SR 121463

Identification

Name
SR 121463
Accession Number
DB05455
Description

SR 121463 is a nonpeptide aquaretic compound with potent selective antagonism of the vasopressin V2 (V1b) receptor subtype. It is a candidate for control of hyponatremia and in the treatment of syndrome of inappropriate secretion of anti-diuretic hormone (SIADH).

Type
Small Molecule
Groups
Investigational
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Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in cardiovascular disorders, in the treatment of syndrome of inappropriate secretion of anti-diuretic hormone (SIADH) and in hyponatremia.

Contraindications & Blackbox Warnings
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Pharmacodynamics

Increases urine volume through selective antagonism of V1b/V2 receptors.

Mechanism of action

Selectively antagonizes v1b receptors.

TargetActionsOrganism
UVasopressin V1b receptorNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
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Toxicity

Phase 11b showed a good clinical safety profile.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Soupart A, Gross P, Legros JJ, Alfoldi S, Annane D, Heshmati HM, Decaux G: Successful long-term treatment of hyponatremia in syndrome of inappropriate antidiuretic hormone secretion with satavaptan (SR121463B), an orally active nonpeptide vasopressin V2-receptor antagonist. Clin J Am Soc Nephrol. 2006 Nov;1(6):1154-60. Epub 2006 Oct 11. [PubMed:17699341]
  2. Palm C, Pistrosch F, Herbrig K, Gross P: Vasopressin antagonists as aquaretic agents for the treatment of hyponatremia. Am J Med. 2006 Jul;119(7 Suppl 1):S87-92. [PubMed:16843091]
  3. Bardoux P, Bruneval P, Heudes D, Bouby N, Bankir L: Diabetes-induced albuminuria: role of antidiuretic hormone as revealed by chronic V2 receptor antagonism in rats. Nephrol Dial Transplant. 2003 Sep;18(9):1755-63. [PubMed:12937221]
PubChem Substance
347910149

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Vasopressin receptor activity
Specific Function
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system.
Gene Name
AVPR1B
Uniprot ID
P47901
Uniprot Name
Vasopressin V1b receptor
Molecular Weight
46970.345 Da

Drug created on November 18, 2007 11:25 / Updated on June 12, 2020 10:52

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