68550-75-4 Usage
Description
Cilostamide (68550-75-4) is a selective inhibitor of phosphodiesterase-3 (PDE3). Displays limited selectivity for PDE3A versus PDE3B (IC50 = 27 and 50 nM).1,2 Blocks PKB/Akt signaling pathway downstream via inhibition of Akt-activated PDE3B.3 Cilostamide reverses the effect of leptin on food intake and body weight.4
Uses
Different sources of media describe the Uses of 68550-75-4 differently. You can refer to the following data:
1. Serotonin receptor ligand
2. Cilostamide (OPC 3689) is a specific phosphodiesterase 3 (PDE3) inhibitor.
Biological Activity
Selective inhibitor of type III phosphodiesterase (PDE3). Displays moderate selectivity for PDE3A isozyme vs. PDE3B (IC 50 values are 0.027 and 0.050 μ M for PDE3A and PDE3B respectively). Inhibits ADP-induced platelet aggregation (IC 50 = 16.8 μ M); anti-thrombotic. Also available as part of the Phosphodiesterase Inhibitor Tocriset? .
Biochem/physiol Actions
Selective inhibitor of PDE3 (cGMP-inhibited phosphodiesterase); IC50 = 70 ± 9 nM. This inhibitory effect increases intracellular cAMP and inhibits platelet aggregation.
References
1) Hidaka et al. (1979), Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation; J. Pharmacol. Exp. Ther., 211 26
2) Christensen and Torphy et al. (1994), Isozyme-Selective Phosphodiesterase Inhibitors as Antiasthmatic Agents; Annu. Rep. Med. Chem., 29 185
3) Ahmad et al. (2000), Cyclic nucleotide phosphodiesterase 3B is a downstream target of protein kinase B and may be involved in regulation of effects of protein kinase B on thymidine incorporation in FDCP2 cells; J. Immunol., 164 4678
4) Zhao et al. (2002), A phosphatidylinositol 3-kinase phosphodiesterase 3B-cyclic AMP pathway in hypothalamic action of leptin on feeding; Nat. Neuroscience, 5 727
Check Digit Verification of cas no
The CAS Registry Mumber 68550-75-4 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,8,5,5 and 0 respectively; the second part has 2 digits, 7 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 68550-75:
(7*6)+(6*8)+(5*5)+(4*5)+(3*0)+(2*7)+(1*5)=154
154 % 10 = 4
So 68550-75-4 is a valid CAS Registry Number.
InChI:InChI=1/C20H26N2O3/c1-22(16-6-3-2-4-7-16)20(24)8-5-13-25-17-10-11-18-15(14-17)9-12-19(23)21-18/h9-12,14,16H,2-8,13H2,1H3,(H,21,23)
68550-75-4Relevant articles and documents
New procedure for the total synthesis of cilostamide
Seyedi, Seyed Mohammad,Sadeghian, Hamid,Arghiani, Zahra
experimental part, p. 183 - 186 (2009/04/06)
An efficient route to synthesise a wide range of N,N-R,R-4-(2-oxo-1,2- dihydroquinolin-6-yloxy)butanamide, specially Cilostamide (R = methyl and R = cyclohexyl), one of the most selective inhibitors of phosphodiesterase3 (PDE3) enzyme, from 5-methoxy-2-ni
Substituted carbostyrils as inhibitors of cyclic AMP phosphodiesterase
Lugnier,Bruch,Stoclet,et al.
, p. 121 - 125 (2007/10/02)
A series of 6-substituted carbostyrils has been synthesized and tested as inhibitors of two vascular smooth muscle phosphodiesterases, one of them selective for cyclic AMP and the other calmodulin dependent and selective for cyclic GMP. The inhibitory act
NOVEL CARBOSTYRIL DERIVATIVES
-
, (2008/06/13)
Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula wherein R1 is hydrogen, C1-4 alkyl, C2-4 alkenyl, phenyl-C1-4 alkyl-; R2 is hydrogen, a halogen atom, hydroxy, phenyl-C1-4 alkoxy; R3 is hydrogen, hydroxy, C1-4 alkyl; R4 is C3-8 cycloalkyl, substituted or unsubstituted phenyl, C3-8 cycloalkyl-C1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R5 is hydrogen, C1-8 alkyl, C2-4 alkenyl, phenyl, C3-8 cycloalkyl, phenyl-C1-4 alkyl, C3-8 cycloalkyl-C1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond
