Annual Reports in Medicinal Chemistry, Vol. 39 by Annette M. Doherty

By Annette M. Doherty

Annual reviews in Medicinal Chemistry keeps to target supplying well timed and important reports of significant subject matters in medicinal chemistry including an emphasis on rising subject matters within the organic sciences, that are anticipated to supply the root for totally new destiny remedies. Sections I-IV are disorder oriented and customarily file on particular medicinal brokers. Sections V and VI proceed to stress very important subject matters in medicinal chemistry, biology, and drug layout. * Annual complete studies of the earlier yr literature in lots of issues of curiosity to medicinal chemists * incorporates a accomplished set of indices to simply find issues in Volumes 1-38 of this sequence * presents severe evaluation on sizzling issues in medicinal chemistry

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Pharm. , 2003, 18, 297. [59] D. J. Davies, R. Faust, P. J. Garratt, C. Marivingt-Mounir, K. -T. Teh and D. Sugden, Bioorg. , 2004, 32, 1. [60] J. Csontos, M. Kalman and G. Tasi, Theochem J. Mol. , 2003, 640, 69. [61] J. Csontos, M. Kalman and G. Tasi, Theochem J. Mol. , 2003, 666– 667, 515. [62] S. Rivara, M. Mor, C. Silva, V. Zuliani, F. Vacondio, G. Spadoni, A. Bedini, G. Tarzia, V. Lucini, M. Pannacci, F. Fraschini and P. V. Plazzi, J. Med. , 2003, 46, 1429. [63] M. Bourin, E. Mocaer and R. Porsolt, J.

Oxenkrug and P. , 2003, 8, 139. V. S. Nedzvetsky, P. A. Nerush and S. V. Kirichenko, Neurophysiology, 2003, 35, 422. E. H. Sharman, K. G. -W. Ge, D. K. Lahiri and S. C. Bondy, J. , 2004, 36, 165. P. K. Zahn, T. Lansmann, E. -J. Speckmann and U. Musshoff, J. , 2003, 35, 24. M. I. Masana, S. Doolen, C. Ersahin, W. M. Al-ghoul, S. P. Duckles, M. L. Dubocovich and D. N. Krause, J. Pharmacol. Exp. , 2002, 302, 1295. C. Rodriguez, J. C. Mayo, R. M. Sainz, I. Antolin, F. Herrera, V. Martin and R. J. Reiter, J.

Agomelatine and derivatives Agomelatine 7 is a potent agonist at melatoninergic receptors. It shows a high affinity for cloned human melatonin receptor MT1 and MT2 sub-types (Ki ¼ 61 and 268 pM, respectively). The affinity of agomelatine at melatonin receptors is comparable to that of melatonin (Ki ¼ 85 and 263 pM, respectively). Agomelatine also shows affinity (IC50 ¼ 270 nM) for human cloned serotonin-2C (5-HT2C) receptors, and acts as an antagonist at this receptor subtype [63]. g. the rat forced swim test (FST) [63] and the rat chronic mild stress model of depression [64] Researchers have suggested that the antidepressant-like activity of agomelatine depends on some combination of its melatonin agonist and 5-HT2C antagonist properties.

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