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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
Structure of COLFORSIN DAROPATE

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

HIDE SMILES / InChI

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

Description
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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Adehl

Approved Use

Acute heart failure
PubMed

PubMed

TitleDatePubMed
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

0.75 ug kg-1 x min-1 colforsin daropate intravenously
Route of Administration: Intravenous
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 Sat Dec 16 04:51:36 UTC 2023
Edited
by admin
on Sat Dec 16 04:51:36 UTC 2023
Record UNII
1196KQZ976
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
COLFORSIN DAROPATE
Common Name English
.BETA.-ALANINE, N,N-DIMETHYL-, (3R,4AR,5S,6S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO(2,1-B)PYRAN-6-YL ESTER
Common Name English
Code System Code Type Description
FDA UNII
1196KQZ976
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
DRUG CENTRAL
729
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
EPA CompTox
DTXSID20150415
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
CAS
113462-26-3
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
PUBCHEM
444029
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY