COLFORSIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H34O7
Molecular Weight	410.5012
Optical Activity	UNSPECIFIED
Defined Stereocenters	8 / 8
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12[C@H](O)[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=OHCQJHSOBUTRHG-KGGHGJDLSA-N

InChI=1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(26)17(28-12(2)23)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1380607 | https://adisinsight.springer.com/drugs/800001302

Colforsin (NKH477) is a water-soluble forskolin derivative. NKH477, like forskolin, showed adenylate cyclase stimulant activity in guinea pig ventricular membrane but did not inhibit Na+, K(+)-ATPase or phosphodiesterase (PDE) activity. The compound was developed by a Japanese company Nippon Kayaku. Colforsin daropate, a prodrug of colforsin, is marketed in Japan for the treatment of acute heart failure under tradename Adehl.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adenylate cyclase 13 Target ID: CHEMBL2097167 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8612348	Activator 1430

PubMed

Title	Date	PubMed
Induced cytoskeletal changes in bovine pulmonary artery endothelial cells by resveratrol and the accompanying modified responses to arterial shear stress.	2001	11178103
Prostacyclin inhibits the production of MMP-9 induced by phorbol ester through protein kinase A activation, but does not affect the production of MMP-2 in Human cultured mesangial cells.	2001	11174002
Activation of 5-HT receptors that stimulate the adenylyl cyclase pathway positively regulates IGF-I in cultured craniofacial mesenchymal cells.	2001	11173928
Differential neuronal localizations and dynamics of phosphorylated and unphosphorylated type 1 inositol 1,4,5-trisphosphate receptors.	2001	11166129
Function of a truncated glucocorticoid receptor form at a negative glucocorticoid response element in the proopiomelanocortin gene.	2001 Feb	11174853
Rapid modulation of Na+/K+-ATPase activity in osmoregulatory tissues of a salmonid fish.	2001 Feb	11171352
The growth hormone-releasing hormone receptor: desensitisation following short-term agonist exposure.	2001 Feb	11169166
Functional and molecular characterization of receptor subtypes mediating coronary microvascular dilation to adenosine.	2001 Feb	11162132
The phosphodiesterase inhibitors pentoxifylline and rolipram suppress macrophage activation and nitric oxide production in vitro and in vivo.	2001 Feb	11161985
Differential actions of PKA and PKC in the regulation of glutamate release by group III mGluRs in the entorhinal cortex.	2001 Feb	11160494
Parathyroid hormone-induced up-regulation of connexin-43 messenger ribonucleic acid (mRNA) is mediated by sequences within both the promoter and the 3'untranslated region of the mRNA.	2001 Feb	11159864
Glucocorticoids protect against apoptosis induced by serum deprivation, cyclic adenosine 3',5'-monophosphate and p53 activation in immortalized human granulosa cells: involvement of Bcl-2.	2001 Feb	11159853
Stimulation of mitogen-activated protein kinase by gonadotropin-releasing hormone in human granulosa-luteal cells.	2001 Feb	11159838
beta(2)-adrenoceptor agonists inhibit release of eosinophil-activating cytokines from human airway smooth muscle cells.	2001 Feb	11159726
Cysteine residues in the D-galactose-H+ symport protein of Escherichia coli: effects of mutagenesis on transport, reaction with N-ethylmaleimide and antibiotic binding.	2001 Feb 1	11171069
Membrane depolarization mediates phosphorylation and nuclear translocation of CREB in vascular smooth muscle cells.	2001 Feb 1	11161711
GH mRNA levels are elevated by forskolin but not GH releasing hormone in GHRH receptor-expressing MtT/S somatotroph cell line.	2001 Feb 14	11165046
Intracellular pathways regulating ciliary beating of rat brain ependymal cells.	2001 Feb 15	11179397
Regulation of neuregulin expression in the injured rat brain and cultured astrocytes.	2001 Feb 15	11160396
Schwann cell proliferative responses to cAMP and Nf1 are mediated by cyclin D1.	2001 Feb 15	11160381
Thyroid hormone activation in human vascular smooth muscle cells: expression of type II iodothyronine deiodinase.	2001 Feb 16	11179199
LDL downregulates CYP51 in porcine vascular endothelial cells and in the arterial wall through a sterol regulatory element binding protein-2-dependent mechanism.	2001 Feb 16	11179193
Opioid-induced adenylyl cyclase supersensitization in human embryonic kidney 293 cells requires pertussis toxin-sensitive G proteins other than G(i1) and G(i3).	2001 Feb 16	11166929
Group III metabotropic glutamate receptors in rat cultured calvarial osteoblasts.	2001 Feb 23	11181052
Involvement of K(ATP) channels in diethylstilbestrol-induced relaxation in rat aorta.	2001 Feb 9	11173069
The proteasome inhibitor MG132 promotes accumulation of the steroidogenic acute regulatory protein (StAR) and steroidogenesis.	2001 Feb 9	11172811
Prostaglandin E2 and vasoactive intestinal peptide increase vascular endothelial cell growth factor mRNAs in lung cancer cells.	2001 Feb-Mar	11165399
Regulation of human neutrophil-mediated cartilage proteoglycan degradation by phosphatidylinositol-3-kinase.	2001 Jan	11168638
NAAG inhibits KCl-induced [(3)H]-GABA release via mGluR3, cAMP, PKA and L-type calcium conductance.	2001 Jan	11168538
Possible role of bradykinin and angiotensin II in the regulation of penile erection and detumescence.	2001 Jan	11164180
Proline transport in MDCK cells expressing a mutant regulatory subunit of cAMP-dependent protein kinase.	2001 Jan	11161828
G protein and cAMP-dependent protein kinase mediate amyloid beta-peptide inhibition of neuronal glucose uptake.	2001 Jan	11161593
Reduced neuritic outgrowth and cell adhesion in neuronal cells transfected with human alpha-synuclein.	2001 Jan	11161475
Relationships between lipolysis induced by various lipolytic agents and hormone-sensitive lipase in rat fat cells.	2001 Jan	11160373
Inhibition of stimulated Jurkat cell adenosine 3',5'-cyclic monophosphate synthesis by the immunomodulatory compound HR325.	2001 Jan 15	11163337
Relaxation of rat aorta by adenosine in diabetes with and without hypertension: role of endothelium.	2001 Jan 19	11166736
Regulation of osteoprotegerin secretion from primary cultures of human bone marrow stromal cells.	2001 Jan 26	11162596
cAMP mediated upregulation of CYP2A5 in mouse hepatocytes.	2001 Jan 26	11162586
Mechanisms of phospholipase C activation by the vasoactive intestinal polypeptide/pituitary adenylate cyclase-activating polypeptide type 2 receptor.	2001 Mar	11181537
Regulation and actions of Smad7 in the modulation of activin, inhibin, and transforming growth factor-beta signaling in anterior pituitary cells.	2001 Mar	11181520
Expression of tyrosinase-related protein 2/DOPAchrome tautomerase in the retinoblastoma.	2001 Mar	11180971
3',5'-cyclic adenosine monophosphate regulates expression of synaptotagmin in neonatal sympathetic ganglia in vitro.	2001 Mar	11180155
Selective enhancement of l-type calcium currents by corticotropin in acutely isolated rat amygdala neurons.	2001 Mar	11179456
Vascular beta-adrenergic receptor system is dysfunctional after myocardial infarction.	2001 Mar	11179056
Adenosine signaling in outer medullary descending vasa recta.	2001 Mar	11171666
Regulation of slow wave frequency by IP(3)-sensitive calcium release in the murine small intestine.	2001 Mar	11171626
G-protein-coupled receptor kinase 3- and protein kinase C-mediated desensitization of the PACAP receptor type 1 in human Y-79 retinoblastoma cells.	2001 Mar	11166332
(S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord.	2001 Mar	11166323
Model of the 3-D structure of the GLUT3 glucose transporter and molecular dynamics simulation of glucose transport.	2001 Mar 1	11170207
Second messenger modulation of electrotonic coupling between region CA3 pyramidal cell axons in the rat hippocampus.	2001 Mar 2	11172925

Patents

Name

Type

Language

COLFORSIN

Official Name

English

HL 362

Code

English

COLFORSIN [MI]

Common Name

English

NSC-375489

Code

English

HL-362

Code

English

FORSKOLIN [USP-RS]

Common Name

English

FORSKOLIN

Common Name

English

L 75 1362B

Code

English

colforsin [INN]

Common Name

English

COLFORSIN [MART.]

Common Name

English

Colforsin [WHO-DD]

Common Name

English

FORSKOLIN (CONSTITUENT OF FORSKOHLII) [DSC]

Common Name

English

COLFORSIN [USAN]

Common Name

English

NSC-357088

Code

English

FORSKOLIN [VANDF]

Common Name

English

L-751362B

Code

English

(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-Dodecahydro-5,6,10,10b-tetrahydroxy-3,4a,7,7,10a-pentamethyl-3-vinyl-1H-naphtho[2,1-b]pyran-1-one 5-acetate

Common Name

English

L-75-1362B

Code

English

Classification Tree Code System Code

DSLD

151 (Number of products:123)