지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
커뮤니티
연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
초록· 키워드
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KR-31064 was developed for the strong angiotensin II receptor antagonist among the one of pyridyl imidazol series compounds. To investigate the receptor-ligand binding characteristics of this nonpeptide antagonist, binding experiments were deployed in various conditions and ex vivo contractile responses were tested toward the standard compound, losartan. Receptor binding experiments with radiolabeled angiotensin II, the $IC_{50}$ value for KR-31064 resulted 0.67 nM without any activities toward type 2 angiotensin II receptor. The comparative potency against losartan was more than 18 fold and the specific activity in type 1 angiotensin II receptor was more than 10,000 fold comparing to the type 2 receptor. Scatchard analysis of saturation binding data showed KR-31064 acted on the receptor in a competitive mode. KR-31064 inhibited the contractile response derived by angiotensin II ($pK_B$: 9.86) similar to that of losartan with decreased maximum signals. As a potent and specific type 1 angiotensin II receptor antagonist, KR-31064 may have possibilities for the development of diagnostic ligands that can be used as tools for various biochemical research experiments and non-invasive diagnostics.
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참고문헌 (23)
참고문헌 신청
Timmermans, P. B. / 1993 / Angiotensin II receptors and angiotensin II receptor antagonists / Pharmacol. Rev 45:205
Sever, P. S. / 2009 / Managing cardiovascular and renal risk: the potential of direct renin inhibition / J. Renin Angiotensin Aldosterone Syst 10:65
Williams, G. H. / 1988 / Converting-enzyme inhibitors in the treatment of hypertension / N. Engl. J. Med 319:1517
Coulter, D. M. / 1987 / Cough associated with captopril and enalapril / Br. Med. J. (Clin. Res. Ed.) 294(1521)
Roberts, J. R. / 1991 / Clinical characteristics of angiotensin-converting enzyme inhibitor-induced angioedema / Ann. Emerg. Med 20:555
Sever, P. S. / 2009 / Managing cardiovascular and renal risk: the potential of direct renin inhibition / J. Renin Angiotensin Aldosterone Syst 10:65
Williams, G. H. / 1988 / Converting-enzyme inhibitors in the treatment of hypertension / N. Engl. J. Med 319:1517
Coulter, D. M. / 1987 / Cough associated with captopril and enalapril / Br. Med. J. (Clin. Res. Ed.) 294(1521)
Roberts, J. R. / 1991 / Clinical characteristics of angiotensin-converting enzyme inhibitor-induced angioedema / Ann. Emerg. Med 20:555
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