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Chemical Compound Review:

Beclobrate ethyl2-[4-[(4- chlorophenyl)methyl]phenoxy...

Synonyms: Beclobrato, Beclobratum, Beclosclerin, SureCN49779, CHEMBL152684, ...

Manzoni, C. et al., Mayer, S. et al., Kocarek, T.A. et al., Adrian, R.W. et al., Avogaro, P. et al., et al.

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Sgd 24774

Beclobrate and liver disease [1].
From a comparison of the ED25 values of beclobrate and clofibrate, the new drug is 11 times more potent with respect to its hypocholesterolemic activity and 36 times more hypotriglyceridemic in normally fed rats, and lowers fructose-induced hypertriglyceridemia in rats 20 times as effectively as does clofibrate [2].

High impact information on Sgd 24774

We conclude that (1) Beclo is more potent than CPIB as an inducer of peroxisome proliferation-associated enzyme activities; (2) two metabolites of Beclo are more potent than the parent molecule as inducers of these activities and (3) these metabolites may contribute to the lipid-lowering and/or hepatomegalic effects of beclobrate in rats [3].
In addition, beclobrate administration dramatically increased the activity of the high-affinity receptors for beta-VLDL in isolated liver membranes (Bmax: 208 +/- 17.6 vs. 146 +/- 2.6 ng/mg of protein for controls) [4].
The adduct densities for (-)- and (+)-beclobric acid after single 100 mg beclobrate doses were 0.147 x 10(-4) and 0.177 x 10(-4) mol/mol protein [5].
The electrophoretic pattern of LP in patients treated with beclobrate revealed a decrease of VLDL, a normalization of the LDL fraction and an increase of HDL [6].
The chiral lipid regulating agent beclobrate (CAS 55937-99-0), which was marketed as racemate, is - like clofibrate - rapidly hydrolyzed to beclobric acid immediately after absorption [7].

Biological context of Sgd 24774

Pharmacokinetics of beclobric acid enantiomers and their conjugates after single and multiple oral dosage of racemic beclobrate [7].

Associations of Sgd 24774 with other chemical compounds

Lipid-lowering effect of the new drugs eniclobrate and beclobrate in patients with hyperlipidemia type II a and type II b [8].

Gene context of Sgd 24774

Beclobrate enhances hepatic HMG-CoA reductase activity but does not affect cholesterol-7 alpha hydroxylase [9].

Analytical, diagnostic and therapeutic context of Sgd 24774

The metabolic clearance of 125I-labelled beta-very low density lipoproteins (beta-VLDL) injected into these animals almost doubled (0.20 1/h vs. 0.13 1/h in controls) after treatment with 20 mg/kg of beclobrate [4].
After oral administration unchanged beclobrate was not detected in plasma [7].

References

Beclobrate and liver disease. Aebi, U., Reinhart, W.H. Ann. Intern. Med. (1990) [Pubmed]
Pharmacological studies with beclobrate, a new hypolipidemic agent. Adrian, R.W., Ismail, S., Jahn, U. Arzneimittel-Forschung. (1983) [Pubmed]
Induction of peroxisomal fatty acyl-CoA oxidase and microsomal laurate hydroxylase activities by beclobric acid and two metabolites in primary cultures of rat hepatocytes. Kocarek, T.A., Feller, D.R. Biochem. Pharmacol. (1987) [Pubmed]
Differential effects of beclobrate on lipid/lipoprotein distribution in normal and hypercholesterolemic rats. Manzoni, C., Lovati, M.R., Bonelli, A., Galli, G., Sirtori, C.R. Eur. J. Pharmacol. (1990) [Pubmed]
In vitro and in vivo irreversible plasma protein binding of beclobric acid enantiomers. Mayer, S., Mutschler, E., Benet, L.Z., Sphahn-Langguth, H. Chirality. (1993) [Pubmed]
A cross-over controlled study on beclobrate versus bezafibrate in the treatment of type IIb hyperlipoproteinaemia. Avogaro, P., Bittolo Bon, G., Cazzolato, G., Soldan, S., Bufalino, L. Drugs under experimental and clinical research. (1989) [Pubmed]
Pharmacokinetics of beclobric acid enantiomers and their conjugates after single and multiple oral dosage of racemic beclobrate. Mayer, S., Spahn-Langguth, H., Gikalov, I., Mutschler, E. Arzneimittel-Forschung. (1993) [Pubmed]
Lipid-lowering effect of the new drugs eniclobrate and beclobrate in patients with hyperlipidemia type II a and type II b. Najemnik, C., Lageder, H., Regal, H., Irsigler, K. Arzneimittel-Forschung. (1981) [Pubmed]
Influence of beclobrate and eniclobrate on cholesterol metabolism in rats. Kritchevsky, D., Tepper, S.A., Mueller, M.A., Klurfeld, D.M. Arzneimittel-Forschung. (1983) [Pubmed]

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