Drug intelligence / Profile preview

ro 41-0960

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

**Ro 41-0960** is a synthetic small molecule and a potent, selective inhibitor of the enzyme catechol-O-methyltransferase (COMT). COMT catalyzes the methylation and inactivation of catecholamines and catechol estrogens. Ro 41-0960 offers high selectivity in inhibiting COMT's catalytic site, thereby blocking methylation and increasing levels of substrates such as L-Dopa and catechol estrogens in tissues[1][4][6][9]. It is fluorine-containing and acts peripherally as well as in tissues like kidney and liver where COMT activity is high, although in vivo it shows poor brain uptake[3]. Ro 41-0960 served in research contexts for the study of COMT function, estrogen metabolism, and potential modulation of biochemical pathways relevant to neurodegenerative and hormone-dependent diseases. It is structurally related to Ro 40-7592 (tolcapone), utilized in Parkinson's disease clinical research[3]. Ro 41-0960 additionally acts as a selective activator of cardiac SERCA2a-PLB complex, increasing the apparent Ca affinity in cardiac muscle but not skeletal muscle[7].

Other names
RO 41-0960 COMT INHIBITORRO41-0960 COMT INHIBITORRO-41-0960 COMT INHIBITOR2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone(3,4-dihydroxy-5-nitrophenyl)(2-fluorophenyl)methanone(3,4-Dihydroxy-5-nitrophenyl)(2-fluorophenyl)-methanonMethanone, (3,4-dihydroxy-5-nitrophenyl)(2-fluorophenyl)-SXV6U29ZOISXV-6U29ZOISXV 6U29ZOI
02

Targets

COMT (Catechol-O-methyltransferase)ATP2A2 (Sarco/endoplasmic reticulum calcium ATPase isoform 2a)

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