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 |
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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 |
|---|---|---|
| Estrogen attenuates the drinking response induced by activation of angiotensinergic pathways from the lateral hypothalamic area to the subfornical organ in female rats. | 2001 Jul |
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| Angiotensin regulates endothelin-B receptor in rat inner medullary collecting duct. | 2001 Jun |
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| Angiotensin II elicits water seeking behavior and the water absorption response in the toad Bufo bufo. | 2001 May |
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| Inhibition of the formation or action of angiotensin II reverses attenuated K+ currents in type 1 and type 2 diabetes. | 2001 Nov 15 |
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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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| Inhibitory effect of the angiotensin converting enzyme inhibitors captopril and enalapril on the conversion of procollagen to collagen. | 2001 Oct |
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| Estrogen decreases the responsiveness of subfornical organ neurons to angiotensinergic neural inputs from the lateral hypothalamic area in the female rat. | 2001 Oct |
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| Differentiation in the angiotensin II receptor 1 blocker class on autonomic function. | 2001 Sep |
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| Norepinephrine induces alveolar epithelial apoptosis mediated by alpha-, beta-, and angiotensin receptor activation. | 2001 Sep |
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| Effect of angiotensin II on ANP-dependent guanylyl cyclase activity in cultured mouse and rat podocytes. | 2002 |
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| Influence of ANG II on cytoplasmic sodium in cultured rabbit nonpigmented ciliary epithelium. | 2002 Aug |
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| Angiotensin AT(1)-receptors depolarize neonatal spinal motoneurons and other ventral horn neurons via two different conductances. | 2002 Nov |
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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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| Saralasin, a nonspecific angiotensin II receptor antagonist, attenuates oxidative stress and tissue injury in cerulein-induced acute pancreatitis. | 2003 Apr |
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| Role of PKC in autocrine regulation of rat ventricular K+ currents by angiotensin and endothelin. | 2003 Apr |
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| Bleomycin-induced apoptosis of alveolar epithelial cells requires angiotensin synthesis de novo. | 2003 Mar |
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| Differential effects of saralasin and ramiprilat, the inhibitors of renin-angiotensin system, on cerulein-induced acute pancreatitis. | 2003 Mar 28 |
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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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| Cardiac memory is associated with decreased levels of the transcriptional factor CREB modulated by angiotensin II and calcium. | 2003 Sep 5 |
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| Stimulation of NHE3 in OKP cells by an autocrine mechanism. | 2004 |
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| Endogenous angiotensin II in the regulation of hypoxic pulmonary vasoconstriction in anaesthetized dogs. | 2004 Aug |
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| Angiotensin II receptor blockade inhibits pneumocyte apoptosis in experimental meconium aspiration. | 2004 Feb |
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| Intracerebroventricular administration of the angiotensin II receptor antagonist saralasin reduces respiratory rate and tidal volume variability in freely moving Wistar rats. | 2004 Jan |
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| Flow-dependent dilation mediated by endogenous kinins requires angiotensin AT2 receptors. | 2004 Jun 25 |
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| Pharmacological properties of angiotensin II receptors in cultured rabbit gingival fibroblasts. | 2004 Mar |
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| Intracoronary angiotensin II causes inotropic and vascular effects via different paracrine mechanisms. | 2004 May-Jun |
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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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| Angiotensin II receptor inhibition prevents pneumocyte apoptosis in surfactant-depleted rat lungs. | 2005 Apr |
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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 Aug 22 |
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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 and III upregulate body fluid volume of the clam worm Perinereis sp. via angiotensin II receptors in different manners. | 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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| 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 Jun |
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| Angiotensin II reverses the inhibitory action produced by theca cells on bovine oocyte nuclear maturation. | 2005 Mar 1 |
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| Memory strengthening by a real-life episode during reconsolidation: an outcome of water deprivation via brain angiotensin II. | 2005 Oct |
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| Role of the vasodilator peptide angiotensin-(1-7) in cardiovascular drug therapy. | 2007 |
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| Role of the brain renin-angiotensin system in blood pressure regulation. | 2007 Aug |
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| Stretch-induced alveolar type II cell apoptosis: role of endogenous bradykinin and PI3K-Akt signaling. | 2007 Dec |
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| The role of angiotensin II in the early stages of bovine ovulation. | 2007 Nov |
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| Evidence that the effect of angiotensin II on bovine oocyte nuclear maturation is mediated by prostaglandins E2 and F2alpha. | 2008 Dec |
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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 Feb |
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| Peripheral mechanisms involved in the pressor and bradycardic effects of centrally administered arachidonic acid. | 2008 Jun |
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| Receptor-dependent prorenin activation and induction of PAI-1 expression in vascular smooth muscle cells. | 2008 Oct |
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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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| Two dissimilar AT(1) agonists distinctively activate AT(1) receptors located on the luminal membrane of coronary endothelium. | 2009 Nov-Dec |
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| Paraquat increases connective tissue growth factor and collagen expression via angiotensin signaling pathway in human lung fibroblasts. | 2010 Apr |
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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| Sequence Type | COMPLETE |
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FO21Z580M4
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Validated (UNII)
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NCI_THESAURUS |
C270
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DTXSID701027501
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FO21Z580M4
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7830
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C66528
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CHEMBL938
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DBSALT001433
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11954381
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m9779
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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