By Christoph Stein, Christoph Stein

This quantity makes an attempt to summarize the present nation of information on mechanisms underlying a number of the results of analgesics, their part impression profiles, and their symptoms and contraindications in medical use. It additionally provides insights into present efforts to find novel mechanisms underlying the new release of alternative kinds of discomfort and the ensuing improvement of latest modulating compounds.

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3 Opioid Receptor Ligands and Sites of Action . Endogenous Ligands . . . . . . . Exogenous Ligands . . . . . . . . Sites of Action . . . . . . . . . Supraspinal and Spinal Sites . . . . . Peripheral Sites . . . . . . . . . Peripheral Opioid Receptors and Inflammation .

2a). Ion-channel regulation by opioids 38 C. Zöllner · C. Stein is mainly mediated via direct G protein βγ-subunits (Herlitze et al. 1996). All three opioid receptors couple to various N, T-type and P/Q-type Ca2+ channels, suppress Ca2+ influx and subsequently the excitation and/or neurotransmitter release in many neuronal systems. A prominent example is the inhibition of (pronociceptive) substance P release from primary afferent sensory neurons in the spinal cord and from their peripheral terminals (Kondo et al.

49 49 49 49 50 50 51 51 51 52 52 . . . . . . . . . . . . . . . . . . . . . 32 C. Zöllner · C. 2 Chronic Opioid Application . . . . . . . . . . . . . . 1 Tolerance . . . . . . . . . . . . . . . . . . . 2 Physical Dependence . . . . . . . . . . . . . . . . 53 53 54 References . . . . . . . . . . . . . . . . . . . . 54 Abstract Opioids are the most effective and widely used drugs in the treatment of severe pain.

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