By David J Triggle, John B Taylor (editors)
The 1st variation of finished Medicinal Chemistry was once released in 1990 and was once rather well got. finished Medicinal Chemistry II is far greater than an easy updating of the contents of the 1st variation. thoroughly revised and increased, this new version has been refocused to mirror the numerous advancements and adjustments over the last decade in genomics, proteomics, bioinformatics, combinatorial chemistry, high-throughput screening and pharmacology, and extra. The content material includes the main up to date, authoritative and finished reference textual content on modern medicinal chemistry and drug examine, protecting significant healing sessions and pursuits, learn procedure and enterprise, high-throughput applied sciences, computer-assisted layout, ADME and chosen case histories. it truly is this insurance of the method, applied sciences, ideas and purposes of medicinal chemistry in one paintings that may make complete Medicinal Chemistry II a distinct paintings of reference and a unmarried element of access to the literature for pharmaceutical and biotechnology scientists of all disciplines and for lots of executives as well.Also on hand on-line through ScienceDirect (2006) - that includes large shopping, looking out, and inner cross-referencing among articles within the paintings, plus dynamic linking to magazine articles and summary databases, making navigation versatile and straightforward. for additional information, pricing recommendations and availability stopover at www.info.sciencedirect.com. * Comprehensively experiences - the recommendations, applied sciences, rules and functions of recent medicinal chemistry * offers an international and present standpoint of brand new drug discovery procedure and discusses the key healing periods and objectives* contains a precise choice of case reviews and private assays reviewing the invention and improvement of key medicinal drugs
Read Online or Download Comprehensive Medicinal Chemistry II, Eight-Volume Set, Volume 6 : Therapeutic Areas I: Central Nervous System, Pain, Metabolic Syndrome, Urology, Gastrointestinal and Cardiovascular PDF
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Additional info for Comprehensive Medicinal Chemistry II, Eight-Volume Set, Volume 6 : Therapeutic Areas I: Central Nervous System, Pain, Metabolic Syndrome, Urology, Gastrointestinal and Cardiovascular
Example text
Other partial DA agonists, including terguride 55, have shown antipsychotic efficacy albeit in small clinical trials. At least part of the beneficial effects of aripiperazole 5658 may be related to its partial DA agonist properties. As expected of a partial agonist, this drug acts as an antagonist at the D2 receptors in a state of excessive dopaminergic neurotransmission, while it acts as an agonist at the D2 receptor in a state of low dopaminergic neurotransmission. Aripiperazole, therefore, appears to stabilize dopaminergic neurotransmission.
P. Nat. Rev. Drug Disc. 2005, 4, 1015–1026. ; Linszen, D. Psychopharmacology 2006, 183, 500–505. Martin, L. ; Kem, W. ; Freedman, R. Psychopharmacology 2004, 174, 54–64. ; Meltzer, H. Nat. Rev. Drug Disc. 2005, 4, 967–975. ; Perret, L. Nat. Rev. Drug Disc. 2005, 4, 467–476. Insel, T. ; Scolnick, E. M. Mol. Psychiatry 2006, 11, 11–17. ; Arancio, O. et al. Science 2003, 301, 805–809. Kippin, T. ; Van Der Kooy, D. J. Neurosci. 2005, 25, 5815–5823. Bodick, N. ; Offen, W. ; Levey, A. ; Cutler, N. ; Gauthier, S.
As expected of a partial agonist, this drug acts as an antagonist at the D2 receptors in a state of excessive dopaminergic neurotransmission, while it acts as an agonist at the D2 receptor in a state of low dopaminergic neurotransmission. Aripiperazole, therefore, appears to stabilize dopaminergic neurotransmission. However, aripiperazole also exhibits high affinity for serotonin 5HT1A and 5HT2A receptors, moderate affinity for DA D4, 5HT2c and 5HT7, a1-adrenergic and histamine H1 receptors. Thus, its activity as a partial DA agonist must be viewed against the background of other receptor activities.