The first potent and selective non-imidazole human histamine H4 receptor antagonists.
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
Jablonowski
Jill A
JA
Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, USA.
Grice
Cheryl A
CA
Chai
Wenying
W
Dvorak
Curt A
CA
Venable
Jennifer D
JD
Kwok
Annette K
AK
Ly
Kiev S
KS
Wei
Jianmei
J
Baker
Sherry M
SM
Desai
Pragnya J
PJ
Jiang
Wen
W
Wilson
Sandy J
SJ
Thurmond
Robin L
RL
Karlsson
Lars
L
Edwards
James P
JP
Lovenberg
Timothy W
TW
Carruthers
Nicholas I
NI
D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006633:Histamine Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D007700:Kinetics; D008024:Ligands; D009474:Neurons / Q000166:cytology; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D011994:Recombinant Proteins / Q000187:drug effects / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection
C418607:HRH4 protein, human; D006633:Histamine Antagonists; C498828:Hrh4 protein, rat; D007211:Indoles; D008024:Ligands; D010879:Piperazines; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D011994:Recombinant Proteins