O1016
OPC-21268 hydrate
≥98% (HPLC)
同義詞:
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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About This Item
經驗公式（希爾表示法）:
C26H31N3O4 · xH2O
CAS號碼:
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 a vasopressin V1a selective antagonist.
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
Y Tashima et al.
Pflugers Archiv : European journal of physiology, 442(5), 652-661 (2001-08-21)
The intrarenal localization and role of the V1a vasopressin receptor in body fluid homeostasis are unclear. We investigated the intranephron localization of V1a receptor mRNA and protein using reverse transcription (RT)-competitive polymerase chain reaction (PCR) and immunohistochemistry with a specific
A E Bogolepova
Zhurnal evoliutsionnoi biokhimii i fiziologii, 47(1), 49-53 (2011-04-08)
Active transport of sodium ions across the isolated abdominal skin of the frog Rana temporaria after application of arginine-vasotocin (AVT) and 1-deamino-arginine-vasotocin (1dAVT) was studied by measurement of the short-circuit current (SCC). The maximal increase in the SCC values (26
[Renal action of vasopressin].
Masami Sasaki et al.
Nihon rinsho. Japanese journal of clinical medicine, 64 Suppl 2, 257-264 (2006-03-10)
A B Roald et al.
Acta physiologica Scandinavica, 182(2), 197-204 (2004-09-29)
Arginine vasopressin (AVP) might influence urinary concentration ability by altering the intrarenal distribution of glomerular filtration rate (GFR). To study this possibility we have measured the intracortical distribution of GFR following acute AVP-V1 receptor stimulation in anaesthetized female Sprague-Dawley (SPD)
C Serradeil-Le Gal et al.
Progress in brain research, 139, 197-210 (2002-11-20)
The involvement of vasopressin (AVP) in several pathological states has been reported recently and the selective blockade of the different AVP receptors could offer new clinical perspectives. During the past few years, various selective, orally active AVP V1a (OPC-21268, SR49059
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