3-(4-Aminobutyn-1-yl)pyridines: binding at α4β2 nicotinic cholinergic receptors

• Published in: Bioorganic & medicinal chemistry letters Vol. 14; no. 2; pp. 523 - 526
• Main Authors: Dogruer, Deniz, Lee, Mase, Dukat, Malgorzata, Damaj, M.Imad, Martin, Billy R., Glennon, Richard A.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 2004; Elsevier
• Subjects: Biological and medical sciences; Cholinergic system; Medical sciences; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; Pharmacology. Drug treatments; Biological fixation; Cholinergic receptor; Acetylenic compound; Structure activity relation; Nitrogen heterocycle; Ligand; Six membered ring; Affinity; Chemical synthesis; In vitro; Nicotinic receptor; Secondary amine
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2003.10.033

The binding of a series pyridylbutynylamines
6 was examined at α4β2 nACh receptors. Structural modifications, comparing
6 with pyridyl ethers
2, did not consistently result in parallel effects on receptor affinity, suggesting possible differences in their modes of binding. Furthermore, the binding of amine
6a seemed to be accounted for by the newer vector pharmacophore models.
The binding of a series of pyridylbutynylamines at α4β2 nACh receptors was shown to be sensitive to, and dependent upon, the nature of ring and terminal amine substituents.