [33] | |
| 5 | SL65.0155 | Drug Info | Discontinued in Phase 2 | Parkinson disease | [34], [35] | |
| 6 | TD-2749 | Drug Info | Discontinued in Phase 1 | Gastrointestinal disease | [36] | |
| 7 | DAU-6285 | Drug Info | Terminated | Vomiting | [37], [38] | |
| 8 | LY-353433 | Drug Info | Terminated | Inflammatory bowel disease | [39] | |
| 9 | SC-53116 | Drug Info | Terminated | Gastric motility disorder | [40], [41] | |
| 10 | SK-951 | Drug Info | Terminated | Gastrointestinal disease | [42] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 25 Agonist drugs | + | ||||
| 1 | Cisapride | Drug Info | [1], [43] | |||
| 2 | HTF 919 | Drug Info | [44] | |||
| 3 | R0-93877 | Drug Info | [45] | |||
| 4 | Tegaserod | Drug Info | [8] | |||
| 5 | Mosapride | Drug Info | [46] | |||
| 6 | DSP-6952 | Drug Info | [48] | |||
| 7 | PF-885706 | Drug Info | [49] | |||
| 8 | SPD-557 | Drug Info | [51] | |||
| 9 | TD-5108 | Drug Info | [43], [46] | |||
| 10 | YKP-GI | Drug Info | [53] | |||
| 11 | DA-6886 | Drug Info | [51] | |||
| 12 | M-0004 | Drug Info | [51] | |||
| 13 | PF-04995274 | Drug Info | [54] | |||
| 14 | SUVN-D4010 | Drug Info | [28], [29] | |||
| 15 | Naronapride | Drug Info | [58] | |||
| 16 | SL65.0155 | Drug Info | [60] | |||
| 17 | TD-2749 | Drug Info | [61] | |||
| 18 | SK-951 | Drug Info | [65] | |||
| 19 | alpha-methyl-5-HT | Drug Info | [69] | |||
| 20 | ER-21018 | Drug Info | [51] | |||
| 21 | RQ-00000010 | Drug Info | [51] | |||
| 22 | RS 57639 | Drug Info | [69] | |||
| 23 | RS 67333 | Drug Info | [79] | |||
| 24 | RS67506 | Drug Info | [80] | |||
| 25 | SUVN-1004028 | Drug Info | [51] | |||
| Modulator | [+] 16 Modulator drugs | + | ||||
| 1 | Renzapride | Drug Info | [47] | |||
| 2 | Lintopride | Drug Info | [10] | |||
| 3 | PRX-3140 | Drug Info | [50] | |||
| 4 | TD-8954 | Drug Info | [52] | |||
| 5 | BIMU-1 | Drug Info | [23] | |||
| 6 | E-3620 | Drug Info | [56] | |||
| 7 | Fabesetron | Drug Info | [57] | |||
| 8 | DAU-6285 | Drug Info | [62] | |||
| 9 | SC-53116 | Drug Info | [64] | |||
| 10 | (R)-zacopride | Drug Info | [66] | |||
| 11 | MDDR 287569 | Drug Info | [4], [73] | |||
| 12 | ML-10302 | Drug Info | [75] | |||
| 13 | SC-52491 | Drug Info | [82] | |||
| 14 | SC-54750 | Drug Info | [82] | |||
| 15 | SDZ-205-557 | Drug Info | [83] | |||
| 16 | VRX-03011 | Drug Info | [84] | |||
| Antagonist | [+] 15 Antagonist drugs | + | ||||
| 1 | Piboserod | Drug Info | [45] | |||
| 2 | SB-207266A | Drug Info | [45] | |||
| 3 | SER-101 | Drug Info | [55] | |||
| 4 | LY-353433 | Drug Info | [63] | |||
| 5 | SB 203186 | Drug Info | [44] | |||
| 6 | AF-3473 | Drug Info | [51] | |||
| 7 | GR 125487 | Drug Info | [71] | |||
| 8 | ML 10375 | Drug Info | [74] | |||
| 9 | R-116712 | Drug Info | [76] | |||
| 10 | RO 116 1148 | Drug Info | [77] | |||
| 11 | RS 100235 | Drug Info | [78] | |||
| 12 | RS 116 0086 | Drug Info | [77] | |||
| 13 | SB 204070 | Drug Info | [69] | |||
| 14 | [11C]SB207145 | Drug Info | [85] | |||
| 15 | [123I]SB 207710 | Drug Info | [51] | |||
| Inhibitor | [+] 7 Inhibitor drugs | + | ||||
| 1 | Norcisapride | Drug Info | [59] | |||
| 2 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [67] | |||
| 3 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [68] | |||
| 4 | BARETTIN | Drug Info | [70] | |||
| 5 | GR-113808 | Drug Info | [72] | |||
| 6 | SB-207710 | Drug Info | [81] | |||
| 7 | SEROTONIN | Drug Info | [70] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | cAMP signaling pathway | |||||
| 3 | Neuroactive ligand-receptor interaction | |||||
| 4 | Serotonergic synapse | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
| 2 | 5HT4 type receptor mediated signaling pathway | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Excitatory Neural Signalling Through 5-HTR 4 and Serotonin | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Serotonin receptors | |||||
| 2 | G alpha (s) signalling events | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Serotonin Receptor 4/6/7 and NR3C Signaling | |||||
| 2 | Monoamine GPCRs | |||||
| 3 | GPCRs, Class A Rhodopsin-like | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5... Endocr Relat Cancer. 2009 Mar;16(1):281-90. | |||||
| REF 2 | URL: 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: 240). | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020210. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006410) | |||||
| REF 6 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 7 | URL: 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: 244). | |||||
| REF 8 | Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. | |||||
| 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 800034751) | |||||
| REF 10 | The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9. | |||||
| REF 11 | ClinicalTrials.gov (NCT00730665) Efficacy And Safety Of PF-00885706 For The Relief Of Symptoms In Subjects With Gastro-esophageal Reflux Disease (GERD). U.S. National Institutes of Health. | |||||
| REF 12 | URL: 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: 225). | |||||
| REF 13 | ClinicalTrials.gov (NCT00421746) A Clinical Study Assessing the Potential of Piboserod for the Treatment of Heart Failure. U.S. National Institutes of Health. | |||||
| 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 800021864) | |||||
| REF 15 | Clinical pipeline report, company report or official report of Department of Pharmacology University of Wisconsin School of Medicine. | |||||
| REF 16 | ClinicalTrials.gov (NCT01370863) An Explorative Trial to Evaluate the Pharmacodynamic Effect of SPD557 on Reflux Parameters in Refractory GERD Patients. U.S. National Institutes of Health. | |||||
| REF 17 | URL: 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: 8425). | |||||
| REF 18 | ClinicalTrials.gov (NCT00391820) Evaluate the Safety and Efficacy of a 5-HT4 Agonist in Chronic Constipation (ACCORD Trial). U.S. National Institutes of Health. | |||||
| REF 19 | ClinicalTrials.gov (NCT03827655) A Study of TAK-954 to Treat Gastrointestinal Dysfunction in Adults After Surgery. U.S. National Institutes of Health. | |||||
| REF 20 | URL: 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: 8427). | |||||
| REF 21 | ClinicalTrials.gov (NCT01989234) A Multicenter, Double-Blind, Randomized, Placebo-Controlled, 12-Week, Dose-Range-Finding Trial of YKP10811 Capsules Administered Once Daily to Subjects With Chronic Idiopathic Constipation. U.S. National Institutes of Health. | |||||
| REF 22 | URL: 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: 234). | |||||
| REF 23 | Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45. | |||||
| REF 24 | ClinicalTrials.gov (NCT01633723) Phase I Clinical Trial of DA-6886 in Healthy Male Subjects. U.S. National Institutes of Health. | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026666) | |||||
| REF 26 | ClinicalTrials.gov (NCT01193062) Study In Healthy Subjects To Evaluate The Changes In The Protein sAPP-Alpha In Cerebrospinal Fluid Following A Single Oral Dose Of PF-04995274. U.S. National Institutes of Health. | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033318) | |||||
| REF 28 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 29 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004004) | |||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001434) | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019926) | |||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007174) | |||||
| REF 34 | URL: 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: 29). | |||||
| REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014352) | |||||
| REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021879) | |||||
| REF 37 | URL: 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: 246). | |||||
| REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002002) | |||||
| REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007508) | |||||
| REF 40 | URL: 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: 238). | |||||
| REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003270) | |||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011740) | |||||
| REF 43 | The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47. | |||||
| REF 44 | 5-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58. | |||||
| REF 45 | Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32. | |||||
| REF 46 | The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37. | |||||
| REF 47 | Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63. | |||||
| REF 48 | DSP-6952, a high affinity serotonin (5-HT4) receptor partial agonist. Sumitomo Dainippon Pharma Co. Ltd. | |||||
| REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025579) | |||||
| REF 50 | Clinical pipeline report, company report or official report of Nanotherapeutics. | |||||
| REF 51 | URL: 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. (Target id: 9). | |||||
| REF 52 | The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011 May 30;2:25. | |||||
| REF 53 | A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015 Apr;13(4):701-8.e1. | |||||
| REF 54 | Pharmacokinetics, safety and tolerability of PF04995274: A 5HT4 partial agonist being developed for the treatment of Alzheimer's disease. Alzheimer's and Dementia. | |||||
| REF 55 | Phase I clinical trail of SER101 (RO1160367) for treating heart failure leukemia. Roche. | |||||
| REF 56 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 57 | Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther. 1993 May;265(2):752-8. | |||||
| REF 58 | Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders. Aliment Pharmacol Ther. 2012 Apr;35(7):745-67. | |||||
| REF 59 | mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83. | |||||
| REF 60 | SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther. 2002 Aug;302(2):731-41. | |||||
| REF 61 | A Hybrid Structural Approach to Analyze Ligand Binding by the Serotonin Type 4 Receptor (5-HT4). Mol Cell Proteomics. 2013 May; 12(5): 1259-1271. | |||||
| REF 62 | The novel 5-HT4 receptor antagonist DAU 6285 antagonizes 5-hydroxytryptamine-induced tachycardia in pigs. Eur J Pharmacol. 1993 Mar 23;233(2-3):295-7. | |||||
| REF 63 | LY353433, a potent, orally effective, long-acting 5-HT(4) receptor antagonist: comparison to cisapride and RS23597-190. J Pharmacol Exp Ther. 1996 Apr;277(1):97-104. | |||||
| REF 64 | Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3073-5. | |||||
| REF 65 | Identification of SK-951, a novel benzofuran derivative, as an agonist to 5-HT4 receptors. Jpn J Pharmacol. 1999 Feb;79(2):203-12. | |||||
| REF 66 | R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):283-9. | |||||
| REF 67 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28. | |||||
| REF 68 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
| REF 69 | [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors. Neuropharmacology. 1997 Apr-May;36(4-5):671-9. | |||||
| REF 70 | Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4. | |||||
| REF 71 | Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor. FEBS Lett. 1996 Nov 25;398(1):19-25. | |||||
| REF 72 | Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers. J Med Chem. 2007 Sep 6;50(18):4482-92. | |||||
| REF 73 | Phase II study of Cilengitide (EMD 121974, NSC 707544) in patients with non-metastatic castration resistant prostate cancer, NCI-6735. A study by the DOD/PCF Prostate Cancer Clinical Trials Consortium. Invest New Drugs. 2012 April; 30(2): 749-757. | |||||
| REF 74 | Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling. Br J Pharmacol. 2000 Jun;130(3):527-38. | |||||
| REF 75 | Intestinal motor stimulation by the 5-HT4 receptor agonist ML10302: differential involvement of tachykininergic pathways in the canine small bowel ... Neurogastroenterol Motil. 2001 Dec;13(6):543-53. | |||||
| REF 76 | Mapping of serotonin 5-HT(4) receptor mRNA and ligand binding sites in the post-mortem human brain. Synapse. 2000 Apr;36(1):35-46. | |||||
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