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
| Molecular Formula | C42H65N13O10 |
| Molecular Weight | 912.0466 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 7 / 7 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | C2H4O2 |
| Molecular Weight | 60.052 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 receptor in the heart of Bothrops jararaca snake. | 2001 Apr 6 |
|
| 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 |
|
| Angiotensinergic and noradrenergic mechanisms in the hypothalamic paraventricular nucleus participate in the drinking response induced by activation of the subfornical organ in rats. | 2001 Jan 29 |
|
| Dipsogenic response induced by angiotensinergic pathways from the lateral hypothalamic area to the subfornical organ in rats. | 2001 Jan 29 |
|
| 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 |
|
| Angiotensin II elicits water seeking behavior and the water absorption response in the toad Bufo bufo. | 2001 May |
|
| Angiotensin II priming of aldosterone secretion with agents that enhance Ca(2+) influx. | 2001 May 25 |
|
| Effects of central angiotensin II receptor antagonism on fetal swallowing and cardiovascular activity. | 2001 Oct |
|
| Cardiorespiratory effects of prolonged angiotensin II block in resting conscious dogs. | 2001 Sep |
|
| Respiratory and metabolic effects of decreased osmolality in conscious rats. | 2001 Sep |
|
| Renal nuclear angiotensin II receptors in normal and hypertensive rats. | 2002 |
|
| Attenuated drinking response induced by angiotensinergic activation of subfornical organ projections to the paraventricular nucleus in estrogen-treated rats. | 2002 May 24 |
|
| Angiotensin AT(1)-receptors depolarize neonatal spinal motoneurons and other ventral horn neurons via two different conductances. | 2002 Nov |
|
| 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 |
|
| Alpha-adrenergic control of ANG II-induced drinking in the rat median preoptic nucleus. | 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 |
|
| Antihyperglycemic action of angiotensin II receptor antagonist, valsartan, in streptozotocin-induced diabetic rats. | 2003 Apr |
|
| Bleomycin-induced apoptosis of alveolar epithelial cells requires angiotensin synthesis de novo. | 2003 Mar |
|
| Microinjection of renin-angiotensin system peptides in discrete sites within the rat periaqueductal gray matter elicits antinociception. | 2003 May 16 |
|
| Stimulation of NHE3 in OKP cells by an autocrine mechanism. | 2004 |
|
| 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 |
|
| 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 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 |
|
| 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 |
|
| Angiotensin-TGF-beta 1 crosstalk in human idiopathic pulmonary fibrosis: autocrine mechanisms in myofibroblasts and macrophages. | 2007 |
|
| Role of the brain renin-angiotensin system in blood pressure regulation. | 2007 Aug |
|
| 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 |
|
| The secretory phospholipase A2 group IIA: a missing link between inflammation, activated renin-angiotensin system, and atherogenesis? | 2008 |
|
| 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 and myosin light-chain phosphorylation contribute to the stretch-induced slow force response in human atrial myocardium. | 2008 Sep 1 |
|
| 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 |
|
| Brain renin-angiotensin system modifies the blood pressure response to intracerebroventricular cadmium in rats. | 2010 Jul |
|
| 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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:22:35 GMT 2023
by
admin
on
Fri Dec 15 16:22:35 GMT 2023
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| Record UNII |
U603K01682
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| Record Status |
Validated (UNII)
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| Record Version |
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U603K01682
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16051934
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54194-01-3
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| Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS |
