Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
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.
Aslanian
Robert
R
The Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. robert.aslanian@spcorp.com
Mutahi
Mwangi wa
Mw
Shih
Neng-Yang
NY
Piwinski
John J
JJ
West
Robert
R
Williams
Shirley M
SM
She
Susan
S
Wu
Ren-Long
RL
Hey
John A
JA
D000818:Animals; D002744:Chlorpheniramine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006634:Histamine H1 Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D008024:Ligands; D011969:Receptors, Histamine H1 / Q000378:metabolism*; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D006633:Histamine Antagonists; D006634:Histamine H1 Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1; D018100:Receptors, Histamine H3; D002744:Chlorpheniramine