In vitro optimization of structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists.
Hancock
Arthur A
AA
Department of Exploratory Neurobiology, Global Pharmaceuticals Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6125, USA. art.a.hancock@abbott.com
Diehl
Marilyn S
MS
Faghih
Ramin
R
Bush
Eugene N
EN
Krueger
Kathleen M
KM
Krishna
Gopala
G
Miller
Thomas R
TR
Wilcox
Denise M
DM
Nguyen
Phong
P
Pratt
John K
JK
Cowart
Marlon D
MD
Esbenshade
Timothy A
TA
Jacobson
Peer B
PB
D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000494:pharmacology*; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D004195:Disease Models, Animal; D015195:Drug Design; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D008810:Mice, Inbred C57BL; D015162:Micronucleus Tests; D015394:Molecular Structure; D009570:Nitriles / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology*; D011869:Radioligand Assay; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship; D015431:Weight Loss / Q000187:drug effects
C496814:4'-(3-((3R)-3-(dimethylamino)-1-pyrrolidinyl)-propoxy)-3',5'-difluoro-1,1'-biphenyl-4-carbonitrile; C496813:4'-(3-((3R)-3-(dimethylamino)-1-pyrrolidinyl)propoxy)-3'-fluoro-1,1'-biphenyl-4-carbonitrile; C493218:4'-(3-(3(R)-(dimethylamino)-pyrrolidin-1-yl)-propoxy)-biphenyl-4-carbonitrile; D019440:Anti-Obesity Agents; D001713:Biphenyl Compounds; D006633:Histamine Antagonists; D009570:Nitriles; D011759:Pyrrolidines; D018100:Receptors, Histamine H3