Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.

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Thomas C, Hubner H, Gmeiner P

Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.

Bioorg Med Chem Lett. 1999 Mar 22;9(6):841-6.

PubMed ID

10206547 [ View in PubMed

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Abstract

Subreceptor selectivity tuning of N-(3-pyrrolidinyl)benzamides leading to the selective dopamine D3 ligand ent1h and the derivatives 1g and 1e/ent1e which preferably recognize human D2 or D4 receptors, respectively, is described. Binding profiles were controlled by both, absolute and relative configuration. The enantiopure target compounds were synthesized from aspartic acid.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sulpiride	Dopamine D2 receptor	Ki (nM)	120	N/A	N/A	Details
Sulpiride	Dopamine D2 receptor	Ki (nM)	51	N/A	N/A	Details
Sulpiride	Dopamine D3 receptor	Ki (nM)	88	N/A	N/A	Details