Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography.
The effects of pharmacological intervention on brain muscarinic cholinergic receptor (mAChR) binding were assessed in seven patients with Parkinson's disease by positron emission tomography and carbon-11 labelled N-methyl-4-piperidyl benzilate ([11C]NMPB). [11C]NMPB was injected twice, approximately 2 hours apart, in each patient, to assess the effect of single doses of 4 mg of trihexyphenidyl (n = 5) or 400 mg of L-dopa with 57 mg of benserazide (n = 2) on the binding parameter of mAChRs (K3). There was a mean 28% inhibition of K3 values in the brain in the presence of trihexyphenidyl, which was assumed to reflect mAChR occupancy. No significant change in K3 was observed in the presence of L-dopa. This study demonstrates the feasibility of measuring mAChR occupancy by an anticholinergic medication with PET.
Shinotoh
H
H
Department of Neurology, School of Medicine, Chiba University, Japan.
Asahina
M
M
Inoue
O
O
Suhara
T
T
Hirayama
K
K
Tateno
Y
Y
D000368:Aged; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D005260:Female; D006801:Humans; D007700:Kinetics; D007980:Levodopa / Q000494:pharmacology*; D008297:Male; D008875:Middle Aged; D010300:Parkinson Disease / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014055:Tomography, Emission-Computed; D014282:Trihexyphenidyl / Q000494:pharmacology*
D011976:Receptors, Muscarinic; D007980:Levodopa; D014282:Trihexyphenidyl