On  6 Mar 00 at 9:14, Leo Fuhr wrote:

> Larry,  What drug are you receiving via the Transdermal Patch?  Do you have
> to be monitored daily, weekly or bi-weekly in Phase II trials?
>
> Jeanette Fuhr 49/47/44?
>
Hi again Jeanette,
Sorry, I mislead you a tad about the archives.... Brian Collins and I discussed
it offlist...
But it wasn't a secret or personal or nuthin'... so here is a copy....

Hi Brian and all others...
Here is the web site for the clinical study...
http://clinicalstudies.info.nih.gov/detail/A_99-N-0104.html
*******************************************************
On 17 Feb 00 at 13:56, Brian Collins wrote:

> I am sorry to be the bearer of bad news, but the excitement at the news
> of imminent release of Dopamine patches is a little premature. The last
> time that I checked up on this subject the outcome was as follows:
>
> 1/ Dopamine patches would not work, because the Dopamine would be
> attacked and destroyed before it could travel from the patch to the
> brain.
>
> 2/ A levodopa patch would take care of the destruction while the chemical
> was in transit, but there is another factor which over-rides points 1
> and 2. That is:
>
> 3/ Levodopa and Dopamine are such large molecules, and we need it in such
> large quantities, that I doubt if you could could get the flow rate
> required even if you used a full body patch!! (What an apalling thought)
>
> 4/ I think you will find, it you scan the press releases which have been
> issued from time to time the magic word 'agonist' lurking quietly in
> the release.
>
> I can't help wondering what is the point of a Dopamine Agonist patch,
> when the dopamine agonist tablets have such a long half-life that in
> the case of Cabergoline for instance you only take one per day anyway!!
> Regards
>
> --
> Brian Collins  <[log in to unmask]>  (60/39/34)
>


On 20 Feb 00 at 19:54, Brian Collins wrote:

> Thanks Murray for pointing out the Web Site; so it is indeed a Dopamine
> Agonist that the study is using. It seems to be a new agonist though,
> since it is referred to only as N-0923.
>
> I would like to know :  How much is known about N-0923 ?
>                         What is its half-life?
>                         Is it useable only in patch form?
>                         Any known side-effects?
>

Hi Brian,
You can pose these questions via e-mail at:
http://clinicalstudies.info.nih.gov/cgi/protmail.cgi?PRPL+99-N-0104

Let us all know what you find out..... murray

...And I looked too...

Hi Brian,
I didn't find out much of any substance but it was an interesting exercise

Search results of N-0923

http://www.farm.rug.nl/cor/medchem/mc.html
Hhmmmmm... since the eighties....

http://www.mtdesk.com/n.shtml
http://www.pjbpubs.com/scriprep/867.html
http://www.nwpf.org/news/item990522a.html
http://www.prous.es/mom/jun_96/mom.html

UBC right here in Vancouver......
http://www.medicine.ubc.ca/AnnualReport97/grants_3of4_.shtml
Scroll down to ...
Neurology    Tsui, Joseph    Clinical   Cato Research Ltd.
A randomized, parallel, double-blind, placebo-controlled study of N-0923 TDS in patients with
Parkinson's disease

PMID- 0010415147
August 1999
DOMINO EF, Ni L, Zhang H.
Nicotine alone and in combination with L-DOPA methyl ester or the D(2) agonist
N-0923 in MPTP-induced chronic hemiparkinsonian monkeys.
Exp Neurol 1999;158:414-21.
http://www.amedeo.com/medicine/pd/expneuro.htm

Dopamine Receptors and Reinforcement:
Dr. James Belluzzi (University of California, Irvine) has been investigating the
involvement of different dopamine receptor subtypes in the mediation of
reinforcement  (primary vs. conditioned vs. classical). Using a series of D1
(SKF 82958, SCH 23390) D2 (N-0923, [+]-PHNO, pergolide) and D3 compound
 (7-OH-DPAT, PD-128,907), Dr. Belluzzi has concluded that cocaine-like
self-administration is most closely mimicked by D1 agonists and that D1
receptors have a primary role in cocaine place preference and classical
conditioning phenomena.
http://www.nida.nih.gov/DirReports/DirRep995/DirectorReport1.html


Calabrese V et al; Mov Disord 1998; 13: 768-774
The novel soluble D2 agonist N-0923 given intravenously to nine Parkinson's
subjects was fast-acting, and fast-fading, suggesting use as an oral medication
would be impractical. It was well-tolerated in therapeutic amounts, although
higher dosage caused nausea and vomiting.
http://www.parkinsonsdisease.com/lwp/CSR/SR11_98.htm

On 20 Feb 00 at 19:54, Brian Collins wrote:

> Thanks Murray for pointing out the Web Site; so it is indeed a Dopamine
> Agonist that the study is using. It seems to be a new agonist though,
> since it is referred to only as N-0923.

Apparently not new....
http://www.farm.rug.nl/cor/medchem/mc.html
Hhmmmmm... since the eighties....

> I would like to know :  How much is known about N-0923 ?

A number of studies spanning more than a decade?  Suggests they must
know more than a little?

>                        What is its half-life?
>                      Is it useable only in patch form?
>                        Any known side-effects?

Calabrese V et al; Mov Disord 1998; 13: 768-774
The novel soluble D2 agonist N-0923 given intravenously to nine Parkinson's
subjects was fast-acting, and fast-fading, suggesting use as an oral medication
would be impractical. It was well-tolerated in therapeutic amounts, although
higher dosage caused nausea and vomiting.
http://www.parkinsonsdisease.com/lwp/CSR/SR11_98.htm

The above suggests a short half life, impractical except as a patch, with
known side effects of nausea and vomiting...

BTW, I found this site bookmarkable...
http://www.mtdesk.com/

cheers .......... murray

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