VASOPRESSIN

First marketed in 1928

Description
Sources: Marieb E (2014). Anatomy & physiology. Glenview, IL: Pearson Education, Inc. ISBN 978-0-321-86158-0.
Curator's Comment: description was created based on several sources, including https://www.medicines.org.uk/emc/medicine/26512 https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204485Orig1s000lbl.pdf

Argipressin is a neurohypophysial hormone from the vasopressin hormone family. Its two primary functions are to retain water in the body and to constrict blood vessels. The antidiuretic action of Argipressin is ascribed to increase in reabsorption of water by the renal tubules. Argipressin can cause contraction of smooth muscle of the gastrointestinal tract, gall bladder, urinary bladder and all parts of the vascular bed, especially the capillaries, small arterioles and venules with less effect on the smooth musculature of the large veins. Agripressin for injections is used for use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices. In addition, argipressin is indicated to increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vasopressin V1a receptor 17 Target ID: P37288 Gene ID: 552.0 Gene Symbol: AVPR1A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21688787	Agonist 2678	0.24 nM [EC50]
Vasopressin V1b receptor 6 Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21688787	Agonist 2678	0.05 nM [EC50]
Vasopressin V2 receptor 15 Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21688787	Agonist 2678	4.3 nM [EC50]

Conditions

Condition	Modality	Highest Phase	Product
Diabetes insipidus 3 Sources: https://www.medicines.org.uk/emc/medicine/26512	Primary	Approved 8429	Argipressin 20 IU/ml Solution for Injection Approved Use For use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices.
Oesophageal varices 1 Sources: https://www.medicines.org.uk/emc/medicine/26512	Primary	Approved 8429	Argipressin 20 IU/ml Solution for Injection Approved Use For use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices.
Vasodilatory shock 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204485Orig1s000lbl.pdf	Primary	Approved 8429	VASOSTRICT Approved Use To increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines. Launch Date 2014
Post-operative abdominal distention 1 Sources: https://www.drugs.com/pro/vasopressin.html	Palliative	Approved 8429	PITRESSIN Approved Use Vasopressin Injection, USP is indicated for prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows and in diabetes insipidus
Abdominal roentgenography 1 Sources: https://www.drugs.com/pro/vasopressin.html	Diagnostic	Approved 8429	PITRESSIN Approved Use Vasopressin Injection, USP is indicated for prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows and in diabetes insipidus.

PubMed

Title	Date	PubMed
Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.	1994 Feb 4	8106369
Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.	1995	7475979
Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.	1995 May 15	7774575
Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.	1996 Nov 18	8955347
1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.	1997 Jun 1	9264324
The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.	1997 Oct	9322919
Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.	1997 Oct 17	9334232
Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.	1998 Dec	9884074
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.	1998 Dec	9864265
Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.	1998 Jan	9459574
Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.	2000 Jul	10866830
Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.	2001 Jul 20	11337500
[1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.	2002 Dec	12446593
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.	2004 Apr 22	15084136
Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.	2005 Nov	16158071

Patents

Sample Use Guides

In Vivo Use Guide

For treatment of diabetes insipidus: A dose of 0.25ml to 1ml (5 to 20 units) by subcutaneous or intramuscular injection every four hours. For the initial control of variceal bleeding Argipressin should be given intravenously. Argipressin, 20 units diluted in 100ml dextrose 5% w/v may be infused over a 15 minute period.

Route of Administration: Other

In Vitro Use Guide

Agonist activity of compound at the human vasopressin V1aR was determined in a reporter gene assays (RGA) in HEK293 cells by transiently cotransfecting recombinant vasopressin V1aR expression vectors and the reporter plasmid containing a luciferase gene under the control of NFAT response elements (NFAT-luciferase). Argipressin activates V1aR with EC50 of 0.24 nM.

Name

Type

Language

VASOPRESSIN

Official Name

English

ARGIPRESSIN

Preferred Name

English

VASOPRESSIN, 8-ARGININE

Common Name

English

VASOPRESSIN [USP MONOGRAPH]

Common Name

English

ARGIPRESSIN [MART.]

Common Name

English

CYS-TYR-PHE-GLN-ASN-CYS-PRO-ARG-GLY-NH2 (1-6 DISULFIDE)

Common Name

English

VASOPRESSIN [VANDF]

Common Name

English

ARGININE VASOPRESSIN

Common Name

English

VASOPRESSIN [USP-RS]

Common Name

English

VASOPRESSIN [ORANGE BOOK]

Common Name

English

ARGININE VASOPRESSIN [MI]

Common Name

English

argipressin [INN]

Common Name

English

Vasopressin [WHO-DD]

Common Name

English

VASOSTRICT

Brand Name

English

VASOPRESSIN COMPONENT OF HBN-1

Common Name

English

CYS-TYR-PHE-GLN-ASN-CYS-PRO-ARG-GLY-NH2 (1-6 DISULPHIDE)

Common Name

English

VASOPRESSIN, 8-L-ARGININE-

Common Name

English

Argipressin [WHO-DD]

Common Name

English

HBN-1 COMPONENT VASOPRESSIN

Common Name

English

8-L-ARGININEVASOPRESSIN

Common Name

English

Classification Tree Code System Code

LOINC

26928-2