Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine

Robert Aslanian; Mwangi wa Mutahi; Neng-Yang Shih; John J Piwinski; Robert West; Shirley M Williams; Susan She; Ren-Long Wu; John A Hey

doi:10.1016/s0960-894x(03)00357-3

Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine

Bioorg Med Chem Lett. 2003 Jun 16;13(12):1959-61. doi: 10.1016/s0960-894x(03)00357-3.

Authors

Robert Aslanian¹, Mwangi wa Mutahi, Neng-Yang Shih, John J Piwinski, Robert West, Shirley M Williams, Susan She, Ren-Long Wu, John A Hey

Affiliation

¹ The Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. robert.aslanian@spcorp.com

PMID: 12781173
DOI: 10.1016/s0960-894x(03)00357-3

Abstract

Combining the first generation H(1) antihistamine chlorpheniramine (1) with H(3) ligands of the alkylamine type has led to the identification of compound 9d, a dual ligand of both the H(1) and H(3) receptors.

MeSH terms

Animals
Chlorpheniramine / analogs & derivatives*
Chlorpheniramine / metabolism
Chlorpheniramine / pharmacology
Guinea Pigs
Histamine Antagonists / chemistry*
Histamine Antagonists / metabolism
Histamine Antagonists / pharmacology*
Histamine H1 Antagonists / chemistry
Histamine H1 Antagonists / metabolism
Histamine H1 Antagonists / pharmacology
Ligands
Receptors, Histamine H1 / metabolism*
Receptors, Histamine H3 / metabolism*
Structure-Activity Relationship

Substances

Histamine Antagonists
Histamine H1 Antagonists
Ligands
Receptors, Histamine H1
Receptors, Histamine H3
Chlorpheniramine