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Chemical Compound Review:

Lopac-R-108 (3,4-dihydroxy-5-nitro- phenyl)-(2...

Synonyms: AC1MRNAO, R108_SIGMA, CHEMBL1256291, SureCN6036458, OR-1139, ...

Rivas, E. et al., Blessing, H. et al., Törnwall, M. et al., van Duursen, M.B. et al., Percy, E. et al., et al.

van Duursen, Sanderson, de Jong, Kraaij, van den Berg,

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Psychiatry related information on OR 1139

2. QO IA (3-(3-hydroxy-4-methoxy-5-nitrobenzylidene)-2,4-pentanedione), QO IIR ([2-(3,4-dihydroxy-2-nitrophenyl)vinyl]phenyl ketone), nitecapone and Ro-41-0960 (30 mg kg(-1), i.p.) were given to reserpinized rats 1 h before the administration of L-DOPA/carbidopa (LD/CD, 50:50 mg kg(-1), i.p.). Locomotor activity was assessed 1 h later [1].

High impact information on OR 1139

L-DOPA-induced lipid peroxidation in mesencephalic cultures was not modified by the COMT inhibitor Ro 41-0960 (1 micro M) [2].
In contrast, COMT inhibitors, U-0521 and Ro 41-0960, dose-dependently increased intracellular [3H]-NE retention with a maximal increase of 4.5 fold [3].
1. The effects of two new synthetic compounds showing in vitro catechol-O-methyl transferase (COMT) inhibitor properties were studied in vivo and compared with the effects of nitecapone and Ro-41-0960 [1].
The effects of three new catechol O-methyltransferase (COMT) inhibitors (nitecapone, entacapone and Ro 41-0960) were assessed on brain neurochemistry and psychomotor tests in levodopa/carbidopa-treated rats and mice [4].

Associations of OR 1139 with other chemical compounds

Effect of L-Dopa and the catechol-O-methyltransferase inhibitor Ro 41-0960 on sulfur amino acid metabolites in rats [5].

Gene context of OR 1139

Distinct interindividual variations were observed in sensitivity toward COMT inhibition among the various tissue samples, as was shown by the range in IC(50) values for Ro 41-0960 (5-42 nM) [6].

Analytical, diagnostic and therapeutic context of OR 1139

Investigations of L-DOPA uptake in rat striatal cultures using HPLC revealed a significant reduction of extracellular L-DOPA concentrations by Ro 41-0960 [2].

References

In vivo effects of new inhibitors of catechol-O-methyl transferase. Rivas, E., de Ceballos, M.L., Nieto, O., Fontenla, J.A. Br. J. Pharmacol. (1999) [Pubmed]
Catechol-O-methyltransferase inhibition protects against 3,4-dihydroxyphenylalanine (DOPA) toxicity in primary mesencephalic cultures: new insights into levodopa toxicity. Blessing, H., Bareiss, M., Zettlmeisl, H., Schwarz, J., Storch, A. Neurochem. Int. (2003) [Pubmed]
Catechol-O-methyltransferase activity in CHO cells expressing norepinephrine transporter. Percy, E., Kaye, D.M., Lambert, G.W., Gruskin, S., Esler, M.D., Du, X.J. Br. J. Pharmacol. (1999) [Pubmed]
Neurochemical and psychomotor interactions of new selective COMT inhibitors with clorgyline and nomifensine in levodopa-treated rats and mice. Törnwall, M., Tuomainen, P., Männistö, P.T. Archives internationales de pharmacodynamie et de thérapie. (1992) [Pubmed]
Effect of L-Dopa and the catechol-O-methyltransferase inhibitor Ro 41-0960 on sulfur amino acid metabolites in rats. Miller, J.W., Shukitt-Hale, B., Villalobos-Molina, R., Nadeau, M.R., Selhub, J., Joseph, J.A. Clinical neuropharmacology. (1997) [Pubmed]
Phytochemicals inhibit catechol-O-methyltransferase activity in cytosolic fractions from healthy human mammary tissues: implications for catechol estrogen-induced DNA damage. van Duursen, M.B., Sanderson, J.T., de Jong, P.C., Kraaij, M., van den Berg, M. Toxicol. Sci. (2004) [Pubmed]

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