4548 J. Med. Chem. 2009, 52, 4548–4548
Theilheimer’s Synthetic Methods of Organic Chemistry. Volume 73. Edited by Gillian Tozer-Hotchkiss. S. Karger AG, Basel, Switzerland. 2008. xviii þ 428 pp. 16 23 cm. ISBN 978-3-8055-9069-3. $790.00. This second volume of Theilheimer’s Synthetic Methods of Organic Chemistry for 2008 contains abstracts of new synthetic methods and supplementary data from papers published up to June 2008. It also contains the customary “Advice to the User” and “Further Trends and Developments in Synthetic Organic Chemistry 2008” sections in addition to a 19-page index of reviews of synthetic organic chemistry published from May to October 2008 and an extensive 48-page reaction starting material and product index. Jonathan L. Vennerstrom College of Pharmacy University of Nebraska Medical Center Omaha, Nebraska 68198-6025
DOI: 10.1021/jm900901w Published on Web 06/25/2009
The Cannabinoid Receptors. Edited by Patrica H. Reggio. Humana Press, New York. 2009. xiv þ 396 pp. 16 245 cm. ISBN 978-1-58829-712-9. $139.00. The Cannabinoid Receptors arrives as the 18 member of The Receptors series and offers the reader a sophisticated overview of the structure-activity relationship advances realized in the design of cannabinoid (CB) based drugs. The book presents CB receptors in five parts: (I) structure-activity relationships with an emphasis on indoles, pyrazoles, and native derivatives; (II) biology; (III) molecular pharmacology; (IV) physiology; and (V) preclinical and clinical pharmacology. These parts are subdivided into 13 selfstanding and complementary chapters, each with an abstract preceding the authoritative review. The chapters are thoroughly referenced, including the latest primary literature, and the index serves well. A total of 28 authors were contributors. The intended audience includes industry/academic medicinal chemists and pharmacologists who are new to the CB field.
Detailed receptor site theory and signal transduction pathways are explained with the support of modern molecular pharmacology. Such investigations have already resulted in approved CB agonist drugs for the treatment of neuropathic pain, nausea, and weight loss. In addition, the inverse agonist/ antagonist CB drug rimonabant is currently used to treat weight gain. CB1 receptor subtype ligands are addressed in the context of the central nervous system. Various chemotypes are shown to offer promise for pipeline drugs selectively modulating GABA, glutamate, muscarinic, dopamine, or opioid tone for the potential treatment of neurodegenerative diseases, seizure disorders, schizophrenia, neuralgia, or drug abuse. Peripheral CB2 receptor targeting is discussed in terms of therapeutic leads for immunomodulation, inflammation, cancer, osteoporosis, and artherosclerosis. The CB1 endocannabinoid system is explained as functioning in retrograde signal transduction, where the CB lipid products are released postsynaptically for presynaptic downregulation. Rationally designed CB congeners are shown to differentially trigger microconformational changes in the associated presynaptic CB receptor proteins to direct specific coupling with a range of Gprotein isoforms for selective stimulus trafficking. The book conveys the sense that a universal CB pharmacophore may not exist, in part because of the low level of homology between CB1 versus CB2 receptors, as well as the confounds of allosteric modulation. The clinical use of CB based drugs has become mainstream as medical prejudice is shed in the face of an increasingly well elucidated endocannabinoid system. The Cannabinoid Receptors exquisitely details the significant therapeutic advances and future promise of this forerunning area of drug discovery. Kennerly S. Patrick Department of Pharmaceutical and Biomedical Sciences South Carolina College of Pharmacy Medical University of South Carolina Charleston, South Carolina 29425
DOI: 10.1021/jm900606t Published on Web 06/03/2009
