[Tropoxin--a new serotonin antagonist and potential antimigraine agent].
The search for serotonin antagonists with cerebrovascular activity was conducted among newly synthesized aromatic and heteroaromatic ethers of tropinone oxim. One of these compounds, namely, hydrochloride-3(3,4,5-trimethoxybenzoiloxiimino-1)-8-methyl-8-a zab icyclo [3,2,1] octane, called tropoxin, prevented the development of serotonin-induced constriction of cerebral vessels in vitro and in vivo experiments. This effect was demonstrated also in experiments with oral administration of the drug. Tropoxin was found to possess affinity for 5-HT2 receptors of the rat brain. Tropoxin surpasses the anti-migraine drug methysergide in antiserotonin cerebrovascular activity. This allows tropoxin to be recommended for study as a means for the treatment of migraine.
Mirzoian
R S
RS
Laboratory of Pharmacology of Cerebrovascular Disorders, Russian Academy of Medical Sciences, Moscow, Russia.
Seredenin
S B
SB
Gan'shina
T S
TS
Kostochka
L M
LM
Romanycheva
N A
NA
Rusakov
D Iu
DIu
D000818:Animals; D001372:Aza Compounds / Q000494:pharmacology*; D001488:Basilar Artery / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000187:drug effects; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology*; D002415:Cats; D002560:Cerebrovascular Circulation / Q000187:drug effects; D008297:Male; D008784:Methysergide / Q000494:pharmacology; D008881:Migraine Disorders / Q000188:drug therapy*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000187:drug effects; D012701:Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology*
C114333:3-(3,4,5-trimethoxybenzoyloximino)-8-methyl-8-azabicyclo(3,2,1)octane; D001372:Aza Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D012701:Serotonin; D008784:Methysergide