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Chemical Compound Review:

AC1MHZMV 4-[6-oxo-3-(8-phenyl-1,9...

Synonyms: CHEMBL292917, FK-838, AG-D-63304, SureCN2641189, ACMC-20mtz5, ...

Uehara, Y. et al., Bak, M. et al., Akahane, A. et al.

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Disease relevance of FK-838

FK-838 attenuated the development of hypertension in Dahl S rats, and caused a decrease in aortic weight in a dose dependent fashion [1].

High impact information on FK-838

Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity [2].
CONCLUSION: It is concluded that in conscious unstressed rats, acute adenosine A(1) receptor inhibition by FK 838 led to a significant natriuresis that was caused by inhibition of proximal tubular Na(+) reabsorption, possibly with a contribution from inhibition of distal nephron Na(+) reabsorption [3].
We investigated the effects of the adenosine type-1 receptor antagonist FK-838 on salt-induced hypertension in Dahl-Sea salt-sensitive (Dahl S) rats [1].
The blood pressure reduction by FK-838 was associated with attenuation of glomerular and arterial injury in the kidney [1].
The renal protective effect of FK-838 treatment was associated with a reduction of plasma renin activity and plasma aldosterone concentration [1].

Gene context of FK-838

Effects of the adenosine A1 receptor inhibitor FK 838 on proximal tubular fluid output in rats [3].

References

A new adenosine subtype-1 receptor antagonist, FK-838, attenuates salt-induced hypertension in Dahl salt-sensitive rats. Uehara, Y., Numabe, A., Hirawa, N., Kawabata, Y., Nagoshi, H., Kaneko, H., Gomi, T., Goto, A., Toyo-oka, T., Omata, M. Am. J. Hypertens. (1995) [Pubmed]
Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity. Akahane, A., Katayama, H., Mitsunaga, T., Kato, T., Kinoshita, T., Kita, Y., Kusunoki, T., Terai, T., Yoshida, K., Shiokawa, Y. J. Med. Chem. (1999) [Pubmed]
Effects of the adenosine A1 receptor inhibitor FK 838 on proximal tubular fluid output in rats. Bak, M., Thomsen, K. Nephrol. Dial. Transplant. (2004) [Pubmed]

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