Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
Structure-activity relationship studies on novel non-imidazole, D-amino acid containing ligands of histamine 3 receptors are presented. A-304121 is a D-alanine piperazine amide with high affinity at the rat H(3) receptor.
Faghih
Ramin
R
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6123, USA. ramin.faghih@abbott.com
Dwight
Wesley
W
Black
Larry
L
Liu
Huaqing
H
Gentles
Robert
R
Phelan
Kathleen
K
Esbenshade
Timothy A
TA
Ireland
Lynne
L
Miller
Thomas R
TR
Kang
Chae-Hee
CH
Krueger
Kathy M
KM
Fox
Gerard B
GB
Hancock
Arthur A
AA
Bennani
Youssef L
YL
D000215:Acylation; D020816:Amino Acid Motifs; D000596:Amino Acids / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D001682:Biological Availability; D002540:Cerebral Cortex / Q000378:metabolism; D006633:Histamine Antagonists / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008024:Ligands; D010879:Piperazines / Q000737:chemistry; D051381:Rats; D011969:Receptors, Histamine H1 / Q000378:metabolism; D011970:Receptors, Histamine H2 / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000596:Amino Acids; D006633:Histamine Antagonists; D008024:Ligands; D010879:Piperazines; D011969:Receptors, Histamine H1; D011970:Receptors, Histamine H2; D018100:Receptors, Histamine H3