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Parkinson's Disease: Join a NIH Fipamezole experimental drug study. Call 800-411-1222. SOURCE: Maryland Gazette Newspapers, MD http://www.gazette.net/200416/princegeorgescty/healthyliving/211982-1.html * * * WHO assigned FIPAMEZOLE as the International Non-proprietary Name for JP-1730, Juvantia’s clinical drug candidate for Parkinson’s disease World Health Organisation (WHO) announced that the Expert Advisory Panel on the International Pharmacopoeia and Pharmaceuticals Preparations selected fipamezole as the International Non-proprietary name for Juvantia’s clinical drug candidate, JP-1730. Juvantia is currently conducting Phase II clinical study with fipamezole for patients with advanced Parkinson’s disease at the National Institutes of Health (NIH) in Bethesda, Maryland, USA. http://www.juvantia.com/eng/news/newsarchive/?nid=8 * * * Fipamezole (JP-1730) is a potent alpha2 adrenergic receptor antagonist that reduces levodopa-induced dyskinesia in the MPTP-lesioned primate model of Parkinson's disease. Savola JM, Hill M, Engstrom M, Merivuori H, Wurster S, McGuire SG, Fox SH, Crossman AR, Brotchie JM. Juvantia Pharma Ltd., PharmaCity, Turku, Finland. Previous studies in the MPTP-lesioned primate model of Parkinson's disease have demonstrated that alpha(2) adrenergic receptor antagonists such as idazoxan, rauwolscine, and yohimbine can alleviate L-dopa-induced dyskinesia and, in the case of idazoxan, enhance the duration of anti-parkinsonian action of L-dopa. Here we describe a novel alpha(2) antagonist, fipamezole (JP-1730), which has high affinity at human alpha(2A) (K(i), 9.2 nM), alpha(2B) (17 nM), and alpha(2C) (55 nM) receptors. In functional assays, the potent antagonist properties of JP-1730 were demonstrated by its ability to reduce adrenaline-induced (35)S-GTPgammaS binding with K(B) values of 8.4 nM, 16 nM, 4.7 nM at human alpha(2A), alpha(2B), and alpha(2C) receptors, respectively. Assessment of the ability of JP-1730 to bind to a range of 30 other binding sites showed that JP-1730 also had moderate affinity at histamine H1 and H3 receptors and the serotonin (5-HT) transporter (IC(50) 100 nM to 1 microM). In the MPTP-lesioned marmoset, JP-1730 (10 mg/kg) significantly reduced L-dopa-induced dyskinesia without compromising the anti-parkinsonian action of L-dopa. The duration of action of the combination of L-dopa and JP-1730 (10 mg/kg) was 66% greater than that of L-dopa alone. These data suggest that JP-1730 is a potent alpha(2) adrenergic receptor antagonist with potential as an anti-dyskinetic agent in the treatment of Parkinson's disease. Copyright 2003 Movement Disorder Society PMID: 12889076 [PubMed - indexed for MEDLINE] http://tinyurl.com/yrb8q * * * ---------------------------------------------------------------------- To sign-off Parkinsn send a message to: mailto:[log in to unmask] In the body of the message put: signoff parkinsn