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Molecular Aspect of Opioid Receptors

1997; Springer Science+Business Media; Linguagem: Inglês

10.1007/978-3-642-60777-6_11

1865-0325

Brigitte L. Kieffer,

Pharmacological Receptor Mechanisms and Effects

Opiates, the prototype of which is morphine, are the most potent available analgesic compounds. They also are strong addictive drugs. Opiates act by mimicking endogenous opioid peptides and specifically activate membrane receptors of the nervous system. The receptors, named opioid receptors, were first discovered in 1973 with the demonstration of stereospecific and saturable binding of radiolabelled opiates to brain membrane preparations (Pert and Snyder 1973; Simon et al. 1973; Terenius 1973). Study of the pharmacological activity of a wide variety of alkaloid compounds and the discovery of enkephalins (Hughes et al. 1975) led to the classification of opioid binding sites into three classes referred to as μ, δ and κ (see Goldstein and Naidu 1989). Autoradiography showed a distinct distribution for each receptor class in brain (Mansour et al. 1987) and evidence has accumulated for a differential role of the three receptors in pain modulation (see Dickenson 1991). μ, δ and κ specific agonists have also been associated with variable abuse liability and distinct mood-altering, autonomic and neuroendocrine effects have been shown mediated by each receptor type (Milan 1990). More recently the availability of novel synthetic opiates and their use in biological assays have highlighted a possible heterogeneity within each receptor class.