Saralasin is an angiotensin II analogue which was developed for the treatment of hypertension in 1970s. For many years saralasin was supposed to be angiotensin receptors blocker, but recent studies have revealed that its pharmacological action can be explained by agonistic behavior toward angiotensin II receptor. The drug was approved by FDA under the name Sarenin, however, it is no longer available on the market.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2094256 |
0.38 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
Sources: DOI: 10.1007/978-1-4613-3822-2 J. Strauss, Acute Renal Disorders and Renal Emergencies (1984), page 164, retrieved from: https://books.google.es/books?id=B_QGCAAAQBAJ&dq |
Primary | SARENIN Approved UseUnknown Launch Date1981 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Angiotensin modulates long-term memory expression but not long-term memory storage in the crab Chasmagnathus. | 2010-11 |
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| Horse chestnut extract contracts bovine vessels and affects human platelet aggregation through 5-HT(2A) receptors: an in vitro study. | 2010-09 |
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| Brain renin-angiotensin system modifies the blood pressure response to intracerebroventricular cadmium in rats. | 2010-07 |
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| Determinants of CREB degradation and KChIP2 gene transcription in cardiac memory. | 2010-07 |
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| Paraquat increases connective tissue growth factor and collagen expression via angiotensin signaling pathway in human lung fibroblasts. | 2010-04 |
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| Angiotensin II type 1 receptor blockade: high hopes sent back to reality? | 2009-12 |
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| Angiotensin II induces apoptosis in human mural granulosa-lutein cells, but not in cumulus cells. | 2009-05 |
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| Two dissimilar AT(1) agonists distinctively activate AT(1) receptors located on the luminal membrane of coronary endothelium. | 2009-02-28 |
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| Direct pro-arrhythmogenic effects of angiotensin II can be suppressed by AT1 receptor blockade in human atrial myocardium. | 2008-12 |
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| Evidence that the effect of angiotensin II on bovine oocyte nuclear maturation is mediated by prostaglandins E2 and F2alpha. | 2008-12 |
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| Receptor-dependent prorenin activation and induction of PAI-1 expression in vascular smooth muscle cells. | 2008-10 |
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| Angiotensin II and myosin light-chain phosphorylation contribute to the stretch-induced slow force response in human atrial myocardium. | 2008-09-01 |
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| Physiological effects of complexes of angiotensins with functionally different carrier proteins. | 2008-08 |
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| Angiotensin converting enzyme-2 is protective but downregulated in human and experimental lung fibrosis. | 2008-07 |
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| Peripheral mechanisms involved in the pressor and bradycardic effects of centrally administered arachidonic acid. | 2008-06 |
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| Angiotensin II- and glucose-stimulated extracellular matrix production: mediation by the insulin-like growth factor (IGF) axis in a murine mesangial cell line. | 2008-02 |
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| The secretory phospholipase A2 group IIA: a missing link between inflammation, activated renin-angiotensin system, and atherogenesis? | 2008 |
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| Importance and limits of ischemia in renal partial surgery: experimental and clinical research. | 2008 |
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| Cardiovascular effects of centrally injected melittin in hemorrhaged hypotensive rats: the investigation of peripheral mechanisms. | 2007-12 |
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| Stretch-induced alveolar type II cell apoptosis: role of endogenous bradykinin and PI3K-Akt signaling. | 2007-12 |
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| Effect of angiotensin II receptor blocker on glucose-induced mRNA expressions of matrix metalloproteinase-9 and tissue inhibitor of metalloproteinase-1 in rat mesangial cells. | 2007-11-05 |
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| The role of angiotensin II in the early stages of bovine ovulation. | 2007-11 |
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| Interaction between endothelin and angiotensin II in the up-regulation of vasopressin messenger RNA in the inner medullary collecting duct of the rat. | 2007-10 |
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| Role of the brain renin-angiotensin system in blood pressure regulation. | 2007-08 |
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| Role of the AT1A receptor in the CO2-induced stimulation of HCO3- reabsorption by renal proximal tubules. | 2007-07 |
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| Cardiovascular response to renin substrate microinjection into the central nucleus of the amygdala of rats. | 2007-05-07 |
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| Role of the vasodilator peptide angiotensin-(1-7) in cardiovascular drug therapy. | 2007 |
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| Angiotensin-TGF-beta 1 crosstalk in human idiopathic pulmonary fibrosis: autocrine mechanisms in myofibroblasts and macrophages. | 2007 |
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| Regulation of cGMP synthesis in cultured podocytes by vasoactive hormones. | 2006-12 |
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| Angiotensin-II is a putative neurotransmitter in lactate-induced panic-like responses in rats with disruption of GABAergic inhibition in the dorsomedial hypothalamus. | 2006-09-06 |
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| Analysis of the mechanisms underlying the vasorelaxant action of angiotensin II in the isolated rat carotid. | 2006-05-01 |
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| Direct regulation of insulin secretion by angiotensin II in human islets of Langerhans. | 2006-02 |
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| Nongenomic oestrogen signalling in oestrogen receptor negative breast cancer cells: a role for the angiotensin II receptor AT1. | 2006 |
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| Inhibition of angiotensin II- and endothelin-1-stimulated proliferation by selective MEK inhibitor in cultured rabbit gingival fibroblastsdagger. | 2005-12 |
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| Angiotensin II and III upregulate body fluid volume of the clam worm Perinereis sp. via angiotensin II receptors in different manners. | 2005-12 |
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| Memory strengthening by a real-life episode during reconsolidation: an outcome of water deprivation via brain angiotensin II. | 2005-10 |
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| Angiotensin II directly induces muscle protein catabolism through the ubiquitin-proteasome proteolytic pathway and may play a role in cancer cachexia. | 2005-08-22 |
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| Antiproliferative action of an angiotensin I-converting enzyme inhibitory peptide, Val-Tyr, via an L-type Ca2+ channel inhibition in cultured vascular smooth muscle cells. | 2005-06 |
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| A non-radioactive method for angiotensin II receptor binding studies using the rat liver. | 2005-05-03 |
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| Angiotensin II receptor inhibition prevents pneumocyte apoptosis in surfactant-depleted rat lungs. | 2005-04 |
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| Angiotensin II reverses the inhibitory action produced by theca cells on bovine oocyte nuclear maturation. | 2005-03-01 |
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| Angiotensin II inhibition of Ca2+ currents is independent of ATR1 angiotensin II receptor activation in rat adult vagal afferent neurons. | 2005-02-07 |
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| A new role for the renin-angiotensin system in the rat periaqueductal gray matter: angiotensin receptor-mediated modulation of nociception. | 2005 |
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| Endogenous angiotensin II in the regulation of hypoxic pulmonary vasoconstriction in anaesthetized dogs. | 2004-08 |
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| Intracoronary angiotensin II causes inotropic and vascular effects via different paracrine mechanisms. | 2004-07-08 |
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| Flow-dependent dilation mediated by endogenous kinins requires angiotensin AT2 receptors. | 2004-06-25 |
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| Pharmacological properties of angiotensin II receptors in cultured rabbit gingival fibroblasts. | 2004-03 |
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| Angiotensin II receptor blockade inhibits pneumocyte apoptosis in experimental meconium aspiration. | 2004-02 |
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| Stimulation of NHE3 in OKP cells by an autocrine mechanism. | 2004 |
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| Expression and localization of AT1 receptors in hepatic Kupffer cells: its potential role in regulating a fibrogenic response. | 2003-11-15 |
Sample Use Guides
In Vivo Use Guide
Sources: DOI 10.1007/978-1-4613-3822-2, J. Strauss, Acute Renal Disorders and Renal Emergencies (1984), p. 164, Retrieved from https://books.google.es/books?id=B_QGCAAAQBAJ&dq
The recommended dose is 0.05-15 ug/kg/min given as continous IV infusion by pump.
Route of Administration:
Intravenous
| Substance Class |
Protein
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| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
H2AFV2HE66
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| Record Status |
Validated (UNII)
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NCI_THESAURUS |
C270
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| Code System | Code | Type | Description | ||
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SARALASIN
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m9779
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100000084094
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34273-10-4
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H2AFV2HE66
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C66527
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SUB10447MIG
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DTXSID2046549
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DB06763
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CHEMBL938
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D012504
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3484
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9556
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3542
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| Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
Bingding Assay
IC50
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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 |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_1] | GLYCINE | SARCOSINE | Z711V88R5F |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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