Table of Contents

April 2007; 7 (2)

Speaking of Pharmacology

Reflections

    • Stanley Scheindlin

    Medicine in the Days of the Caliphs

    Mol Interv April 2007 7:59-64; doi:10.1124/mi.7.2.2

Nascent Transcripts

  • Emerging concepts from the recent literature

    Mol Interv April 2007 7:65; doi:10.1124/mi.7.2.3

Significant Deciles

  • ASPET celebrates its centennial anniversary: 1900–1910

    Mol Interv April 2007 7:66-67; doi:10.1124/mi.7.2.4

Viewpoints

    • John K. Amory

    Inhibiting Sperm Motility for Male Contraception: Will the Sperm Tail Be its “Achilles Heel”?

    Mol Interv April 2007 7:68-70; doi:10.1124/mi.7.2.5

    Blocking sperm motility has great appeal as a male contraceptive. A drug that targets sperm motility might have a very rapid onset of action, possibly allowing for administration immediately prior to intercourse and minimizing concerns about compliance. Promising sperm motility targets include transmembrane calcium channels, a unique adenylyl cyclase, and novel flagellar proteins. Future efforts directed towards effectively antagonizing the activities of these or other such targets will be required to completely impair sperm production, function, or both and create a usable male “pill.”

    • Val J. Watts

    Adenylyl Cyclase Isoforms as Novel Therapeutic Targets: An Exciting Example of Excitotoxicity Neuroprotection

    Mol Interv April 2007 7:70-73; doi:10.1124/mi.7.2.6

    The use of transgenic animals lacking one or multiple adenylyl cyclase (AC) isoforms has provided significant information on the roles of AC-dependent signaling in the central nervous system. A recent study provides evidence that AC type 1 (AC1) might be important in glutamate-induced neuronal toxicity. However, the absolute AC specificity revealed in this study contrasts earlier work examining other forms of neurodegeneration. Nonetheless, these observations suggest that specific AC isoforms may represent novel targets for the treatment of central nervous system disorders. It is anticipated that such findings will help catalyze new drug discovery efforts to identify small-molecule modulators of individual AC isoforms.

    • Mary Jeanne Kreek and
    • K. Steven LaForge

    Stress Responsivity, Addiction, and a Functional Variant of the Human Mu-Opioid Receptor Gene

    Mol Interv April 2007 7:74-78; doi:10.1124/mi.7.2.7

    Discovery and characterization of the functional A118G mu-(μ)-opioid receptor variant led to hypotheses, now in part proven, about its role in alterations of endogenous human physiology and in responses to opioid antagonist administration. Differences in cellular expression levels, ligand binding, and signal transduction for variant receptors have been documented in vitro. Human genetic studies also indicate that individuals carrying one or two copies of the 118G allele may have increased risk for opiate and alcohol addictions and that this polymorphism may also explain some of the variability in success of opioid antagonist treatment for alcoholism. Future research will further define the role of the A118G variant in addictive diseases and their treatment, in pain perception and opioid analgesia, and for a myriad of other responses mediated by the μ-opioid receptor.

Reviews

    • Karl-Erik Andersson and
    • George J. Christ

    REGENERATIVE PHARMACOLOGY: THE FUTURE IS NOW

    Mol Interv April 2007 7:79-86; doi:10.1124/mi.7.2.8

    The idea of regenerative medicine has been with us for so long that the concept has been relegated to mythology (think of Prometheus) or to the wildly creative (think of Walt Disney). But the reality is that regenerative biomedicine has begun to show great promise in the laboratory and clinic, and the field may well be poised to revolutionize worldwide healthcare. Cells cultured from the failing organs of patients can be conditioned in “bio-reactors” and grown on scaffolds to take on shapes that recapitulate functional organs. “Neo-organs” constructed in this way represent fully immunocompatible resources for organ implants, and encouraging clinical results with “neobladders” and tissue-engineered vasculature are established in the literature. The demands and opportunities that regenerative medicine places on pharmacology are enormous, from experimental systems on which to test bioactive agents, to the characterization of neo-organs for use in medicine and research.

    • R. Kyle Palmer

    The Pharmacology and Signaling of Bitter, Sweet, and Umami Taste Sensing

    Mol Interv April 2007 7:87-98; doi:10.1124/mi.7.2.9

    Many of the molecular components of the signal transduction pathways underlying taste have been elucidated. In taste buds, the chemosensory receptors for bitter, sweet, and umami (i.e., savory) tastes now are known to be G protein–coupled receptors, whereas salty and sour tastes result from tastant-activation of ion channels. The sense of taste has been investigated for many years using the methods of psychophysics and neurophysiology, and several excellent animal-based taste models are in use. New methods now are being developed for evaluating taste signaling in isolated taste bud and taste cells, and in cells that heterologously express taste receptors and other taste-specific signal transduction proteins.

    • Vanja Petrovic,
    • Shirley Teng,
    • and Micheline Piquette-Miller

    REGULATION OF DRUG TRANSPORTERS: DURING INFECTION AND INFLAMMATION

    Mol Interv April 2007 7:99-111; doi:10.1124/mi.7.2.10

    Membrane transporters play an important role in determining the absorption and activity of many drugs. Intriguingly, inflammation alters the expression and activity of many drug transporters and thereby affects drug absorption and efficacy. The effects of inflammatory conditions on drug transporter regulation and a possible link between differences in drug disposition and inflammation are discussed.

Beyond the Bench

    • Christie Carrico

    Telescopic Hindsight

    Mol Interv April 2007 7:112-113; doi:10.1124/mi.7.2.11

Net Results

Outliers

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This Issue

April 2007; 7 (2)
Cover
  1. Speaking of Pharmacology
  2. Reflections
  3. Nascent Transcripts
  4. Significant Deciles
  5. Viewpoints
  6. Reviews
  7. Beyond the Bench
  8. Net Results
  9. Outliers

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