DescriptionSources: https://www.drugs.com/mmx/diapid.htmlCurator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&varApplNo=016755
Sources: https://www.drugs.com/mmx/diapid.html
Curator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&varApplNo=016755
Lypressin is synthetic analog of porcine antidiuretic hormone vasopressin. Itis a cyclic nonapeptide that differs from Arg-vasopressin by one amino acid, containing Lys at residue 8 instead of Arg. Lypressin-containing nasal spray was used to treat diabetes insipidus, but its marketing by Sandoz (Novartis) was discontinued.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2363078 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8393786 |
7.3 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | DIAPID Approved UseIncreases water reabsorption in the kidney by increasing the cellular permeability of the collecting ducts, resulting in an increase in urine osmolality with a concurrent decrease in urine output. Lypressin is indicated for the prevention or control of polydipsia, polyuria, and dehydration associated with central diabetes insipidus caused by insufficient antidiuretic hormone. |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/mmx/diapid.html
Adults: lypressin spray (diapid) contains contains approximately 0.007 mg lypression per spray. (equivalent to 2 Posterior Pituitary Units). For treatment of diabetes insipidus, 1-2 sprays should be administered in each nostril 4 times daily.
Route of Administration:
Nasal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8393786
V2[Lys8]VP-receptor was transfected into COS7 cells. The displacement experiments were performed with 10 nM [3H] [Arg8]VP in the presence of 0.1 - 10000 nM lypressin. Incubation was performed for 30 min at 30°C in duplicate. Bound ligand was separated from free ligand by filtering the incubation mixture through Whatman GF/B filters soaked in 0.05% bovine serum albumin. Lypressin binds to vasopressin receptor with Ki of 7.3 nM.
| Substance Class |
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| Sequence Type | COMPLETE |
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7CZF3L922Y
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C80212
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WHO-VATC |
QH01BA03
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H01BA03
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ACTIVE MOIETY |
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_9] | 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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