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Prostaglandin biosynthesis in rabbit kidney medulla: Inhibition in-vitro vs. in-vivo by aspirin, indomethacin and meclofenamic acid
Year:
1978
Source of publication :
Prostaglandins
Authors :
Gafni, Yedidya
;
.
Volume :
15
Co-Authors:
Gafni, Y., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Schwartzman, M., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Raz, A., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Facilitators :
From page:
759
To page:
772
(
Total pages:
14
)
Abstract:
The non-steroidal anti-inflammatory drugs aspirin, indomethacin and meclofenamic acid were compared for their potency and duration of inhibition of prostaglandin biosynthesis in rabbit kidney medulla. Indomethacin and meclofenamic acid showed equal potency of inhibition in-vitro (IC50 0.88 μM and 0.85 μM respectively) while aspirin was a much weaker inhibitor (IC50 120 μM). In-vivo, indomethacin was the most powerful inhibitor (ID50 0.034 mg/kg) followed by meclofenamic acid (0.45 mg/kg) and aspirin (2.35 mg/kg). Studies on the duration of in-vivo inhibition by these compounds showed the effect of indomethacin and meclofenamic acid to be completely reversed within 4-6 hours. In contrast, return of kidney prostaglandin biosynthetic activity following aspirin inhibition is very slow and significant inhibition is still present 48 hours after a single aspirin injection. The inhibitory effect of aspirin in-vivo could be blocked by pretreatment with indomethacin, indicating that both drugs interact with related sites on the cyclo-oxygenase enzyme. The irreversible inhibition of the cyclo-oxygenase by aspirin as demonstrated in studies of other investigators suggests that the return of kidney prostaglandin synthetase activity after aspirin inhibition represents synthesis of new cyclo-oxygenase protein. © 1978.
Note:
Related Files :
Animal
Female
In vitro
Kidney Medulla
Meclofenamic Acid
Prostaglandins
Rabbits
Show More
Related Content
More details
DOI :
10.1016/0090-6980(78)90142-9
Article number:
Affiliations:
Database:
Scopus
Publication Type:
article
;
.
Language:
English
Editors' remarks:
ID:
29430
Last updated date:
02/03/2022 17:27
Creation date:
17/04/2018 00:46
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Scientific Publication
Prostaglandin biosynthesis in rabbit kidney medulla: Inhibition in-vitro vs. in-vivo by aspirin, indomethacin and meclofenamic acid
15
Gafni, Y., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Schwartzman, M., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Raz, A., Department of Biochemistry The George S. Wise Center for Life Sciences Tel-Aviv University, Tel-Aviv, Israel
Prostaglandin biosynthesis in rabbit kidney medulla: Inhibition in-vitro vs. in-vivo by aspirin, indomethacin and meclofenamic acid
The non-steroidal anti-inflammatory drugs aspirin, indomethacin and meclofenamic acid were compared for their potency and duration of inhibition of prostaglandin biosynthesis in rabbit kidney medulla. Indomethacin and meclofenamic acid showed equal potency of inhibition in-vitro (IC50 0.88 μM and 0.85 μM respectively) while aspirin was a much weaker inhibitor (IC50 120 μM). In-vivo, indomethacin was the most powerful inhibitor (ID50 0.034 mg/kg) followed by meclofenamic acid (0.45 mg/kg) and aspirin (2.35 mg/kg). Studies on the duration of in-vivo inhibition by these compounds showed the effect of indomethacin and meclofenamic acid to be completely reversed within 4-6 hours. In contrast, return of kidney prostaglandin biosynthetic activity following aspirin inhibition is very slow and significant inhibition is still present 48 hours after a single aspirin injection. The inhibitory effect of aspirin in-vivo could be blocked by pretreatment with indomethacin, indicating that both drugs interact with related sites on the cyclo-oxygenase enzyme. The irreversible inhibition of the cyclo-oxygenase by aspirin as demonstrated in studies of other investigators suggests that the return of kidney prostaglandin synthetase activity after aspirin inhibition represents synthesis of new cyclo-oxygenase protein. © 1978.
Scientific Publication
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