Novel agonists

There are not yet any agonists that are truly selective for the A2BAR, known as the low affinity adenosine A2 receptor. A novel agonist, the 2-(6-bromotryptophol) ether derivative MRS3997 16, is a full agonist with mixed selectivity at A2a and A2BARs. 

Novel agonist 5HTia receptor position emission tomography (PET) ligands derived form l,2,4-triazine-3,5-dione 19 have been synthesized and evaluated in vivo <06JMC125 06BMCL2101>. 

Burgermeister, E., Schnoebelen, A., Flament, A., Benz, J., Stihle, M., Gsell, B., Rufer, A., Ruf, A., Kuhn, B., Marki, H. P., Mizrahi, J., Sebokova, E., et al. (2006). A novel agonist of peroxiome proliferator-activated receptor-y (PPAR y) recruits PPAR y-coactivator-la, prevents triglyceride accumulation, and potentiates insuling signalling in vitro. Mol. Endocrinol. 20, 809-830. 

Mogg AJ, Jones FA, PuUar lA, Sharpies CG, Wonnacott S (2004) Functional responses and subunit composition of presynaptic nicotinic receptor subtypes explored using the novel agonist 5-iodo-A-85380. Neuropharmacology 47 848-859... 

Fig. 13.4 (continued) (e) This reduction persisted in the presence of the Aj receptor antagonist DPCPX in WT animals (n = 10 mice), in support of the concept that the protective response to this novel agonist is mediated by the A3 but not the Aj receptor, (f) The protective effect of MRS3558 was completely abrogated in PLC(32/(33 null-mice, providing further evidence for the hypothesis that the A3 receptor signals via PLCfS to achieve its cytoprotective effect... 

Deprotonation of indoles 128 followed by alkylation with 2-methyloxirane led to the secondary alcohols 129 that were used as starting compounds in the preparation of substituted 2-(l//-indol-l-yl)-l-methylethylamines 130, novel agonists of 5HT2C receptors. Sn2 reaction of the corresponding mesylates with sodium azide and reduction of the azides with either hydrogen or LiAlH4 produced amines 130 in excellent yields (Scheme 28) <1997JME2762>. 

Bos, M., Jenck, E., Martin, J. R., Moreau, J.-L., Sleight, A. J., Wichmann, J., Widmer, U. Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-l-yl)-l-methylethylamines and 2-(indeno[l,2-h]pyrrol-l-yl)-l-methylethyl-amines. Improved therapeutics for obsessive compulsive disorder. 7. Med. Chem. 1997,40,2762-2769. 

Rayasam GV, Tulasi VK, Sundaram S et al (2010) Identification of berberine as a novel agonist of fatty acid receptor GPR40. Phytother Res 24(8) 1260-1263... 

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