Benzolactam derivatives and their affinity for alpha 1- and alpha 2-adrenoreceptors.
A series of benzolactam derivatives has been evaluated for their affinity for alpha 1 and alpha 2-adrenoreceptors. The influence of terminal amine and amide fragments on the affinity and selectivity has been investigated. It has been found that derivatives containing 1,2,3,4-tetrahydroisoquinoline (THIQ) as the basic component can form potent alpha 1 and/or alpha 2 ligands, and that their alpha 1/alpha 2 selectivity depends on the benzolactam fragment.
Mokrosz
M J
MJ
Department of Medicinal Chemistry, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland.
Charakchieva-Minol
S
S
Kowalski
P
P
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D007769:Lactams / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism*; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism*
D007769:Lactams; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2