Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.
In vitro assays on a series of cis- and trans-octahydrobenzo[g]quinolines indicated an unusual trend of affinities at the dopaminergic receptors and alpha adrenoceptors. The trans N-benzyl analogues exhibited affinity at the alpha2 as well as the D1-like receptors whereas their N-unsubstituted congeners showed a distinct preference for the alpha2 adrenoceptor. Enhanced activity for the alpha2 receptors was also exhibited by the cis N-benzylated isomers. These observations are interpreted by theoretical calculations.
Thermos
K
K
Laboratory of Pharmacology, School of Medicine, University of Crete, Heraklion, Greece.
Froudakis
G E
GE
Tagmatarchis
N
N
Katerinopoulos
H E
HE
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D015259:Dopamine Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D008962:Models, Theoretical; D011224:Prazosin / Q000378:metabolism; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000737:chemistry / Q000187:drug effects*; D018341:Receptors, Adrenergic, alpha-2 / Q000737:chemistry / Q000187:drug effects*; D013134:Spiperone / Q000378:metabolism
D015259:Dopamine Agents; D011804:Quinolines; D011942:Receptors, Adrenergic, alpha; D018341:Receptors, Adrenergic, alpha-2; D013134:Spiperone; D011224:Prazosin