Administration of the new COMT inhibitor OR-611 increases striatal uptake of fluorodopa.
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Administration of the new COMT inhibitor OR-611 increases striatal uptake of fluorodopa. / Guttman, M; Léger, G; Reches, A; Evans, A; Kuwabara, H; Cedarbaum, J M; Gjedde, A.
In: Movement Disorders, Vol. 8, No. 3, 1993, p. 298-304.Research output: Contribution to journal › Journal article › Research › peer-review
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T1 - Administration of the new COMT inhibitor OR-611 increases striatal uptake of fluorodopa.
AU - Guttman, M
AU - Léger, G
AU - Reches, A
AU - Evans, A
AU - Kuwabara, H
AU - Cedarbaum, J M
AU - Gjedde, A
PY - 1993
Y1 - 1993
N2 - L-Dopa is metabolized to 3-O-methyldopa (3OMD) by catechol-O-methyltransferase (COMT). This reduces the amount of L-dopa available for entry into brain. We studied the effect of OR-611, a new COMT inhibitor, on plasma and brain 6-[18F]-fluoro-L-dopa (6FD) metabolism in cynomolgus monkeys with positron emission tomography (PET). OR-611 pretreatment substantially reduced plasma 6FD metabolism to 3-O-methylfluorodopa (3OMFD). PET measurements of striatal 6FD concentrations showed an average 2.3-fold increase following OR-611 pretreatment, compared to the same animals in the control state. OR-611 inhibits plasma metabolism of 6FD and increases brain uptake of this L-dopa analog. OR-611 appears to be a promising agent as an adjunct to L-dopa for the treatment of patients with Parkinson's disease.
AB - L-Dopa is metabolized to 3-O-methyldopa (3OMD) by catechol-O-methyltransferase (COMT). This reduces the amount of L-dopa available for entry into brain. We studied the effect of OR-611, a new COMT inhibitor, on plasma and brain 6-[18F]-fluoro-L-dopa (6FD) metabolism in cynomolgus monkeys with positron emission tomography (PET). OR-611 pretreatment substantially reduced plasma 6FD metabolism to 3-O-methylfluorodopa (3OMFD). PET measurements of striatal 6FD concentrations showed an average 2.3-fold increase following OR-611 pretreatment, compared to the same animals in the control state. OR-611 inhibits plasma metabolism of 6FD and increases brain uptake of this L-dopa analog. OR-611 appears to be a promising agent as an adjunct to L-dopa for the treatment of patients with Parkinson's disease.
U2 - 10.1002/mds.870080308
DO - 10.1002/mds.870080308
M3 - Journal article
C2 - 8341294
VL - 8
SP - 298
EP - 304
JO - Movement Disorders
JF - Movement Disorders
SN - 0885-3185
IS - 3
ER -
ID: 14944407