Novel human histamine H(3) receptor antagonists.
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.
Shah
Chandra
C
Johnson and Johnson Pharmaceutical Research and Development, L.L.C., San Diego, CA 92121, USA.
McAtee
Laura
L
Breitenbucher
J Guy
JG
Rudolph
Dale
D
Li
Xiaobing
X
Lovenberg
Timothy W
TW
Mazur
Curt
C
Wilson
Sandy J
SJ
Carruthers
Nicholas I
NI
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001812:Blood-Brain Barrier; D001923:Brain Chemistry; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry*; D013329:Structure-Activity Relationship
D006633:Histamine Antagonists; D008024:Ligands; D011725:Pyridines; D018100:Receptors, Histamine H3