Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor

Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated as ligands for the human dopamine D4 receptor. Compounds 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 15j) have a 5-phenyl r...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1998-10, Vol.6 (10), p.1731-1743
Main Authors: Bourrain, S, Collins, I, Neduvelil, J G, Rowley, M, Leeson, P D, Patel, S, Emms, F, Marwood, R, Chapman, K L, Fletcher, A E, Showell, G A
Format: Article
Language:English
Subjects:
Antipsychotic Agents - chemistry
Antipsychotic Agents - metabolism
Antipsychotic Agents - pharmacology
Drug Design
Heterocyclic Compounds - chemical synthesis
Heterocyclic Compounds - metabolism
Heterocyclic Compounds - pharmacology
Humans
Ion Channels - drug effects
Ion Channels - metabolism
Piperazines - chemical synthesis
Piperazines - metabolism
Piperazines - pharmacology
Pyrazoles - chemistry
Pyrazoles - metabolism
Receptors, Dopamine D2 - metabolism
Receptors, Dopamine D4
Structure-Activity Relationship
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Summary:Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated as ligands for the human dopamine D4 receptor. Compounds 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 15j) have a 5-phenyl ring linked by a saturated chain to the 4-position of the pyrazole. Both series supplied compounds with excellent affinity for the human D4 and good selectivity over other dopamine receptors. Excellent selectivity over calcium, sodium, and potassium ion channels was also achieved.
ISSN:0968-0896
DOI:10.1016/S0968-0896(98)00134-5