SKF 100398

Names

[ Name ]:
SKF 100398

[Synonym ]:
M.W. 1136.41 C53H77N13O11S2
type 1 arginine vasopressin antagonist
(d(CH2)51,Tyr(Et)2,Val4,Arg8)-Vasopressin

Biological Activity

[Description]:

SKF 100398 (d(CH2)5Tyr(Et)VAVP) is an arginine vasopressin (AVP) analogue, and acts as a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor

Research Areas >> Metabolic Disease

[In Vivo]

SKF 100398 is a specific antagonist of the hydrosmotic effect of exogenous and endogenous AVP[1]. SKF 100398 (8 μg/kg; i.v.) abolishes the antidiuretic effect of AVP[1]. Animal Model: Male Sprague-Dawley rats (250-300 g)[1] Dosage: 8 μg/kg Administration: Intravenous injection Result: Completely blocked the antidiuretic effect of exogenous AVP (4 ng/kg body wt i.v.).

[References]

[1]. S Ishikawa, et al. Further in vivo evidence for antagonist-to-antidiuretic action of arginine vasopressin. Am J Physiol. 1983 Nov;245(5 Pt 1):R713-9.

Chemical & Physical Properties

[ Density]:
1.44g/cm3

[ Molecular Formula ]:
C₅₃H₇₇N₁₃O₁₁S₂

[ Molecular Weight ]:
1136.39000

[ Exact Mass ]:
1135.53000

[ PSA ]:
431.92000

[ LogP ]:
4.60970

[ Index of Refraction ]:
1.676

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H332

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn: Harmful;

[ Risk Phrases ]:
20

[ Safety Phrases ]:
36

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Articles

Vasopressin increases water permeability of kidney collecting duct by inducing translocation of aquaporin-CD water channels to plasma membrane.

Proc. Natl. Acad. Sci. U. S. A. 92(4) , 1013-7, (1995)

Water excretion by the kidney is regulated by the peptide hormone vasopressin. Vasopressin increases the water permeability of the renal collecting duct cells, allowing more water to be reabsorbed fro...

Arginine vasopressin enhances pHi regulation in the presence of HCO3- by stimulating three acid-base transport systems.

Nature 337(6208) , 648-51, (1989)

Growth factors raise intracellular pH (pHi) by stimulating Na+/H+ exchange in the absence of HCO3-. In mutant cells that lack the Na+/H+ exchange activity, this alkalinization does not occur, and the ...

Pharmacological characterization of V1a vasopressin receptors in the rat cortical collecting duct.

Am. J. Physiol. 262 , F546-F553, (1992)

Vasopressin receptors in distal segments of the rat nephron were identified in isolated tubules using two labeled ligands: the [1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid), 2-(O-meth...