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Details

Stereochemistry ACHIRAL
Molecular Formula C32H26N4O2
Molecular Weight 498.5744
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CONIVAPTAN

SMILES

CC1=NC2=C(N1)C3=C(C=CC=C3)N(CC2)C(=O)C4=CC=C(NC(=O)C5=C(C=CC=C5)C6=CC=CC=C6)C=C4

InChI

InChIKey=IKENVDNFQMCRTR-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Molecular Formula C32H26N4O2
Molecular Weight 498.5744
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Conivaptan is an arginine vasopressin (AVP) receptor antagonist with affinity for AVP receptor subtypes V1A and V2. The antidiuretic action of AVP is mediated through activation of the V2 receptor, which functions to regulate water and electrolyte balance at the level of the collecting ducts in the kidney. Conivaptan was approved in 2004 for hyponatremia caused by syndrome of inappropriate antidiuretic hormone. Conicaptan is being evaluated for reduce intracranial pressure in patients with traumatic brain injury, and as a treatment for heart failure.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.43 nM [Ki]
0.36 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VAPRISOL IN 5% DEXTROSE IN PLASTIC CONTAINER
Palliative
Unknown
Palliative
Unknown
Palliative
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
2681 ng/mL
50 mg single, intravenous
CONIVAPTAN plasma
Homo sapiens
619 ng/mL
40 mg/kg single, intravenous
CONIVAPTAN plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
4813 ng × h/mL
50 mg single, intravenous
CONIVAPTAN plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.1 h
50 mg single, intravenous
CONIVAPTAN plasma
Homo sapiens
5 h
40 mg/kg single, intravenous
CONIVAPTAN plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
40 mg/kg single, intravenous
CONIVAPTAN plasma
Homo sapiens

Doses

AEs

OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
IV: 20 mg infused over 30 minutes as a loading dose, followed by a continuous infusion of 20 mg over 24 hours (0.83 mg/hour) for 2 to 4 days; may increase to a maximum dose of 40 mg over 24 hours (1.7 mg/hour) if serum sodium not rising sufficiently; total duration of therapy not to exceed 4 days. Note: If patient requires 40 mg/24 hours, may administer two consecutive 20 mg/100 mL premixed solutions over 24 hours (ie, 20 mg over 12 hours followed by 20 mg over 12 hours).
Route of Administration: Intravenous
In Vitro Use Guide
Binding of conivaptan with recombinant human vasopressin V1a and V2 receptors was studied using [3H]-Arg-vasopressin as a radioligand. Conivaptan binds to V1a with Ki of 0.43 and to V2 receptor with Ki of 0.36 nM.
Substance Class Chemical
Record UNII
0NJ98Y462X
Record Status Validated (UNII)
Record Version