conivaptan

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/25 16:17:29」(JST)

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Conivaptan

Systematic (IUPAC) name
N-(4-((4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
Clinical data
Trade names	Vaprisol
AHFS/Drugs.com	monograph
Pregnancy category	US: C (Risk not ruled out)
Legal status	US: ℞-only
Routes of administration	intravenous
Pharmacokinetic data
Bioavailability	N/A
Identifiers
CAS Number	210101-16-9 Y
ATC code	C03XA02
PubChem	CID: 151171
IUPHAR/BPS	2203
DrugBank	DB00872 Y
ChemSpider	133239 Y
UNII	0NJ98Y462X Y
KEGG	D01236 N
ChEBI	CHEBI:681850 Y
ChEMBL	CHEMBL1755 Y
Chemical data
Formula	C32H26N4O2
Molecular mass	498.583 g/mol
SMILES O=C(c2ccccc2c1ccccc1)Nc3ccc(cc3)C(=O)N5c6c(c4nc(nc4CC5)C)cccc6
InChI InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37) Y Key:IKENVDNFQMCRTR-UHFFFAOYSA-N Y
N (what is this?)  (verify)

Conivaptan (YM 087, brand name Vaprisol) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH), and there is some evidence it may be effective in heart failure. It is marketed by Cumberland Pharmaceuticals, Inc.

Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2). Effectively, it causes iatrogenic nephrogenic diabetes insipidus.

Conivaptan has not been approved by the FDA for the treatment of decompensated congestive heart failure. However, in theory, vasopressin receptor antagonism would be particularly useful in this setting, and an initial study shows that it has some promise.

References

UpToDate Contents

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• 1. 低ナトリウム血症の治療：抗利尿ホルモン不適合分泌（SIADH）症候群およびreset osmostat症候群 treatment of hyponatremia syndrome of inappropriate antidiuretic hormone secretion siadh and reset osmostat
• 2. 肝硬変患者における低ナトリウム血症 hyponatremia in patients with cirrhosis
• 3. 成人における低ナトリウム血症の治療の概要 overview of the treatment of hyponatremia in adults
• 4. 心不全患者における低ナトリウム血症 hyponatremia in patients with heart failure
• 5. 心不全に対する試験中および新規の治療 investigational and emerging therapies for heart failure

English Journal

• Hypertension in mice with transgenic activation of the brain renin-angiotensin system is vasopressin dependent.

• Littlejohn NK, Siel RB Jr, Ketsawatsomkron P, Pelham CJ, Pearson NA, Hilzendeger AM, Buehrer BA, Weidemann BJ, Li H, Davis DR, Thompson AP, Liu X, Cassell MD, Sigmund CD, Grobe JL.SourceDept. of Pharmacology, Roy J. and Lucille A. Carver College of Medicine, Univ. of Iowa, 51 Newton Rd., 2-307 BSB, Iowa City, IA 52242. justin-grobe@uiowa.edu.
• American journal of physiology. Regulatory, integrative and comparative physiology.Am J Physiol Regul Integr Comp Physiol.2013 May;304(10):R818-28. doi: 10.1152/ajpregu.00082.2013. Epub 2013 Mar 27.
• An indispensable role for the brain renin-angiotensin system (RAS) has been documented in most experimental animal models of hypertension. To identify the specific efferent pathway activated by the brain RAS that mediates hypertension, we examined the hypothesis that elevated arginine vasopressin (A
• PMID 23535460

• Pharmacokinetics of intravenous conivaptan in subjects with hepatic or renal impairment.

• Roy MJ, Erdman KA, Abeyratne AT, Plumb LC, Lasseter K, Riff DS, Keirns JJ.SourceAstellas Pharma Global Development, Inc., 1 Astellas Way, Northbrook, IL 60062, USA.
• Clinical pharmacokinetics.Clin Pharmacokinet.2013 May;52(5):385-95. doi: 10.1007/s40262-013-0047-8.
• BACKGROUND: Conivaptan is a non-peptide dual antagonist of vasopressin V1A and V2 receptors that is approved in the United States as an intravenous formulation for the treatment of euvolemic and hypervolemic hyponatremia in hospitalized patients. The pharmacokinetics of intravenous conivaptan had no
• PMID 23456393

• [Conivaptan inhibites cell proliferation and collagen production of cardiac fibroblasts induced by arginine vasopressin].

• Xie Y, Sun Z, Gai L.SourceDepartment of Cardiology, General Hospital of PLA, Beijing 100853, China.
• Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology.Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi.2013 May;29(5):477-80.
• Objective To investigate the effects of arginine vasopressin (AVP) and its receptor antagonist conivaptan (CON) on the proliferation of cardiac fibroblasts (CFs) and the production of collagen I and III. Methods CFs were isolated by collagenase II method and purified with differential attachment and
• PMID 23643265

Japanese Journal

• Therapeutic Potential of Vasopressin-Receptor Antagonists in Heart Failure

• Journal of Pharmacological Sciences 124(1), 1-6, 2014
• NAID 130003382634

• New Topics in Vasopressin Receptors and Approach to Novel Drugs : Research and Development of Conivaptan Hydrochloride (YM087), a Drug for the Treatment of Hyponatremia

• Journal of pharmacological sciences 109(1), 53-59, 2009-01-20
• NAID 10025733636

• A Novel Vasopressin Dual V_<1A>/V_2 Receptor Antagonist, Conivaptan Hydrochloride, Improves Hyponatremia in Rats with Syndrome of Inappropriate Secretion of Antidiuretic Hormone (SIADH)(Pharmacology)

• Biological & pharmaceutical bulletin 30(1), 91-95, 2007-01-01
• NAID 110006153273

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