OPC-21268,OPC21268|cas 131631-89-5

Cas No.:	131631-89-5
Chemical Name:	Fuscoside
Synonyms:	OPC-21268;OPC21268;1-(1-(4-(3-Acetylaminopropoxy)benzoyl)-4-piperidyl)-3,4-dihydro-2(1H)-quinolinone;N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide;OPC 21268;N-[3-(4-{[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]carbonyl}phenoxy)propyl]acetamide;N-[3-[4-[4-(2-Oxo-1,2,3,4-tetrahydro-1-quinolinyl)piperidin-1-ylcarbonyl]phenoxy]propyl]acetamide;OPC-21268;OPC-21268 hydrate;1-[1-[4-(3-Acetylaminopropoxy)benzoyl]-4-piperidyl]-3,4-dihydroquinolin-2(1H)-one;1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate;N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide;N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate;Fuscoside;N-[3-[4-[[4-(3，4-Dihydro-2-oxo-1(2H)quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide;EX-A593;OPC-21268;OPC21268;AC-35504;J-006031;131631-89-5;BCP14853;DA-46083;L001417;Acetamide, N-(3-(4-((4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl)carbonyl)phenoxy)propyl)-;CHEMBL296908;OPC 21268?;AKOS024457877;NCGC00370961-01;SCHEMBL3504368;OPC-1268;BRD-K19426040-001-01-1;GTPL2196;BDBM50029644;DTXSID70927295;33U7944QCQ;HY-15009;N-(3-{4-[4-(2-Oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl]phenoxy}propyl)ethanimidic acid;N-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide;1262770-69-3;CS-0003694;Acetamide, N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-;N-(3-{4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy}propyl)acetamide;N-(3-{4-[4-(2-Oxo-3,4-dihydro-2H-quinolin-1-yl)-piperidine-1-carbonyl]-phenoxy}-propyl)-acetamide;MS-28145;Q27088205
SMILES:	O=C1CCC2C=CC=CC=2N1C1CCN(C(C2C=CC(=CC=2)OCCCNC(C)=O)=O)CC1
Formula:	C₂₆H₃₁N₃O₄
M.Wt:	449.54
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	OPC-21268 is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
Target:	IC50: 0.4 μM (vasopressin V1) Ki: 0.14 μM (vasopressin V1)[1]
In Vivo:	OPC-21268 competitively and specifically antagonizes pressor responses to AVP in vivo. Oral administration of OPC-21268 (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose- and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg[1]. OPC-21268 predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. OPC-21268 treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages[2].
In Vitro:	The concentration of OPC-21268 that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of OPC-21268 for V1 receptors (0.14 μM)[1].
Kinase Assay:	Liver and kidney plasma membranes are prepared from Sprague-Dawley rats of 300 to 400 g. Various concentrations of AVP and OPC-21268 are incubated with 50 μg of liver membranes or 600 μg of kidney membranes in 0.25 ml of tris buffer (100 mM, pH 8.0) containing 5 mM MgCI2, 1 mM EDTA, 0.1% bovine serum albumin, and 1.9 nM [3H]AVP (53.6 Ci/mmol) in the liver or 3.8 nM [3H]AVP in the kidney. After incubation for 10 min at 37°C (liver membranes) or 4 hours at 4°C (kidney membranes), 3 mL of ice-cold Tris buffer (100 mM, pH 8.0) is added to each assay tube, and bound and free ligands are separated by filtration through a glass microfiber filter and then washed three times. Specific binding is determined by subtraction of the nonspecific binding, which is measured in the presence of 1 μM unlabeled AVP[1].
Animal Administration:	Rats[1] Male Sprague-Dawley rats, 300 to 400 g, are injected with OPC-21268 (0.1, 0.3, 1 mg/kg). OPC-21268 is given 2 min before the injection of AVP at 30 mU/kg i.v., angiotensin II at 0.3 μg/kg i.v., and noradrenaline at 3 μg/kg i.v.[1].
References:	[1]. Yamamura Y, et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science. 1991 Apr 26;252(5005):572-4. [2]. Bemana I, et al. Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats. Neurosurgery. 1999 Jan;44(1):148-54.

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Fuscoside