Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H43NO8 |
Molecular Weight | 509.6322 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12[C@H](OC(=O)CCN(C)C)[C@H](OC(C)=O)[C@@]3(C)O[C@](C)(CC(=O)[C@]3(O)[C@@]1(C)[C@@H](O)CCC2(C)C)C=C
InChI
InChIKey=RSOZZQTUMVBTMR-XGUNBQNXSA-N
InChI=1S/C27H43NO8/c1-10-24(5)15-18(31)27(33)25(6)17(30)11-13-23(3,4)21(25)20(35-19(32)12-14-28(8)9)22(34-16(2)29)26(27,7)36-24/h10,17,20-22,30,33H,1,11-15H2,2-9H3/t17-,20-,21-,22-,24-,25-,26+,27-/m0/s1
Molecular Formula | C27H43NO8 |
Molecular Weight | 509.6322 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://adisinsight.springer.com/drugs/800001302Curator's Comment: Description was created based on several sources, including
http://www.genome.jp/dbget-bin/www_bget?D01697 and https://www.ncbi.nlm.nih.gov/pubmed/12499623
Sources: http://adisinsight.springer.com/drugs/800001302
Curator's Comment: Description was created based on several sources, including
http://www.genome.jp/dbget-bin/www_bget?D01697 and https://www.ncbi.nlm.nih.gov/pubmed/12499623
Colforsin daropate (a derivative of Colforsin) is cardiotonic, adenylate cyclase activator. It is reported as an ingredient of Adehl in Japan. Colforsin daropate hydrochloride is used for the treatment of acute heart failure. Colforsin daropate is capable of directly stimulating adenylate cyclase, which in turn causes vasorelaxation via elevated intracellular concentrations of cyclic adenosine monophosphate, making it a useful therapeutic tool in treating cerebral vasospasm.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10217303
Curator's Comment: COLFORSIN DAROPATE has been reported to penetrate the blood- brain barrier after peripheral administration and can thereby be used to activate adenylyl cyclase in the CNS
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2097167 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10511949 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Adehl Approved UseAcute heart failure |
PubMed
Title | Date | PubMed |
---|---|---|
Antiinflammatory effects of colforsin daropate hydrochloride, a novel water-soluble forskolin derivative. | 2001 Jun |
|
Characterization of adenylyl cyclase isoforms in rat peripheral pulmonary arteries. | 2001 Jun |
|
Impaired intracellular signal transduction via cyclic AMP contributes to cerebral vasospasm in rats with subarachnoid hemorrhage. | 2002 Apr |
|
Influence of colforsin daropate hydrochloride on internal mammary artery grafts. | 2002 Apr |
|
Role of cyclic nucleotides in ischemia and reperfusion injury of canine livers. | 2002 Apr 15 |
|
Effect of mild hypothermia on inodilator-induced vasodilation of pial arterioles in cats. | 2002 Oct |
|
Expression of aquaporin 8 and its up-regulation by cyclic adenosine monophosphate in human WISH cells. | 2003 Apr |
|
Effect of prophylactic bronchodilator treatment with intravenous colforsin daropate, a water-soluble forskolin derivative, on airway resistance after tracheal intubation. | 2003 Jul |
|
[Colforsin daropate does not affect the cerebral blood-flow in cardiac surgery patients under cardiopulmonary bypass]. | 2004 Apr |
|
Mechanism of cicaprost-induced desensitization in rat pulmonary artery smooth muscle cells involves a PKA-mediated inhibition of adenylyl cyclase. | 2004 Aug |
|
Colforsin analogues: tritiation and characterization. | 2004 Dec |
|
Adenylyl cyclase type VI gene transfer reduces phospholamban expression in cardiac myocytes via activating transcription factor 3. | 2004 Sep 10 |
|
Antiproliferative effects of NKH477, a forskolin derivative, on cytokine profile in rat lung allografts. | 2005 Apr |
|
Effects of coleus forskohlii supplementation on body composition and hematological profiles in mildly overweight women. | 2005 Dec 9 |
|
Both milrinone and colforsin daropate attenuate the sustained pial arteriolar constriction seen after unclamping of an abdominal aortic cross-clamp in rabbits. | 2005 Jul |
|
Functional changes in adenylyl cyclases and associated decreases in relaxation responses in mesenteric arteries from diabetic rats. | 2005 Nov |
|
Chronic direct stimulation of adenylyl cyclase induces cardiac desensitization to catecholamine and beta-adrenergic receptor downregulation in rabbits. | 2006 Nov |
|
Beta-adrenoceptor-mediated vasodilation of retinal blood vessels is reduced in streptozotocin-induced diabetic rats. | 2008 Aug-Sep |
|
Colforsin-induced vasodilation in chronic hypoxic pulmonary hypertension in rats. | 2010 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12826837
0.75 ug kg-1 x min-1 colforsin daropate intravenously
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14512698
COLFORSIN DAROPATE (10(-7)-10(-5) mol/l) inhibited [(3)H]thymidine incorporation into cultured rat MCs in a concentration-dependent manner.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 04:51:36 UTC 2023
by
admin
on
Sat Dec 16 04:51:36 UTC 2023
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Record UNII |
1196KQZ976
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Record Status |
Validated (UNII)
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Record Version |
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