IngentaConnect Receptor regulatory properties evident in the molecular similarit...

Authors: W.R. Williams¹; W.J. Pugh²; P.J. Nicholls²

Source: Journal of Pharmacy and Pharmacology, Volume 56, Number 12, December 2004 , pp. 1563-1572(10)

Abstract:

Previous computational studies have explored the relative molecular similarity inherent in the ligands of neurotransmitter-regulated cell receptors and purine nucleotides. This study presents the results of an investigation of the major serotonin (5-HT) receptor classes, using molecular superimposition and fitting data. Ligands for 5HT_1B/C/D and 5HT_4/7 receptors identified pharmacophores in the adenine ring of ATP. 5-HT₂ and 5-HT₃ receptor ligands identified pharmacophores in the guanosine nucleotide and cyclic nucleotide, respectively. The described molecular similarity is consistent with the cyclic nucleotide responses observed during signal transduction events initiated by 5-HT, and the reported similarity between ligands of the 5-HT_1B and 5-HT_1D, 5-HT_1A and 5-HT₇, and 5-HT₄ and 5-HT₃ receptors. The results are discussed in terms of current pharmacophoric models and signal transduction events involving interaction between G-protein receptors and catalytic sites.

Document Type: Research article

DOI: 10.1211/0022357044940

Affiliations: 1: School of Care Sciences, University of Glamorgan, Wales, UK 2: Welsh School of Pharmacy, Cardiff University, Wales, UK

The full text electronic article is available for purchase. You will be able to download the full text electronic article after payment.

$38.49 plus tax Refund Policy

Receptor regulatory properties evident in the molecular similarity of serotonin receptor ligands and purine nucleotides