Posted by zeugma on December 5, 2004, at 12:17:04
In reply to Re: Second the recommendation for Provigil, posted by linkadge on December 5, 2004, at 10:58:59
> It really helps my mood too. I explained this to my doctor but he didn't care.
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> Coffee alters a lot of things. Opiates, noradrenaline, dopamine, acetylcholine. I tell ya, mother nature is playing games with us.
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> If only coffee had a half life of 36 hours, I'd be a lot happier.
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> Linkadge
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> The psychotropic effects of caffeine have not escaped the attention of pharmacologists. In particular, the AD effects (documented lowering of suicide rates) and anti-Parkinson's effects, have attracted research. This derivative of caffeine looks particularly promising:http://www.jbc.org/cgi/content/full/277/39/36040
ABSTRACT
Caffeine and more specific antagonists of the adenosine A2A receptor recently have been found to be neuroprotective in the MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) model of Parkinson's disease. Here we show that 8-(3-chlorostyryl)caffeine (CSC), a specific A2A antagonist closely related to caffeine, also attenuates MPTP-induced neurotoxicity. Because the neurotoxicity of MPTP relies on its oxidative metabolism to the mitochondrial toxin MPP+, we investigated the actions of CSC on striatal MPTP metabolism in vivo. CSC elevated striatal levels of MPTP but lowered levels of the oxidative intermediate MPDP+ and of MPP+, suggesting that CSC blocks the conversion of MPTP to MPDP+ in vivo. In assessing the direct effects of CSC and A2A receptors on monoamine oxidase (MAO) activity, we found that CSC potently and specifically inhibited mouse brain mitochondrial MAO-B activity in vitro with a Ki value of 100 nM, whereas caffeine and another relatively specific A2A antagonist produced little or no inhibition. The A2A receptor independence of MAO-B inhibition by CSC was further supported by the similarity of brain MAO activities derived from A2A receptor knockout and wild-type mice and was confirmed by demonstrating potent inhibition of A2A receptor knockout-derived MAO-B by CSC. Together, these data indicate that CSC possesses dual actions of MAO-B inhibition and A2A receptor antagonism, a unique combination suggesting a new class of compounds with the potential for enhanced neuroprotective properties.
Interestingly, Provigil is also neuroprotective in the same animal model of Parkinson's-like neurotoxicity.
I read yesterday in a sleep disorders textbook that approx. six cups of coffee produces a psychostimulant effect roughly equal to 5 mg amphetamine.
poster:zeugma
thread:424591
URL: http://www.dr-bob.org/babble/20041201/msgs/424708.html