SUBSTITUTED PYRAZOLES AS NOVEL SELECTIVE LIGANDS FOR THE HUMAN DOPAMINE D-4 RECEPTOR

Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesi sed and evaluated as ligands for the human dopamine D-4 receptor. Comp ounds in series I (exemplified by 8k) have a phenyl ring joined to the 4-position of the pyrazole while those in series II (exemplified by 1 5j) have a 5-phenyl ring linked by a saturated chain to the 4-position of the pyrazole. Both series supplied compounds with excellent affini ty for the human D-4 and good selectivity over other dopamine receptor s. Excellent selectivity over calcium, sodium, and potassium ion chann els was also achieved. (C) 1998 Elsevier Science Ltd. All rights reser ved.