Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

• Allison S. Limpert,
• Margrith E. Mattmann and
• Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

• animals [66]. Additional work from this group identified the dopamine D2 receptor agonist, bromocriptine (32), as an NAIP upregulating compound that reduced oxidative stress through the upregulation of antioxidant proteins, such as activating transcription factor 3 (ATF3) and HO-1 [68]. In vivo studies

Development of peptidomimetic ligands of Pro-Leu-Gly-NH₂ as allosteric modulators of the dopamine D₂ receptor

• Swapna Bhagwanth,
• Ram K. Mishra and
• Rodney L. Johnson

Beilstein J. Org. Chem. 2013, 9, 204–214, doi:10.3762/bjoc.9.24

• changes in the spiro-bicyclic dopamine receptor modulators are capable of causing major changes in the modulatory activity of PLG peptidomimetics. Keywords: allosteric modulation; dopamine D2 receptor; peptidomimetic; Pro-Leu-Gly-NH2; spiro-bicyclic scaffold; Review There has been an increasing effort

• neuropeptide Pro-Leu-Gly-NH2 (PLG) has been shown to be a positive allosteric modulator of the dopamine D2 receptor [3]. PLG was initially isolated from brain tissue in the search for hypothalamic releasing factors, wherein it was found to inhibit the release of melanocyte stimulating hormone from the

• peptidomimetics of PLG were used to show that PLG and its peptidomimetics act as allosteric modulators of the dopamine D2 receptor [3][9]. This represents one of the few examples where a known endogenous molecule has demonstrated allosteric receptor-modulating activity, since most allosteric modulators discovered

Intramolecular carbolithiation of N-allyl-ynamides: an efficient entry to 1,4-dihydropyridines and pyridines – application to a formal synthesis of sarizotan

• Wafa Gati,
• Mohamed M. Rammah,
• Mohamed B. Rammah and
• Gwilherm Evano

Beilstein J. Org. Chem. 2012, 8, 2214–2222, doi:10.3762/bjoc.8.250

• of the 3,5-disubstituted pyridine core of the antidyskinetic drug, 5-HT1A receptor agonist, dopamine D2 receptor ligand sarizotan 19 (Scheme 6). The pyridinyl-chroman sarizotan (also called EMD-128130) was originally developed by Merck KGaA in the late 1990’s [44] and was found to be a dual selective

• starting N-allyl-ynamides. Intramolecular carbolithiation of N-allyl-ynamides to 1,4-dihydropyridines and pyridines. 2,3-Disubstituted pyridines by trapping of the intermediate metallated 1,4-dihydropyridine. Formal synthesis of the anti-dyskinesia agent, 5-HT1A receptor agonist, dopamine D2 receptor