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Chemical Compound Review

AG-K-19261     (2S)-2-[[(2S)-4- (carboxymethyl)-5-oxo-2...

Synonyms: RS-5139, KST-1A0556, AC1Q5QTP, CTK4A6820, AR-1A3204, ...
 
 
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Disease relevance of RS-5139

 

High impact information on RS-5139

 

Chemical compound and disease context of RS-5139

 

Biological context of RS-5139

 

Anatomical context of RS-5139

 

Associations of RS-5139 with other chemical compounds

  • Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR) [5].
  • CONCLUSIONS: These results indicate that impaired renal function has only a limited effect on the pharmacokinetics of temocapril and its active metabolite, temocaprilat [12].
  • Twenty-one hearts were divided into three experimental groups consisting of 7 hearts each: a Tem+CV group perfused with a combination of temocaprilat and CV-11974; a Tem+CV+L-NAME group perfused with a combination of temocaprilat and CV-11974 plus L-NAME, and a control group [7].
  • The dose-dependent inhibition of the up-take of [3H]-estradiol-17beta-D-glucuronide and [3H]-2,4-dinitrophenyl-S-glutathione, which are good substrates for cMOAT, in canalicular membrane vesicles (CMVs) prepared from Sprague-Dawley rats was determined in the presence of trandolaprilat and temocaprilat [13].
 

Gene context of RS-5139

  • The Mrp2 protein expression in dog liver was only 10% of that in rat liver and was comparable with the reported difference in the biliary excretion clearance of temocaprilat as Mrp2 substrate [14].
  • The N-succinimmidyl ester of RS-5139 was coupled with bovine serum albumin (BSA) and its conjugate was used as an immunogen [15].
  • The effect of angiotensin converting enzyme (ACE) inhibitor, temocaprilat and/or angiotensin II type 1 (AT1) receptor antagonist, CV-11974 on myocardial metabolism and contraction during ischemia and reperfusion was examined by phosphorus 31-nuclear magnetic resonance (31P-NMR) in Langendorff rabbit hearts [16].
 

Analytical, diagnostic and therapeutic context of RS-5139

References

  1. Angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers synergistically increase coronary blood flow in canine ischemic myocardium: role of bradykinin. Kitakaze, M., Asanuma, H., Funaya, H., Node, K., Takashima, S., Sanada, S., Asakura, M., Ogita, H., Kim, J., Hori, M. J. Am. Coll. Cardiol. (2002) [Pubmed]
  2. An AT1-receptor antagonist and an angiotensin-converting enzyme inhibitor protect against hypoxia-induced apoptosis in human aortic endothelial cells through upregulation of endothelial cell nitric oxide synthase activity. Matsumoto, N., Manabe, H., Ochiai, J., Fujita, N., Takagi, T., Uemura, M., Naito, Y., Yoshida, N., Oka, S., Yoshikawa, T. Shock (2003) [Pubmed]
  3. Effects of an HMG-CoA reductase inhibitor in combination with an ACE inhibitor or angiotensin II type 1 receptor antagonist on myocardial metabolism in ischemic rabbit hearts. Kawabata, H., Nakagawa, K., Ishikawa, K. Hypertens. Res. (2002) [Pubmed]
  4. Transport of temocaprilat into rat hepatocytes: role of organic anion transporting polypeptide. Ishizuka, H., Konno, K., Naganuma, H., Nishimura, K., Kouzuki, H., Suzuki, H., Stieger, B., Meier, P.J., Sugiyama, Y. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  5. Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR). Ishizuka, H., Konno, K., Naganuma, H., Sasahara, K., Kawahara, Y., Niinuma, K., Suzuki, H., Sugiyama, Y. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  6. Identification of esterases expressed in Caco-2 cells and effects of their hydrolyzing activity in predicting human intestinal absorption. Imai, T., Imoto, M., Sakamoto, H., Hashimoto, M. Drug Metab. Dispos. (2005) [Pubmed]
  7. Cardioprotection with angiotensin converting enzyme inhibitor and angiotensin II type 1 receptor antagonist is not abolished by nitric oxide synthase inhibitor in ischemia-reperfused rabbit hearts. Kawabata, H., Ryomoto, T., Ishikawa, K. Hypertens. Res. (2001) [Pubmed]
  8. Effect of an endothelin receptor antagonist and an angiotensin converting enzyme inhibitor on metabolism and contraction in the ischemic and reperfused rabbit heart. Kawabata, H., Ryomoto, T., Ishikawa, K. Jpn. Circ. J. (1999) [Pubmed]
  9. Single dose and steady state pharmacokinetics of temocapril and temocaprilat in young and elderly hypertensive patients. Püchler, K., Sierakowski, B., Roots, I. British journal of clinical pharmacology. (1998) [Pubmed]
  10. Converting enzyme inhibitor temocaprilat prevents high glucose-mediated suppression of human aortic endothelial cell proliferation. Yasunari, K., Maeda, K., Watanabe, T., Nakamura, M., Asada, A., Yoshikawa, J. J. Cardiovasc. Pharmacol. (2003) [Pubmed]
  11. ACE inhibitor improves insulin resistance in diabetic mouse via bradykinin and NO. Shiuchi, T., Cui, T.X., Wu, L., Nakagami, H., Takeda-Matsubara, Y., Iwai, M., Horiuchi, M. Hypertension (2002) [Pubmed]
  12. Pharmacokinetics of temocapril and temocaprilat after 14 once daily oral doses of temocapril in hypertensive patients with varying degrees of renal impairment. Püchler, K., Eckl, K.M., Fritsche, L., Renneisen, K., Neumayer, H.H., Sierakowski, B., Lavrijssen, A.T., Thomsen, T., Roots, I. British journal of clinical pharmacology. (1997) [Pubmed]
  13. Trandolaprilat, an angiotensin-converting enzyme inhibitor, is not excreted in bile via an ATP-dependent active transporter (cMOAT). Shionoiri, H., Takasaki, I., Minamisawa, K., Ishizuka, H., Konno, K., Naganuma, H., Sasahara, K., Kawahara, Y. Hypertens. Res. (2001) [Pubmed]
  14. Functional analysis of dog multidrug resistance-associated protein 2 (Mrp2) in comparison with rat Mrp2. Ninomiya, M., Ito, K., Horie, T. Drug Metab. Dispos. (2005) [Pubmed]
  15. Enzyme immunoassay of the active metabolite (RS-5139) of angiotensin converting enzyme inhibitor (CS-622). Shioya, H., Shimojo, M., Kawahara, Y. Journal of immunoassay. (1991) [Pubmed]
  16. Effect of angiotensin converting enzyme inhibitor and angiotensin II type 1 receptor antagonist on metabolism and contraction in ischemia-reperfused rabbit heart. Kawabata, H., Ryomoto, T., Ishikawa, K. Jpn. Circ. J. (2000) [Pubmed]
 
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