Novel human histamine H(3) receptor antagonists

Chandra Shah; Laura McAtee; J Guy Breitenbucher; Dale Rudolph; Xiaobing Li; Timothy W Lovenberg; Curt Mazur; Sandy J Wilson; Nicholas I Carruthers

doi:10.1016/s0960-894x(02)00738-2

Novel human histamine H(3) receptor antagonists

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3309-12. doi: 10.1016/s0960-894x(02)00738-2.

Authors

Chandra Shah¹, Laura McAtee, J Guy Breitenbucher, Dale Rudolph, Xiaobing Li, Timothy W Lovenberg, Curt Mazur, Sandy J Wilson, Nicholas I Carruthers

Affiliation

¹ Johnson and Johnson Pharmaceutical Research and Development, L.L.C., San Diego, CA 92121, USA.

PMID: 12392739
DOI: 10.1016/s0960-894x(02)00738-2

Abstract

High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H(3) receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with favorable blood-brain barrier penetration.

MeSH terms

Administration, Oral
Animals
Biological Availability
Blood-Brain Barrier
Brain Chemistry
Histamine Antagonists / chemical synthesis*
Histamine Antagonists / pharmacokinetics*
Histamine Antagonists / pharmacology
Humans
Ligands
Pyridines / chemical synthesis
Pyridines / pharmacokinetics
Pyridines / pharmacology
Radioligand Assay
Rats
Receptors, Histamine H3 / chemistry*
Structure-Activity Relationship

Substances

Histamine Antagonists
Ligands
Pyridines
Receptors, Histamine H3