[Cerebrovascular serotonin antagonists and agonist among tropan derivatives].
A series of new tropan derivatives have been synthesized and investigated, which can both weaken and potentiate the serotonin-induced cerebrovascular constrictory reactions. The compound LK-728 produces a pronounced antiserotonin cerebrovascular action comparable to that of tropoxin, but being superior to the reference drug in the effect duration. On the contrary, another tropan derivative LK-769 enhances the cerebrovascular response to serotonin. A similar effect was demonstrated with the well-known antimigraine agent sumatriptan, which is an agonist of 5HT1B/1D receptors. The ability of sumatriptan to increase the local cerebral blood flow which was observed in our experiments, may also play an important role in the mechanism of the antimigraine action produced by this serotonin receptor agonist.
Gan'shina
T S
TS
Bezhanian
S G
SG
Kostochka
L M
LM
Volkova
M Iu
MIu
Mirsoian
R S
RS
D000818:Animals; D001372:Aza Compounds / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology; D002560:Cerebrovascular Circulation / Q000187:drug effects*; D008297:Male; D051381:Rats; D012701:Serotonin / Q000378:metabolism*; D058825:Serotonin 5-HT1 Receptor Agonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000494:pharmacology*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*; D018170:Sumatriptan / Q000494:pharmacology; D014326:Tropanes / Q000494:pharmacology*; D014363:Tryptamines / Q000494:pharmacology / Q000627:therapeutic use; D014662:Vasoconstrictor Agents / Q000494:pharmacology*
C114333:3-(3,4,5-trimethoxybenzoyloximino)-8-methyl-8-azabicyclo(3,2,1)octane; D001372:Aza Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D058825:Serotonin 5-HT1 Receptor Agonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D014326:Tropanes; D014363:Tryptamines; D014662:Vasoconstrictor Agents; D012701:Serotonin; D018170:Sumatriptan