Function
It has long been understood that κ-opioid receptor agonists are dysphoric but dysphoria from κ-opioid receptor agonists has been shown to differ between the sexes. More recent studies have shown the aversive properties in a variety of ways and the κ-opioid receptor has been strongly implicated as an integral neurochemical component of addiction and the remission thereof.
It is now widely accepted that κ-opioid receptor (partial) agonists have dissociative and deliriant effects, as exemplified by salvinorin A. These effects are generally undesirable in medicinal drugs and could have had frightening or disturbing effects in the tested humans. It is thought that the hallucinogenic effects of drugs such as butorphanol, nalbuphine, and pentazocine serve to limit their opiate abuse potential. In the case of salvinorin A, a structurally novel neoclerodane diterpene κ-opioid receptor agonist, these hallucinogenic, more specifically deliriant and dissociative, effects are sought after, even though the experience is often considered dysphoric by the user. While salvinorin A is considered a hallucinogen, it is not a psychedelic, and its effects are qualitatively different than those produced by the classical psychedelic hallucinogens such as LSD or mescaline.
The involvement of the κ-opioid receptor in stress response has been elucidated.
Activation of the κ-opioid receptor appears to antagonize many of the effects of the μ-opioid receptor.
κ-Opioid receptor ligands are also known for their characteristic diuretic effects, due to their negative regulation of antidiuretic hormone (ADH).
κ-Opioid agonism is neuroprotective against hypoxia/ischemia; as such, κ-opioid receptors may represent a novel therapeutic target.
Read more about this topic: Kappa Opioid Receptor
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—Frank Smith (b. 1928)
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—George Bernard Shaw (1856–1950)