O1016
OPC-21268 hydrate
≥98% (HPLC)
别名:
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 hydrate
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所有图片(1)
About This Item
经验公式（希尔记法）:
C26H31N3O4 · xH2O
CAS号:
分子量:
449.54 (anhydrous basis)
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.77
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化驗
≥98% (HPLC)
形狀
powder
顏色
white to off-white
溶解度
DMSO: ≥20 mg/mL
起源
Merck & Co., Inc., Kenilworth, NJ, U.S.
儲存溫度
2-8°C
SMILES 字串
O.CC(=O)NCCCOc1ccc(cc1)C(=O)N2CCC(CC2)N3C(=O)CCc4ccccc34
InChI
1S/C26H31N3O4.H2O/c1-19(30)27-15-4-18-33-23-10-7-21(8-11-23)26(32)28-16-13-22(14-17-28)29-24-6-3-2-5-20(24)9-12-25(29)31;/h2-3,5-8,10-11,22H,4,9,12-18H2,1H3,(H,27,30);1H2
InChI 密鑰
QTCWOUIERWBMQV-UHFFFAOYSA-N
生化／生理作用
OPC-21268 is one of 2 non-peptide V1a selective antagonists, along with SR-49059. Arginine vasopressin (AVP) is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes-V1a, V1b, and V2 - all belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF.
特點和優勢
This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral - Aquatic Acute 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Sho Maejima et al.
General and comparative endocrinology, 157(2), 196-202 (2008-06-17)
Anuran amphibians do not drink orally but absorb water osmotically through the highly permeable ventral skin. In this cutaneous water absorption, roles of the putative cerebral osmoreceptors and functions of arginine vasotocin (AVT) were examined in the central nervous system
Chun-Ping Chu et al.
Neuroscience research, 53(2), 147-155 (2005-07-26)
The present study is an investigation of the responses of the cardiovascular system and Fos expression to intracerebroventricular (i.c.v.) administration of hypertonic saline (HS) in conscious arginine vasopressin (AVP)-overexpressing transgenic (Tg) and control rats. Central HS (0.3, 0.67, or 1.0M
James Walter Ferguson et al.
Clinical science (London, England : 1979), 105(1), 1-8 (2003-03-18)
Vasopressin, or antidiuretic hormone, is a peptide hormone that is released from the posterior pituitary gland in response to changes in blood pressure and plasma osmolality. The main pathophysiological states associated with high plasma vasopressin concentrations are cirrhosis, cardiac failure
Kazushige Tachikawa et al.
American journal of physiology. Endocrinology and metabolism, 285(6), E1161-E1166 (2003-08-14)
Although arginine vasopressin (AVP), an antidiuretic hormone, has been widely acknowledged to play an important role in cardiovascular regulation via V1a receptors (V1aR), its precise significance remains unclear. In this study, we investigated the effects of long-standing high plasma AVP
Nina Japundzić-Zigon et al.
Journal of pharmacological sciences, 95(1), 47-55 (2004-05-22)
Effects of V(1) (OPC-21268) and V(2) (OPC-31260) vasopressin antagonists on blood pressure (BP) short-term variability were investigated in adult spontaneously hypertensive rats (SHR) under basal conditions and after the stimulation of vasopressin release by hemorrhage. BP was recorded intra-arterially and
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