Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H37N5O3 |
Molecular Weight | 455.593 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC(=O)N1CCC(CN2CCC(CNC(=O)C3=C4NC(=NC4=CC=C3)C(C)C)CC2)CC1
InChI
InChIKey=MZOITCJKGUIQEI-UHFFFAOYSA-N
InChI=1S/C25H37N5O3/c1-17(2)23-27-21-6-4-5-20(22(21)28-23)24(31)26-15-18-7-11-29(12-8-18)16-19-9-13-30(14-10-19)25(32)33-3/h4-6,17-19H,7-16H2,1-3H3,(H,26,31)(H,27,28)
Molecular Formula | C25H37N5O3 |
Molecular Weight | 455.593 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
TD 8954 (also known as TAK 954) is a selective serotonin 5-HT(4) receptor agonist. It is known a potential role for potent and efficacious 5-HT(4) receptor agonists in the treatment of Alzheimer's disease (AD). TD 8954 participated in phase I clinical trials to study its potential role in the treatment of AD. However, this study was discontinued. In addition, TD 8954 is involved in phase II clinical trials to investigate its effect on gastrointestinal and colonic transit in diabetic or idiopathic gastroparesis participants and for the prophylaxis and treatment of postoperative gastrointestinal dysfunction in participants undergoing large- and small-bowel resection.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Participation of 5-HT3, 5-HT4, and nicotinic receptors in the peristaltic reflex of guinea pig distal colon. | 1996 Nov |
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Rationale for using serotonergic agents to treat irritable bowel syndrome. | 2005 Apr 1 |
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Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. | 2013 Jul 15 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03281577
TAK-954 0.1; 0.3; 1 milligram (mg), 60-minute infusion, intravenous (IV), once daily for up to 3 days.
Route of Administration:
Intravenous
Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 18:17:56 GMT 2023
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on
Sat Dec 16 18:17:56 GMT 2023
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Record UNII |
35F0Y2W16Q
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Record Status |
Validated (UNII)
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Related Record | Type | Details | ||
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TARGET -> AGONIST |
Comments Maximum compound-evoked response 83% expressed as a percentage of the maximum response evoked by 5-HT.
BINDING
EC50
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TARGET -> AGONIST |
BINDING
Ki
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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PERMEABILITY | PHARMACOKINETIC |
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