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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 5 of 5. This is the beginning of the thread.
Posted by SteelyDan on February 26, 2008, at 14:28:26
Can anybody tell me anything about Pagoclone? Is it helpful for anxiety and depression?
Posted by Phillipa on February 26, 2008, at 15:00:06
In reply to PAGOCLONE, posted by SteelyDan on February 26, 2008, at 14:28:26
Dan trying to help this is wiki. Love Phillipa
Pagoclone
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Jump to: navigation, search
Pagoclone
Systematic (IUPAC) name
2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-
2-oxo-hexyl)-3H-isoindol-1-one
Identifiers
CAS number 133737-32-3
ATC code ?
PubChem 131664
Chemical data
Formula C23H22ClN3O2
Mol. mass 407.893 g/mol
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life ?
Excretion ?
Therapeutic considerations
Pregnancy cat. ?
Legal status
Routes ?
Pagoclone is an anxiolytic drug from the cyclopyrrolone family, which is related to other more well known drugs such as the sleeping medication zopiclone. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures.Pagoclone was originally developed as an anti-anxiety drug, but never commercialised. It is a partial agonist acting at GABAA receptors in the brain. In contrast to zopiclone, pagoclone produces anxiolytic effects with little or no sedative or amnestic actions at low doses.[1] This is because pagoclone is a subtype-selective drug which binds primarily to the α2/α3 subtypes of the GABAA receptor which are responsible for the anti-anxiety effects of these kind of drugs, but has relatively little efficacy at the α1 subtype which produces the sedative and memory loss effects.[2]
David Nutt from the University of Bristol has suggested pagoclone as a possible base from which to make a better social drug, as it produces the positive effects of alcohol, such as relaxation and sociability, but without also causing the negative effects like aggression, amnesia, nausea, loss of coordination and liver damage. Its effect can be quickly reversed by the action of flumazenil, which is already used as an antidote to benzodiazepine overdose.[3]
Dr. Nutt has published studies[4] praising the potential of pagoclone which were financed by Indeveus which holds the patents to the pharmaceutical and is, as of Spring 2006, seeking funding for a possible production of the compound. The significance of this is undetermined, but it should be noted that the long-term safety of pagoclone has not been assessed. The abuse potential of pagoclone has been assessed as being similar to, or slightly less than that of diazepam and it would also be expected to be somewhat safer due to its relatively weaker sedative effects,[5] but development of pagoclone as a recreational drug would still be unlikely due to concerns about abuse.
Pagoclone is also being trialed as a drug to improve a stammerer's speech fluency.[1]
[edit] See also
Bretazenil
Stuttering
Basal ganglia
GABA
Posted by Phillipa on February 26, 2008, at 15:01:08
In reply to PAGOCLONE, posted by SteelyDan on February 26, 2008, at 14:28:26
Dan not the best source sometimes but a start. Love Phillipa
Posted by SteelyDan on February 26, 2008, at 15:12:26
In reply to Re: PAGOCLONE » SteelyDan, posted by Phillipa on February 26, 2008, at 15:00:06
> Dan trying to help this is wiki. Love Phillipa
>
> Pagoclone
> From Wikipedia, the free encyclopedia
> Jump to: navigation, search
>
> Pagoclone
> Systematic (IUPAC) name
> 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-
> 2-oxo-hexyl)-3H-isoindol-1-one
> Identifiers
> CAS number 133737-32-3
> ATC code ?
> PubChem 131664
> Chemical data
> Formula C23H22ClN3O2
> Mol. mass 407.893 g/mol
> Pharmacokinetic data
> Bioavailability ?
> Metabolism ?
> Half life ?
> Excretion ?
> Therapeutic considerations
> Pregnancy cat. ?
>
> Legal status
> Routes ?
> Pagoclone is an anxiolytic drug from the cyclopyrrolone family, which is related to other more well known drugs such as the sleeping medication zopiclone. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures.
>
> Pagoclone was originally developed as an anti-anxiety drug, but never commercialised. It is a partial agonist acting at GABAA receptors in the brain. In contrast to zopiclone, pagoclone produces anxiolytic effects with little or no sedative or amnestic actions at low doses.[1] This is because pagoclone is a subtype-selective drug which binds primarily to the α2/α3 subtypes of the GABAA receptor which are responsible for the anti-anxiety effects of these kind of drugs, but has relatively little efficacy at the α1 subtype which produces the sedative and memory loss effects.[2]
>
> David Nutt from the University of Bristol has suggested pagoclone as a possible base from which to make a better social drug, as it produces the positive effects of alcohol, such as relaxation and sociability, but without also causing the negative effects like aggression, amnesia, nausea, loss of coordination and liver damage. Its effect can be quickly reversed by the action of flumazenil, which is already used as an antidote to benzodiazepine overdose.[3]
>
> Dr. Nutt has published studies[4] praising the potential of pagoclone which were financed by Indeveus which holds the patents to the pharmaceutical and is, as of Spring 2006, seeking funding for a possible production of the compound. The significance of this is undetermined, but it should be noted that the long-term safety of pagoclone has not been assessed. The abuse potential of pagoclone has been assessed as being similar to, or slightly less than that of diazepam and it would also be expected to be somewhat safer due to its relatively weaker sedative effects,[5] but development of pagoclone as a recreational drug would still be unlikely due to concerns about abuse.
>
> Pagoclone is also being trialed as a drug to improve a stammerer's speech fluency.[1]
>
>
> [edit] See also
> Bretazenil
> Stuttering
> Basal ganglia
> GABAGreat info! Thank you so much Phillipa.
-Dan
Posted by Dopamine123 on February 27, 2008, at 13:54:43
In reply to Re: PAGOCLONE, posted by SteelyDan on February 26, 2008, at 15:12:26
http://www.stammering.org/pagoclone.html
As far as the author is aware, pagoclone was never commercially available, nor has it ever succeeded in a phase III trial, and knowledge about side effects from phase IV trials is non-existent. Though pagoclone was initially studied for anxiety disorders in larger trials by Pfizer, Inc., Pfizer is said to have "discontinued development of the compound in June 2002" (7). The only phase III trial initiated by Pfizer, Inc., in August 2000 for panic disorder (7) was not available on the Medline (8) as of July 16, 2006, which suggests that it has been stopped."It hasn't been FDA approved. So you can't get it from a doctor.
My blog:
http://brainstimulant.blogspot.com
This is the end of the thread.
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