Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C28H35N5O4.C4H6O6 |
Molecular Weight | 655.6954 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]([C@@H](O)C(O)=O)C(O)=O.CN1N=C2CCN(C[C@@]2(CC3=CC=CC=C3)C1=O)C(=O)[C@@H](COCC4=CC=CC=C4)NC(=O)C(C)(C)N
InChI
InChIKey=MJGRJCMGMFLOET-MYPSAZMDSA-N
InChI=1S/C28H35N5O4.C4H6O6/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20;5-1(3(7)8)2(6)4(9)10/h4-13,22H,14-19,29H2,1-3H3,(H,30,35);1-2,5-6H,(H,7,8)(H,9,10)/t22-,28-;1-,2-/m11/s1
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/19174493 | http://adisinsight.springer.com/drugs/800011628
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/19174493 | http://adisinsight.springer.com/drugs/800011628
Capromorelin is a potent ghrelin receptor agonist. Capromorelin is indicated for appetite stimulation in dogs. Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs. In healthy older adults at risk for functional decline, administration of the capromorelin may improve body composition and physical function. Adverse events included fatigue, insomnia, and small increases in fasting glucose, glycosylated hemoglobin, and indices of insulin resistance.
CNS Activity
Originator
Sources: https://encrypted.google.com/patents/EP0869968A1
Curator's Comment: # Pfizer Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4616 |
7.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | ENTYCE Approved UseENTYCE is indicated for appetite stimulation in dogs Launch Date2016 |
|||
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19174493 |
Palliative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. | 2003 Feb 20 |
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Gastric motor effects of peptide and non-peptide ghrelin agonists in mice in vivo and in vitro. | 2005 Aug |
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Gateways to clinical trials. | 2007 Apr |
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Growth hormone (GH)-releasing hormone and GH secretagogues in normal aging: Fountain of Youth or Pool of Tantalus? | 2008 |
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Effects of an oral growth hormone secretagogue in older adults. | 2009 Apr |
|
The prokinetic face of ghrelin. | 2010 |
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Evidence for functional ghrelin receptors on parasympathetic preganglionic neurons of micturition control pathways in the rat. | 2010 Sep |
|
Smaller cardiac cell size and reduced extra-cellular collagen might be beneficial for hearts of Ames dwarf mice. | 2010 Sep 1 |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11322494
In rat pituitary cell cultures, Capromorelin stimulated growth hormone release with an EC50 = 3 nM.
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C76358
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD