Novel chiral H3-receptor agonists.
Several alkyl-substituted histamine derivatives have been synthesized and investigated for their agonistic potency on three classes of histamine receptors. While all investigated compounds are full agonists at H3-receptors their relative potency vs. histamine is strongly varying and culminates in alpha R, beta S-dimethylhistamine which is a highly potent and selective H3-receptor agonist.
Lipp
R
R
Institute of Pharmacy, Freie Universität Berlin, FRG.
Arrang
J M
JM
Buschmann
J
J
Garbarg
M
M
Luger
P
P
Schunack
W
W
Schwartz
J C
JC
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006632:Histamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects; D008761:Methylhistamines / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011188:Potassium / Q000494:pharmacology; D051381:Rats; D011968:Receptors, Histamine / Q000187:drug effects*; D018100:Receptors, Histamine H3; D013237:Stereoisomerism
D008761:Methylhistamines; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; C069368:alpha,beta-dimethylhistamine; D006632:Histamine; D011188:Potassium