Posted by CrAzYmEd on May 23, 2010, at 10:03:38 [reposted on May 24, 2010, at 22:41:58 | original URL]
In reply to Re: to crazymed, posted by CrAzYmEd on May 23, 2010, at 9:59:46
Also noticed my first post was a bit of a mess, here's the most important stuff:
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[Anxiolytic effects of lisuride and its agonistic action to central 5-HT1A receptors]
[Article in Japanese]Akai T, Takahashi M, Nakada Y, Ohnishi R, Ikoma Y, Yamaguchi M.
Research Department, Nihon Schering K.K., Osaka, Japan.
Abstract
Effects of lisuride, a derivative of ergot alkaloid, on central 5-HT1A receptors were investigated biochemically, behaviorally and electroencephalographically (EEG) in rats and rabbits. Effects of lisuride in water-lick conflict tests were also investigated in rats. Lisuride was found to strongly inhibit the bindings of [3H]8-OH-DPAT to 5-HT1A receptors in the raphe nucleus, hippocampus, cortex, amygdala and hypothalamus of rat brain. Inhibitory effects of lisuride on bindings of [3H]8-OH-DPAT in the hippocampus was almost the same as that of 5-HT (Ki = 0.5 nM) and stronger than those of the 5-HT agonist 5-MeO-DMT (Ki = 2.1 nM) or other ergot derivatives (bromocriptine and pergolide, Ki = 3.0 nM). Lisuride (0.1-0.5 mg/kg, i.p.), like 8-OH-DPAT, dose-dependently induced a 5-HT behavioral syndrome in rats. Lisuride affected locomotor activity in rats, whereas 8-OH-DPAT did not. In hippocampal EEG of rabbits, lisuride (0.01-0.03 mg/kg, i.v.), like 8-OH-DPAT and diazepam, dose-dependently inhibited rhythmical slow activity (RSA) induced by acoustical stimulation (3100 Hz) and also inhibited the RSA increased by administration of anxiogenic FG7142. In water-lick conflict tests, lisuride (0.05-0.1 mg/kg, i.p.), like diazepam, increased the number of shocks. These findings indicated that lisuride acts as a strong agonist on central 5-HT1A receptors and suggested that lisuride might be a potential anxiolytic.
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[Effects in animal models of depression of lisuride alone and upon coadministration with antidepressants]
[Article in Japanese]Nakamura K, Ikoma Y, Kimura K, Nakada Y, Kobayashi S, Yamaguchi M, Nakagawa H.
Research Department, Nihon Schering K.K., Osaka, Japan.
Abstract
Effects of lisuride, a central dopamine and serotonin agonist of the ergot type, in animal models of depression were investigated in comparison with those of desipramine, mianserin and rolipram. Lisuride, like desipramine and mianserin, inhibited reserpine-induced hypothermia in mice (0.5-5.0 mg/kg, i.p.) and suppressed muricide in olfactory bulbectomized rats (ED50 = 0.16 mg/kg, i.p.) in a dose-dependent manner. The anti-muricidal effect was slightly enhanced by the repeated administration of 0.25 mg/kg lisuride. Lisuride (0.05-0.25 mg/kg, i.p.), like desipramine, dose-dependently reduced the duration of immobility in rats forced to swim, and this effect was antagonized by haloperidol. The reduction of immobility time was enhanced by the repeated administration of lisuride; at the same time, the ambulation in rats increased. Furthermore, the immobility-reducing effects of desipramine and rolipram were markedly enhanced by the co-administration of a low dose of lisuride (0.025 mg/kg, i.p.), which by itself had no effect on the immobility time. These results indicate that lisuride may be useful for the treatment of depression and indicate that a low dose of lisuride may enhance the clinical effectiveness of antidepressants such as desipramine.
-------------------------------------------------It has been shown to be a anxiolytic/antidepressant and also that it markedly enhances the efficiacy of other antidepressants in low doses wich itself arent active.
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Pharmacological profileLisuride is a:
5HT1A agonist
5HT1B agonist
5HT2A agonist
5HT2C agonist
5HT6 agonist
5HT7 antagonist
5HT5A didnt find yet
D2 agonist
D4 agonistAccording to the journal not significant:
5ht1e
D5
H2
D3
And interacts with several andronergic receptors.It has a short half life tough, like ritalin thats a bit of a downside.
poster:CrAzYmEd
thread:948688
URL: http://www.dr-bob.org/babble/neuro/20100223/msgs/948696.html