PMID: 11607045Oct 19, 2001Paper

Adrogolide HCl (ABT-431; DAS-431), a prodrug of the dopamine D1 receptor agonist, A-86929: preclinical pharmacology and clinical data

CNS Drug Reviews
W J Giardina, M Williams

Abstract

Adrogolide (ABT-431; DAS-431) is a chemically stable prodrug that is converted rapidly (<1 min) in plasma to A-86929, a full agonist at dopamine D1 receptors. In in vitro functional assays, A-86929 is over 400 times more selective for dopamine D1 than D2 receptors. In rats with a unilateral loss of striatal dopamine, A-86929 produces contralateral rotations that are inhibited by dopamine D1 but not by dopamine D2 receptor antagonists. Adrogolide improves behavioral disability and locomotor activity scores in MPTP-lesioned marmosets, a model of Parkinson's disease (PD), and shows no tolerance upon repeated dosing for 28 days. In PD patients, intravenous (i.v.) adrogolide has antiparkinson efficacy equivalent to that of L-DOPA with a tendency towards a reduced liability to induce dyskinesia. The adverse events associated with its use were of mild-to-moderate severity and included injection site reaction, asthenia, headache, nausea, vomiting, postural hypotension, vasodilitation, and dizziness. Adrogolide can also attenuate the ability of cocaine to induce cocaine-seeking behavior and does not itself induce cocaine-seeking behavior in a rodent model of cocaine craving and relapse. In human cocaine abusers, i.v. adrogolide reduces ...Continue Reading

References

Jun 12, 1992·Brain Research·D W Self, L Stein
Dec 15, 1992·European Journal of Pharmacology·J W KebabianM Williams
Nov 1, 1992·British Journal of Addiction·H R Kranzler, L O Bauer
Jan 1, 1989·Movement Disorders : Official Journal of the Movement Disorder Society·J A TemlettX Lataste
Jan 1, 1987·Journal of Neural Transmission·A BraunT N Chase
Jan 1, 1993·Annual Review of Neuroscience·J A Gingrich, M G Caron
Jan 1, 1993·Annual Review of Medicine·M Stacy, J Jankovic
Oct 23, 1998·Annals of Medicine·D W Self
Jun 9, 1999·Annals of Neurology·O RascolJ G Nutt
Jun 12, 1999·The American Journal on Addictions·F R LevinE V Nunes
Nov 24, 1999·International Journal of Pharmaceutics·Y ZhengA L Adjei
Jul 27, 2000·Annals of the New York Academy of Sciences·D W SelfJ J Spencer

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Citations

Feb 24, 2006·NeuroRx : the Journal of the American Society for Experimental NeuroTherapeutics·José A Apud, Daniel R Weinberger
May 19, 2007·Addiction Biology·Antonio Preti
Aug 16, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Dieter SchellerHermann Lübbert
Jan 18, 2005·CNS Drugs·Mehmet Sofuoglu, Thomas R Kosten
Feb 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Antonio Di StefanoLaura Serafina Cerasa
Jul 31, 2014·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Daniel R RosellLarry J Siever
Dec 12, 2013·Biomarkers in Medicine·Brett A EnglishLarry Ereshefsky
Sep 26, 2019·Current Topics in Medicinal Chemistry·Daniel E FelsingJohn A Allen
Aug 2, 2002·Current Opinion in Neurology·Ron Tintner, Joseph Jankovic
Apr 13, 2012·Expert Opinion on Drug Discovery·Piera SozioAntonio Di Stefano
Jul 6, 2004·Drugs·David A GorelickZheng-Xiong Xi
Feb 16, 2011·Chemical Communications : Chem Comm·Saumen Hajra, Sukanta Bar
Sep 5, 2002·Nature Reviews. Drug Discovery·Philippe Pouletty
Jun 19, 2017·Neuroscience and Biobehavioral Reviews·Daniel MartinsDiana Prata
Aug 24, 2021·Schizophrenia Bulletin·Anissa Abi-DarghamJeffrey Lieberman

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