Binding of dopamine receptor ligands to human D2 and D3 receptors was characterized in
Chinese hamster ovary (CHO) cells using the dopamine D2 receptor antagonist [125I] …

L-745,870,(3-{[4-(4-chlorophenyl)piperazin-1-yl]methyl}-1Hpyrollo[2,3-b] pyridine, was
identified as a selective dopamine D4 receptor antagonist with excellent oral bioavailability and …

Schizophrenia is a mental illness for which there is still a great need for novel drug therapy.
Classical neuroleptics, which are presumed to act by antagonism of dopamine D2 receptors, …

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT 2A antagonists.
Structure–activity relationship studies have shown that h5-HT 2A affinity can be attained via …

5-(4-Chlorophenyl)-3-(1-(4-chlorobenzyl)piperidin-4-yl)pyrazole (3) was identified from
screening of the Merck sample collection as a human dopamine D4 (hD4) receptor ligand with …

The synthesis and cortical muscarinic activityof a novel series of pyrazine-based agonists is
described. Quinuclidine and azanorbomane derivatives were prepared either by reaction of …

The D 2 dopamine receptor is known to be functionally coupled when expressed in CHO cells,
whereas the effector systems for the D 3 , dopamine receptor remain unclear. A chimeric, …

3-(4-Piperidinyl)-5-arylpyrazoles, such as 1, were selective for the cloned human dopamine
D 4 receptor (hD 4 ), but also showed affinity at voltage sensitive calcium, sodium and …

… Showell*, Frances Emms, Rosemarie Marwood, Desmond O’Connor, Smita Patel, Paul D.
Leeson … (b) Rowley M, Broughton HB, Collins I, Baker R, Emms F, Marwood R, Pate1 S …

Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated
as ligands for the human dopamine D 4 receptor. Compounds in series I (exemplified by 8k) …