N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.

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Lim J, Stock N, Pracitto R, Boueres JK, Munoz B, Chaudhary A, Santini AM, Orr K, Schaffhauser H, Bezverkov RE, Aiyar J, Venkatraman S

N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1913-6.

PubMed ID

15050626 [ View in PubMed

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Abstract

A series of N-acridin-9-yl-butane-1,4-diamines were found to be high-affinity ligands of the alpha(2)delta subunit of voltage gated calcium channels. The SAR studies of butane-1,4-diamine side chain resulted in the identification of compound 10 (IC(50)=9 nM), which is more potent than gabapentin (IC(50)=27 nM). Partial saturation of the acridine ring was also pursued and provided a compound with higher binding affinity than 1.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Gabapentin	Voltage-dependent calcium channel subunit alpha-2/delta-1	IC 50 (nM)	27	N/A	N/A	Details