Synthesis and binding studies of some epibatidine analogues.
A series of epibatidine analogues and their positional isomers bearing an 8-azabicyclo[3.2.1]octane moiety is described. Some of the compounds, especially those containing 8-azabicyclo[3.2.1]oct-2-ene moiety show high affinity for the nicotinic cholinergic receptor.
Rádl
S
S
Research Institute of Pharmacy and Biochemistry, Prague, Czech Republic. radl@vufb.cz
Hezký
P
P
Hafner
W
W
Budesínský
M
M
Hejnová
L
L
D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D006325:Heart Atria / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007536:Isomerism; D007700:Kinetics; D018722:Nicotinic Agonists / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D044302:Receptor, Serotonin, 5-HT1B; D011976:Receptors, Muscarinic / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1
D018712:Analgesics, Non-Narcotic; D019086:Bridged Bicyclo Compounds, Heterocyclic; D018722:Nicotinic Agonists; D011725:Pyridines; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D044302:Receptor, Serotonin, 5-HT1B; D011976:Receptors, Muscarinic; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; C082748:epibatidine