DescriptionSources: 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
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
Curator's Comment: As a neurotransmitter and/or neuromodulator VP can modulate CNS autonomic systems controlling heart rate, arterial blood pressure, respiration rate, and sleep patterns, however, physiological significance is not understood. VP may also have an effect on certain learned behaviors, in the development of some complex social problems, and in the pathogenesis of complex psychiatric diseases such as depression.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P37288 Gene ID: 552.0 Gene Symbol: AVPR1A Target Organism: Homo sapiens (Human) |
0.24 nM [EC50] | ||
Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) |
0.05 nM [EC50] | ||
Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) |
4.3 nM [EC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Argipressin 20 IU/ml Solution for Injection Approved UseFor use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices. |
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| Primary | Argipressin 20 IU/ml Solution for Injection Approved UseFor use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices. |
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| Primary | VASOSTRICT Approved UseTo increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines. Launch Date2014 |
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| Palliative | PITRESSIN Approved UseVasopressin Injection, USP is indicated for prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows and in diabetes insipidus |
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| Diagnostic | PITRESSIN Approved UseVasopressin 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 |
|---|---|---|
| Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. | 2005-11 |
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| Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. | 2004-04-22 |
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| [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. | 2002-12 |
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| Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor. | 2001-07-20 |
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| Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463. | 2000-10 |
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| Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding. | 2000-07 |
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| Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes. | 2000-04 |
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| Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. | 1999-10 |
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| Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. | 1998-12 |
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| OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats. | 1998-12 |
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| Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist. | 1998-01 |
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| Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist. | 1997-10-17 |
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| The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways. | 1997-10 |
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| 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor. | 1997-06-01 |
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| Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin. | 1996-11-18 |
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| Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. | 1995-05-15 |
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| Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells. | 1995 |
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| Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor. | 1994-02-04 |
Patents
Sample Use Guides
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
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.
| Substance Class |
Protein
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| Protein Type | HORMONE |
| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
2UU6C9U95P
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| Record Status |
Validated (UNII)
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914200-83-2
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2UU6C9U95P
Created by
admin on Wed Apr 02 19:35:17 GMT 2025 , Edited by admin on Wed Apr 02 19:35:17 GMT 2025
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| MOIETY | ACETATE ION | 569DQM74SC | ||||
| AMINO ACID SUBSTITUTION | [1_9] | C-TERMINUS | GLYCINE |
Amount:
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GLYCINAMIDE | 4JDT453NWO |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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