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Vol. 303, Issue 2, 805-814, November 2002
1/2-Adrenoceptor
Departments of Psychopharmacology (A.N.-T., D.C., F.D., M.J.M.) and
Molecular and Cellular Pharmacology (V.A., J.-P.N., J.-A.B.), Institut
de Recherches Servier, Paris, France
The accompanying multivariate analysis of the binding profiles of
antiparkinson agents revealed contrasting patterns of affinities at
diverse classes of monoaminergic receptor. Herein, we
characterized efficacies at human (h)D2SHORT(S),
hD2LONG(L), hD3, and hD4.4 receptors and at h
2A-, h2B-,
h2C-, and h1A-adrenoceptors (ARs). As
determined by guanosine
5'-O-(3-[35S]thio)triphosphate
([35S]GTP
S) binding, no ligand displayed "full"
efficacy relative to dopamine (100%) at all "D2-like"
sites. However, at hD2S receptors quinpirole, pramipexole,
ropinirole, quinerolane, pergolide, and cabergoline were as efficacious
as dopamine (Emax
S
studies of h2A-ARs, TL99 (108%), pramipexole (52%),
talipexole (51%), pergolide (31%), apomorphine (16%), and
quinerolane (11%) were agonists and ropinirole and roxindole were
inactive, whereas piribedil and other agents were antagonists. Similar
findings were obtained at h2B- and
h2C-ARs. Using [3H]phosphatidylinositol
depletion, roxindole, bromocriptine, lisuride, and
terguride displayed potent antagonist properties at
h1A-ARs. In conclusion, antiparkinson agents display
diverse agonist and antagonist properties at multiple subtypes of
D2-like receptor and
1/2-AR, actions, which likely contribute
to their contrasting functional profiles.
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