Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C42H65N13O10.C2H4O2 |
| Molecular Weight | 972.0986 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 7 / 7 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)=O.CNCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N3CCC[C@H]3C(=O)N[C@@H](C)C(O)=O
InChI
InChIKey=JFPFCTNAFOZCDA-LYHTUURTSA-N
InChI=1S/C42H65N13O10.C2H4O2/c1-22(2)33(53-35(58)28(50-32(57)20-45-6)9-7-15-47-42(43)44)38(61)51-29(17-25-11-13-27(56)14-12-25)36(59)54-34(23(3)4)39(62)52-30(18-26-19-46-21-48-26)40(63)55-16-8-10-31(55)37(60)49-24(5)41(64)65;1-2(3)4/h11-14,19,21-24,28-31,33-34,45,56H,7-10,15-18,20H2,1-6H3,(H,46,48)(H,49,60)(H,50,57)(H,51,61)(H,52,62)(H,53,58)(H,54,59)(H,64,65)(H4,43,44,47);1H3,(H,3,4)/t24-,28-,29-,30-,31-,33-,34-;/m0./s1
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 |
|---|---|---|
| Role of angiotensin and its inhibition in hypertension, ischemic heart disease, and heart failure. | 2001 Feb |
|
| Angiotensin II type 1 receptor blockers. | 2001 Feb 13 |
|
| Contribution of angiotensin II, endothelin 1 and the endothelium to the slow inotropic response to stretch in ferret papillary muscle. | 2001 Jan |
|
| Angiotensin II priming of aldosterone secretion with agents that enhance Ca(2+) influx. | 2001 May 25 |
|
| Renal nuclear angiotensin II receptors in normal and hypertensive rats. | 2002 |
|
| Nonpeptide antagonists of AT1 receptor for angiotensin II delay the onset of acute respiratory distress syndrome. | 2002 Oct |
|
| Involvement of the AT(2)-receptor in angiotensin II-induced facilitation of sympathetic neurotransmission. | 2002 Sep |
|
| 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 |
|
| Reduced dipsogenic response induced by angiotensin II activation of subfornical organ projections to the median preoptic nucleus in estrogen-treated rats. | 2003 Jan |
|
| Microinjection of renin-angiotensin system peptides in discrete sites within the rat periaqueductal gray matter elicits antinociception. | 2003 May 16 |
|
| Endogenous angiotensin II in the regulation of hypoxic pulmonary vasoconstriction in anaesthetized dogs. | 2004 Aug |
|
| Intracoronary angiotensin II causes inotropic and vascular effects via different paracrine mechanisms. | 2004 May-Jun |
|
| A new role for the renin-angiotensin system in the rat periaqueductal gray matter: angiotensin receptor-mediated modulation of nociception. | 2005 |
|
| Angiotensin II receptor inhibition prevents pneumocyte apoptosis in surfactant-depleted rat lungs. | 2005 Apr |
|
| Angiotensin II directly induces muscle protein catabolism through the ubiquitin-proteasome proteolytic pathway and may play a role in cancer cachexia. | 2005 Aug 22 |
|
| Inhibition of angiotensin II- and endothelin-1-stimulated proliferation by selective MEK inhibitor in cultured rabbit gingival fibroblastsdagger. | 2005 Dec |
|
| Angiotensin II and III upregulate body fluid volume of the clam worm Perinereis sp. via angiotensin II receptors in different manners. | 2005 Dec |
|
| Angiotensin II inhibition of Ca2+ currents is independent of ATR1 angiotensin II receptor activation in rat adult vagal afferent neurons. | 2005 Feb 7 |
|
| 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 |
|
| Angiotensin II reverses the inhibitory action produced by theca cells on bovine oocyte nuclear maturation. | 2005 Mar 1 |
|
| Memory strengthening by a real-life episode during reconsolidation: an outcome of water deprivation via brain angiotensin II. | 2005 Oct |
|
| Direct regulation of insulin secretion by angiotensin II in human islets of Langerhans. | 2006 Feb |
|
| Analysis of the mechanisms underlying the vasorelaxant action of angiotensin II in the isolated rat carotid. | 2006 May 1 |
|
| A non-radioactive method for angiotensin II receptor binding studies using the rat liver. | 2006 May-Jun |
|
| Cardiovascular effects of centrally injected melittin in hemorrhaged hypotensive rats: the investigation of peripheral mechanisms. | 2007 Dec |
|
| 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 |
|
| Angiotensin II type 1 receptor blockade: high hopes sent back to reality? | 2009 Dec |
|
| Angiotensin II induces apoptosis in human mural granulosa-lutein cells, but not in cumulus cells. | 2009 May |
|
| Determinants of CREB degradation and KChIP2 gene transcription in cardiac memory. | 2010 Jul |
|
| Angiotensin modulates long-term memory expression but not long-term memory storage in the crab Chasmagnathus. | 2010 Nov |
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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16051934
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54194-01-3
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SUBSTANCE RECORD
