User:Etienne Robillard/Notebook/Paliperidone/2013/06/21

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Current revision (22:48, 6 October 2013) (view source)
(Starting Material)
 
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as always :)
as always :)
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===Objective===
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===Objectives===
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The purposes and aims of this experiment are two folds: First, we want you to avoid being mentally harmed while being forced to take antipsychotics drugs. Second, we want
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you to find a way to functionalize the degradation of the psychoactive compound into a non-psychoactive, and safe [http://jb.oxfordjournals.org/content/112/1/139.short racemase].
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===Design philosophy===
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* broad spectrum specificity : The degradation of the optically-active racemate must accept many substrates. (ie: pines and dones)
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* Fast, safe, and side-effects free bioremoval of the metabolite.
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===One Step Transamination and Degradation of Paliperidone to PLP===
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* Approach 1: racemization of paliperidone to 5'-pyridoxal phosphate (PLP) via [http://www.uniprot.org/uniprot/Q9UBK8 MTRR(ATP) synthase], a B-glucuronide (B-galactosidase) analog. This is an experimental method to neutralize the active metabolite to a more safe mono-aminase, which should hopefully provide a wet blanket for glutamate-induced neurotoxicity.
===Starting Material===
===Starting Material===
* paliperidone: an atypical antipsychotic derived from Risperidone. see [[User:Etienne_Robillard/Notebook/Risperidone|Risperidone]].
* paliperidone: an atypical antipsychotic derived from Risperidone. see [[User:Etienne_Robillard/Notebook/Risperidone|Risperidone]].
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* clozanpine: another atypical antipsychotic
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* isocitrate (citric acid precursor) : refer to "Citric acid cycle" (ascorbic acid)
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* citric acid : refer to "Citric acid cycle"  
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* delta9-tetrahydrocannabinol : competitive GABA antagonist (inhibitor)
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* l-methionine: from eggs (ie: 1 full egg)
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===Glossary===
===Glossary===
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* racemate:
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* racemate:  
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* racemase:
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* [http://goldbook.iupac.org/R05030.html racemization]: "The production of a racemate from a chiral starting material in which one enantiomer is present in excess." (see [http://goldbook.iupac.org/R05025.html Racemate])
* ketoacidosis:
* ketoacidosis:
* reagent:  
* reagent:  
* methylation:
* methylation:
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* glucoronide:  
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* glucuronide:  
* amide:  
* amide:  
* ester:  
* ester:  
* transaminase:
* transaminase:
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* transaldimination:
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* palmitate: Salt/ester of palmitic acid - a saturated fatty acid (reference: [http://en.wikipedia.org/wiki/Palmitate wikipedia])
===Notes===
===Notes===
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* ec 1.1.1.41: NAD-specific isocitrate dehydrogenase (an enzyme): http://www.kegg.jp/dbget-bin/www_bget?ec:1.1.1.41
* ec 1.1.1.41: NAD-specific isocitrate dehydrogenase (an enzyme): http://www.kegg.jp/dbget-bin/www_bget?ec:1.1.1.41
** pathway (Citrate cycle): http://www.kegg.jp/kegg-bin/show_pathway?ec00020+1.1.1.41
** pathway (Citrate cycle): http://www.kegg.jp/kegg-bin/show_pathway?ec00020+1.1.1.41
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* [http://pathman.smpdb.ca/pathways/SMP00033/pathway Methionine Metabolism]
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* [http://en.wikipedia.org/wiki/Beta-glucuronidase Wikipedia:Beta-glucuronidase] (ec 3.2.1.31)
===References===
===References===
# [http://dmd.aspetjournals.org/content/36/4/769.full Absorption, Metabolism, and Excretion of Paliperidone, a New Monoaminergic Antagonist, in Humans]
# [http://dmd.aspetjournals.org/content/36/4/769.full Absorption, Metabolism, and Excretion of Paliperidone, a New Monoaminergic Antagonist, in Humans]
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# [http://en.wikipedia.org/wiki/Beta-glucuronidase Wikipedia page on Beta-glucuronidase]
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# [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3321271/ The Oxidative Stress May be Induced by the Elevated Homocysteine in Schizophrenic Patients]
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# [http://www.omicsonline.org/2161-1459/2161-1459-3-117.php?aid=11374 The Pharmacological Role and Clinical Applications of Antipsychotics’ Active Metabolites: Paliperidone versus Risperidone]
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===Did you know?===
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<blockquote>
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The secret of education lies in respecting the pupil. - Ralph Waldo Emerson
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</blockquote>

Current revision

Contents

Synopsis

So you have been forced by a foolish human-android to acknowledge the insanity of this so-called society ? Don't worry, bud, we'll work something out as always :)

Objectives

The purposes and aims of this experiment are two folds: First, we want you to avoid being mentally harmed while being forced to take antipsychotics drugs. Second, we want you to find a way to functionalize the degradation of the psychoactive compound into a non-psychoactive, and safe racemase.

Design philosophy

  • broad spectrum specificity : The degradation of the optically-active racemate must accept many substrates. (ie: pines and dones)
  • Fast, safe, and side-effects free bioremoval of the metabolite.

One Step Transamination and Degradation of Paliperidone to PLP

  • Approach 1: racemization of paliperidone to 5'-pyridoxal phosphate (PLP) via MTRR(ATP) synthase, a B-glucuronide (B-galactosidase) analog. This is an experimental method to neutralize the active metabolite to a more safe mono-aminase, which should hopefully provide a wet blanket for glutamate-induced neurotoxicity.

Starting Material

  • paliperidone: an atypical antipsychotic derived from Risperidone. see Risperidone.
  • isocitrate (citric acid precursor) : refer to "Citric acid cycle" (ascorbic acid)
  • delta9-tetrahydrocannabinol : competitive GABA antagonist (inhibitor)
  • l-methionine: from eggs (ie: 1 full egg)

Glossary

  • racemate:
  • racemase:
  • racemization: "The production of a racemate from a chiral starting material in which one enantiomer is present in excess." (see Racemate)
  • ketoacidosis:
  • reagent:
  • methylation:
  • glucuronide:
  • amide:
  • ester:
  • transaminase:
  • transaldimination:
  • palmitate: Salt/ester of palmitic acid - a saturated fatty acid (reference: wikipedia)

Notes

References

  1. Absorption, Metabolism, and Excretion of Paliperidone, a New Monoaminergic Antagonist, in Humans
  2. The Oxidative Stress May be Induced by the Elevated Homocysteine in Schizophrenic Patients
  3. The Pharmacological Role and Clinical Applications of Antipsychotics’ Active Metabolites: Paliperidone versus Risperidone

Did you know?

The secret of education lies in respecting the pupil. - Ralph Waldo Emerson
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