## Abstract Certain aminotetralins are known to be potent dopamine D~2~ receptor agonists. Nβ0923, [β]2β(NβpropylβNβ2βthienylethylamino)β5βhydroxytetralin HCl, recognizes the high and low affinity states of the D~2~ receptor in membranes from bovine caudate with a K~low~ of 79 nM. The selectivity r
N-0923, A novel soluble dopamine D2 agonist in the treatment of parkinsonism
β Scribed by Vincent P. Calabrese; K. Alvin Lloyd; Pasquale Brancazio; Eugene Cefali; Pauline Martin; James Wall Jr.; Dominic Sica
- Publisher
- John Wiley and Sons
- Year
- 1998
- Tongue
- English
- Weight
- 614 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0885-3185
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β¦ Synopsis
N-0923, a novel aminotetralin dopamine D2 agonist, was shown to effectively reverse parkinsonian symptoms in nine dopa/agonist-responsive Parkinson's disease patients. The drug was given up to 4.5 hours by continuous intravenous (i.v.) infusion using an i.v. pump. The onset of anti-parkinsonian effect was seen within minutes of the initiation of the infusion and was absent within 90 minutes of cessation of the infusion. The short elimination half-life of N-0923 (90 min) would allow for the rapid initiation of drug effect when necessary and at the same time permit the effect to be terminated quickly if necessary. The drug would be useful in situations where oral medication is not feasible or is associated with erratic absorption. The patients tolerated the drug well. Dose escalation load was limited by nausea and vomiting. It should be noted that the doses were increased until these symptoms occurred, but therapeutic effects were noted well before the side effects occurred. Using a modified Columbia scale, maximum improvement consisted of a 27-95% drop in score. Maximum response was obtained at infusion rates varying from 2-16 microg/kg per hour and at blood levels of 0.11-1.49 microg/mL.
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## Abstract Nβ0923 is a nonβergot, dopaminergic D~2~ agonist designed to be transdermally available. It has antiβparkinsonian effects when infused intravenously. An adhesive matrix patch was developed to deliver Nβ0923 transdermally (Nβ0923 TDS). In this phase II trial, we evaluated the effectiven
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