関: saralasin acetate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/29 15:09:02」(JST)

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Saralasin is a partial agonist of angiotensin II receptors, though it is commonly mistaken as a competitive antagonist. Saralasin's distinction as a partial agonist is based on the fact that its therapeutic effect (i.e. reduced hypertension) is only observed in patients with high plasma angiotensin II levels, but in patients with low angiotensin II levels Saralasin causes hypertension. In other words, the effects of Saralasin on the angiotensin II receptor in the absence of angiotensin II is pharmacodynamically similar to angiotensin II itself thus it is a partial agonist, because if it was an antagonist it would not elicit an effect when bound to its receptor. Saralasin is an angiotensin II analogue, containing sarcosine-1 and alanine-8, hence the name (sarcosine, alanine, angiotensin).

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Saralasin at the US National Library of Medicine Medical Subject Headings (MeSH)
Olsson M, Annerbrink K, Hedner J, Eriksson E (2004). "Intracerebroventricular administration of the angiotensin II receptor antagonist saralasin reduces respiratory rate and tidal volume variability in freely moving Wistar rats.". Psychoneuroendocrinology 29 (1): 107–12. doi:10.1016/S0306-4530(02)00147-6. PMID 14575733.
Ip S, Tsang S, Wong T, Che C, Leung P (2003). "Saralasin, a nonspecific angiotensin II receptor antagonist, attenuates oxidative stress and tissue injury in cerulein-induced acute pancreatitis.". Pancreas 26 (3): 224–9. doi:10.1097/00006676-200304000-00003. PMID 12657946.
Tsang S, Ip S, Wong T, Che C, Leung P (2003). "Differential effects of saralasin and ramiprilat, the inhibitors of renin-angiotensin system, on cerulein-induced acute pancreatitis.". Regul Pept 111 (1–3): 47–53. doi:10.1016/S0167-0115(02)00226-4. PMID 12609748.

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English Journal

Bovine ovarian cells have (pro)renin receptors and prorenin induces resumption of meiosis in vitro.

Dau AM1, da Silva EP1, da Rosa PR1, Bastiani FT1, Gutierrez K1, Ilha GF1, Comim FV2, Gonçalves PB3.
Peptides.Peptides.2016 Jul;81:1-8. doi: 10.1016/j.peptides.2016.03.010. Epub 2016 Apr 6.
The discovery of a receptor that binds prorenin and renin in human endothelial and mesangial cells highlights the possible effect of renin-independent prorenin in the resumption of meiosis in oocytes that was postulated in the 1980s.This study aimed to identify the (pro)renin receptor in the ovary a
PMID 27060674

In vitro method of studying the angiotensin activity of chemical compounds.

Spasov AA1, Yakovlev DS, Bukatina TM, Brigadirova AA.
Bulletin of experimental biology and medicine.Bull Exp Biol Med.2014 Nov;158(1):115-7. doi: 10.1007/s10517-014-2705-8. Epub 2014 Nov 19.
We developed and tested an experimental model to study in vitro the type 1 angiotensin antagonistic activity of compounds on the isolated portal vein of rats. The reliability of this method was confirmed in tests with saralasin (nonselective antagonist of angiotensin receptors) and losartan (selecti
PMID 25403411

Saralasin and Sarile Are AT2 Receptor Agonists.

Guimond MO1, Hallberg M2, Gallo-Payet N1, Wallinder C3.
ACS medicinal chemistry letters.ACS Med Chem Lett.2014 Aug 18;5(10):1129-32. doi: 10.1021/ml500278g. eCollection 2014.
Saralasin and sarile, extensively studied over the past 40 years as angiotensin II (Ang II) receptor blockers, induce neurite outgrowth in a NG108-15 cell assay to a similar extent as the endogenous Ang II. In their undifferentiated state, these cells express mainly the AT2 receptor. The neurite out
PMID 25313325

Japanese Journal

Saralasin, a Nonspecific Angiotensin II Receptor Antagonist, Attenuates Oxidative Stress and Tissue Injury in Cerulein-Induced Acute Pancreatitis

IP Siu Po,TSANG Siu Wai,WONG Tung Po,CHE Chun Tao,LEUNG Po Sing
Pancreas 26(3), 224-229, 2003-04-01
NAID 10016164414

Evidence for the AT_1 Subtype of the Angiotensin II Receptor in the Rat Submandibular Gland

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Biological & pharmaceutical bulletin 23(10), 1185-1188, 2000-10-01
… Ang II, Ang III and saralasin completely displaced the [^3H]Ang II binding, whereas CV-11974,an AT_1 receptor antagonist and PD123319,an AT_2 receptor antagonist maximally displaced up to approximately 87 and 13% of the total binding, respectively. …
NAID 110003639851

Stretch-Induced Proliferation of Cultured Vascular Smooth Muscle Cells and a Possible Involvement of Local Renin-Angiotensin System and Platelet-Derived Growth Factor (PDGF)

LI Qing,MURAGAKI Yasuteru,UENO Hikaru,OOSHIMA Akira
Hypertension research : clinical and experimental : official journal of the Japanese Society of Hypertension 20(3), 217-223, 1997-09-01
NAID 10009562195

「サララシン」

Saralasin
Names
	IUPAC name (2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid
	Other names Sar-Arg-Val-Tyr-Val-His-Pro-Ala
Identifiers
CAS Registry Number	34273-10-4
ChEMBL	ChEMBL938 ; ChEMBL1200670
Jmol-3D images	Image
PubChem	6324663
	SMILES C[C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC2=CN=CN2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC3=CC=C(C=C3)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC ;
UNII	H2AFV2HE66
Properties
Chemical formula	C42H65N13O10
Molar mass	912.05 g/mol
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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	Infobox references