Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.

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Hook BB, Brege C, Linnanen T, Mikaels A, Malmberg A, Johansson AM

Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2167-72.

PubMed ID

10465538 [ View in PubMed

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Abstract

A series of N-arylmethyl substituted (R)-5-methoxy-2-(propylamino)tetralins has been prepared and evaluated for affinity and efficacy at dopamine (DA) D2A receptors. The novel compounds appeared to be antagonists or inverse agonists. (R)-2-[(Benzyl)propylamino]-5-methoxytetralin (7) was characterized as a potent inverse agonists at DA D2A receptors in a [35S]GTPgammaS binding assay.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dopamine	Dopamine D2 receptor	Ki (nM)	1.89	N/A	N/A	Details
Dopamine	Dopamine D2 receptor	Ki (nM)	759	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	0.44	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	0.16	N/A	N/A	Details