Conivaptan

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MedKoo CAT#: 317564

CAS#: 210101-16-9

Description: 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.


Chemical Structure

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Conivaptan
CAS# 210101-16-9

Theoretical Analysis

MedKoo Cat#: 317564
Name: Conivaptan
CAS#: 210101-16-9
Chemical Formula: C32H26N4O2
Exact Mass: 498.20558
Molecular Weight: 498.57
Elemental Analysis: C, 77.09; H, 5.26; N, 11.24; O, 6.42

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Synonym: YM-087; YM 087; YM087; Conivaptan; Conivaptan; Vaprisol

IUPAC/Chemical Name: N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide

InChi Key: IKENVDNFQMCRTR-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: CC1=NC2=C(N1)CCN(C3=CC=CC=C32)C(=O)C4=CC=C(C=C4)NC(=O)C5=CC=CC=C5C6=CC=CC=C6

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 498.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Decker D, Collier L, Lau T, Olivera R, Roma G, Leonardo C, Seifert H, Rowe D, Pennypacker KR. The Effects of Clinically Relevant Hypertonic Saline and Conivaptan Administration on Ischemic Stroke. Acta Neurochir Suppl. 2016;121:243-50. doi: 10.1007/978-3-319-18497-5_43. PubMed PMID: 26463956.

2: Zeynalov E, Jones SM, Seo JW, Snell LD, Elliott JP. Arginine-Vasopressin Receptor Blocker Conivaptan Reduces Brain Edema and Blood-Brain Barrier Disruption after Experimental Stroke in Mice. PLoS One. 2015 Aug 14;10(8):e0136121. doi: 10.1371/journal.pone.0136121. eCollection 2015. PubMed PMID: 26275173; PubMed Central PMCID: PMC4537303.

3: Rajan S, Srikumar S, Paul J, Kumar L. Effectiveness of single dose conivaptan for correction of hyponatraemia in post-operative patients following major head and neck surgeries. Indian J Anaesth. 2015 Jul;59(7):416-20. doi: 10.4103/0019-5049.160943. PubMed PMID: 26257414; PubMed Central PMCID: PMC4523962.

4: Howard MS, Boddu SH, Mauro VF, Churchwell MD. Compatibility of conivaptan injection with select cardiovascular medications. Am J Health Syst Pharm. 2014 Sep 15;71(18):1534-5. doi: 10.2146/ajhp140193. Erratum in: Am J Health Syst Pharm. 2014 Nov 1;71(21):1830. PubMed PMID: 25174012.

5: Buckley MS, Patel SA, Hattrup AE, Kazem NH, Jacobs SC, Culver MA. Conivaptan for treatment of hyponatremia in neurologic and neurosurgical adults. Ann Pharmacother. 2013 Sep;47(9):1194-200. doi: 10.1177/1060028013503126. Review. PubMed PMID: 24259735.

6: Breshears JD, Jiang B, Rowland NC, Kunwar S, Blevins LS. Use of conivaptan for management of hyponatremia following surgery for Cushing's disease. Clin Neurol Neurosurg. 2013 Nov;115(11):2358-61. doi: 10.1016/j.clineuro.2013.08.019. Epub 2013 Aug 27. PubMed PMID: 24041963.

7: Ban K, Sonohara R, Yoshida M, Sako K, Uchida S, Namiki N. Pharmaceutical development of a parenteral formulation of conivaptan hydrochloride. PDA J Pharm Sci Technol. 2013 Jul-Aug;67(4):336-53. doi: 10.5731/pdajpst.2013.00926. PubMed PMID: 23872444.

8: Xie Y, Sun Z, Gai L. [Conivaptan inhibites cell proliferation and collagen production of cardiac fibroblasts induced by arginine vasopressin]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2013 May;29(5):477-80. Chinese. PubMed PMID: 23643265.

9: Peters S, Kuhn R, Gardner B, Bernard P. Use of conivaptan for refractory syndrome of inappropriate secretion of antidiuretic hormone in a pediatric patient. Pediatr Emerg Care. 2013 Feb;29(2):230-2. doi: 10.1097/PEC.0b013e318280d6ca. PubMed PMID: 23546432.

10: Dominguez M, Perez JA, Patel CB. Efficacy of 3% saline vs. conivaptan in achieving hyponatremia treatment goals. Methodist Debakey Cardiovasc J. 2013 Jan-Mar;9(1):49-53. PubMed PMID: 23519387; PubMed Central PMCID: PMC3600885.

Conivaptan

10.0mg / Not available