Posted by Shawn. T. on July 11, 2002, at 16:53:06
M,100,907 is a potent 5-HT2 antagonist. It has the same effects (I would argue better) as current drugs on schizophrenia, only without the extrapyramidal side effects. Take for example Zyprexa (Olanzapine). This drug exerts its effects on a very wide range of receptors. Note that you need to click on the method links to figure out how to interpret the numbers. See
http://www.gpcr.org/7tm/ligand/Organon/Tablig/LIG_C132539061.html5-HT1a effects are within the range of weakly active, so that rules out 5-HT with regards to possible explanation of Zyprexa's efficacy. With regards to the dopamine receptors, action on those is unnecessary for the treatment of schizophrenia in my opinion and leads to
increased extrapyramidal side effects. See
http://www4.infotrieve.com/search/databases/detailsNew.asp?artID=1986311With regards to NAa1, I shouldn't have to show an
informed reader why it isn't implicated in
schizophrenia. The effects on acetylcholine and
histamine are unnecessary and produce side effects. The antihistamine effects will go away, however.This would imply 5-HT2 antagonism as the mechanism of schizophrenia efficacy in Zyprexa.
As mentioned in the study provided above, 5-HT2
antagonism is the key to treating schizophrenia. The effects caused by actions on additional receptors by current treatments are providing both the positive and negative effects of these drugs. M,100,907 would provide all of the positive effects and none of the negative effects caused by anticholinergic, antihistamine, and dopaminergic actions. I suggest that M,100,907, among other positive actions, helps to modulate dopamine release. It would prevent spikes in dopamine in response to stressors or the introduction of drugs such as amphetamines. My
reasoning is taken from the following study.
http://www4.infotrieve.com/search/databases/detailsNew.asp?artID=24612534With regards to the negative and positive effects of schizophrenia and how M,100,907 affects these, examine the next study provided.
http://www4.infotrieve.com/search/databases/detailsNew.asp?artID=7411933
http://www4.infotrieve.com/search/databases/detailsNew.asp?artID=11283291And finally, an explanation of hallucinations in
schizophrenic patients:
http://www4.infotrieve.com/search/databases/detailsNew.asp?artID=24922782Moreover, a 5-HT2 antagonist, Mirtazapin (Remeron) has been given regulatory approval in the United States. For this reason, I would suggest that a 5-HT2 antagonist would be a very tolerable agent to cure schizophrenia. Sorry for bringing up Remeron again, but I just couldn't help it.
M,100,907 has also been shown to be more effective than both clozapine and haloperidol.
M,100,907 is perhaps one of the most important of drugs created recently in my opinion. Also, for those of you who read my comments on natural selection, I can tie schizophrenia into it.
poster:Shawn. T.
thread:112070
URL: http://www.dr-bob.org/babble/20020709/msgs/112070.html