1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.

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Thurkauf A, Yuan J, Chen X, Wasley JW, Meade R, Woodruff KH, Huston K, Ross PC

1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.

J Med Chem. 1995 Dec 8;38(25):4950-2.

PubMed ID

8523409 [ View in PubMed

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Abstract

A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 receptors over cloned African Green monkey D2 receptors was observed with 1-(2-pyridyl)-4-[[3-(1-phenylpyrrolyl)]methyl]piperazine.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	254	N/A	N/A	Details
Clozapine	Dopamine D3 receptor	Ki (nM)	466	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	71	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	5	N/A	N/A	Details
Haloperidol	Dopamine D3 receptor	Ki (nM)	3	N/A	N/A	Details
Remoxipride	Dopamine D2 receptor	Ki (nM)	873	N/A	N/A	Details
Remoxipride	Dopamine D3 receptor	Ki (nM)	4603	N/A	N/A	Details
Remoxipride	Dopamine D4 receptor	Ki (nM)	3872	N/A	N/A	Details