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Vol. 303, Issue 2, 791-804, November 2002
Departments of Psychopharmacology (M.J.M., D.C., A.N.-T.),
Statistics (L.M.), and Molecular and Cellular Pharmacology (V.A.,
J.-A.B.), Institut de Recherches Servier, Paris, France
Because little comparative information is available concerning
receptor profiles of antiparkinson drugs, affinities of 14 agents were
determined at diverse receptors implicated in the etiology and/or
treatment of Parkinson's disease: human (h)D1, hD2S, hD2L, hD3, hD4,
and hD5 receptors; human 5-hydroxytryptamine (5-HT)1A, h5-HT1B, h5-HT1D,
h5-HT2A, h5-HT2B, and h5-HT2C
receptors; h
1A-, h1B-,
h1D-, h2A-, h2B-,
h2C-, rat 2D-, h
1-, and h2-adrenoceptors (ARs); and native
histamine1 receptors. A correlation matrix (294 pKi values) demonstrated substantial
"covariance". Correspondingly, principal components analysis
revealed that axis 1, which accounted for 76% variance, was associated
with the majority of receptor types: drugs displaying overall high
versus modest affinities migrated at opposite extremities. Axis 2 (7%
of variance) differentiated drugs with high affinity for
hD4 and H1 receptors versus
h1-AR subtypes. Five percent of variance was
attributable to axis 3, which distinguished drugs with marked affinity
for h1- and h2-ARs versus hD5
and 5-HT2A receptors. Hierarchical (cluster) analysis of
global homology generated a dendrogram differentiating two major groups
possessing low versus high affinity, respectively, for multiple
serotonergic and hD5 receptors. Within the first group,
quinpirole, quinerolane, ropinirole, and pramipexole interacted principally with hD2, hD3, and hD4
receptors, whereas piribedil and talipexole recognized dopaminergic
receptors and h2-ARs. Within the second group, lisuride
and terguride manifested high affinities for all sites, with
roxindole/bromocriptine, cabergoline/pergolide, and
6,7-dihydroxy-N,N-dimethyl-2-ammotetralin
(TL99)/apomorphine comprising three additional subclusters of closely
related ligands. In conclusion, an innovative multivariate analysis
revealed marked heterogeneity in binding profiles of antiparkinson
agents. Actions at sites other than hD2 receptors likely
participate in their (contrasting) functional profiles.
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