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 II type 1 receptor blockers. | 2001 Feb 13 |
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| Angiotensin II increases neurogenic nitric oxide metabolism in mesenteric arteries from hypertensive rats. | 2001 Jan 26 |
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| Activation of the subfornical organ enhances extracellular noradrenaline concentrations in the hypothalamic paraventricular nucleus in the rat. | 2001 Mar 1 |
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| [The cellular mechanism of angiotensin II inhibition on BKCa of ECV304 cell and the protective effect of gingko leaf extract]. | 2001 Oct |
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| Contractile effects of angiotensin peptides in rat aorta are differentially dependent on tyrosine kinase activity. | 2001 Sep |
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| Influence of ANG II on cytoplasmic sodium in cultured rabbit nonpigmented ciliary epithelium. | 2002 Aug |
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| Decreased monoamine release in the median preoptic area following ventricular treatment with the angiotensin II antagonist saralasin in normotensive and spontaneously hypertensive rats. | 2002 Jul 15 |
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| Involvement of the AT(2)-receptor in angiotensin II-induced facilitation of sympathetic neurotransmission. | 2002 Sep |
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| The effects of peptide and nonpeptide antagonists of angiotensin II receptors on the noradrenaline uptake of different brain structures in rats with angiotensin II-induced increase of water intake. | 2003 |
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| Influence of angiotensin II receptor subtypes of the paraventricular nucleus on the physiological responses induced by angiotensin II injection into the medial septal area. | 2003 Apr |
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| Microinjection of renin-angiotensin system peptides in discrete sites within the rat periaqueductal gray matter elicits antinociception. | 2003 May 16 |
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| Expression and localization of AT1 receptors in hepatic Kupffer cells: its potential role in regulating a fibrogenic response. | 2003 Nov 15 |
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| Stimulation of NHE3 in OKP cells by an autocrine mechanism. | 2004 |
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| Angiotensin II receptor blockade inhibits pneumocyte apoptosis in experimental meconium aspiration. | 2004 Feb |
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| Flow-dependent dilation mediated by endogenous kinins requires angiotensin AT2 receptors. | 2004 Jun 25 |
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| Intracoronary angiotensin II causes inotropic and vascular effects via different paracrine mechanisms. | 2004 May-Jun |
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| Angiotensin II receptor inhibition prevents pneumocyte apoptosis in surfactant-depleted rat lungs. | 2005 Apr |
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| Inhibition of angiotensin II- and endothelin-1-stimulated proliferation by selective MEK inhibitor in cultured rabbit gingival fibroblastsdagger. | 2005 Dec |
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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 Feb 7 |
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| Regulation of cGMP synthesis in cultured podocytes by vasoactive hormones. | 2006 Dec |
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| Cardiovascular effects of centrally injected melittin in hemorrhaged hypotensive rats: the investigation of peripheral mechanisms. | 2007 Dec |
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| Role of the AT1A receptor in the CO2-induced stimulation of HCO3- reabsorption by renal proximal tubules. | 2007 Jul |
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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 Nov 5 |
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| Direct pro-arrhythmogenic effects of angiotensin II can be suppressed by AT1 receptor blockade in human atrial myocardium. | 2008 Dec |
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| Angiotensin II and myosin light-chain phosphorylation contribute to the stretch-induced slow force response in human atrial myocardium. | 2008 Sep 1 |
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| Angiotensin II type 1 receptor blockade: high hopes sent back to reality? | 2009 Dec |
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| Angiotensin II induces apoptosis in human mural granulosa-lutein cells, but not in cumulus cells. | 2009 May |
|
| Horse chestnut extract contracts bovine vessels and affects human platelet aggregation through 5-HT(2A) receptors: an in vitro study. | 2010 Sep |
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
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C270
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ACTIVE MOIETY
SUBSTANCE RECORD