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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 [log in to unmask]