Enadoline
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Enadoline is a drug which acts as a highly selective κ-opioid
agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of
salvinorin A Salvinorin A is the main active psychotropic molecule in '' Salvia divinorum''. Salvinorin A is considered an atypical dissociative hallucinogen. It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psil ...
. It was studied as a potential
analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
, but abandoned because of the dose-limiting effects of
dysphoria Dysphoria (; ) is a profound state of unease or dissatisfaction. It is the semantic opposite of euphoria. In a psychiatric context, dysphoria may accompany depression, anxiety, or agitation. In psychiatry Intense states of distress and uneas ...
, which could be expected from a κ-opioid agonist. There was mention of its potential in treating
coma A coma is a deep state of prolonged unconsciousness in which a person cannot be awakened, fails to Nociception, respond normally to Pain, painful stimuli, light, or sound, lacks a normal Circadian rhythm, sleep-wake cycle and does not initiate ...
tose head injury or
stroke Stroke is a medical condition in which poor cerebral circulation, blood flow to a part of the brain causes cell death. There are two main types of stroke: brain ischemia, ischemic, due to lack of blood flow, and intracranial hemorrhage, hemor ...
victims, where that type of side effect would be immaterial.


Potency

When enadoline was first reported in 1990, it was "the most potent κ-selective analgesic ever reported ... 25 times more potent than morphine and 17 times more potent than U-62066".


See also

* U-69,593 * U-50,488 * U-77891 * AH-7921 * Bromadoline


References

Synthetic opioids Dissociative drugs 1-Pyrrolidinyl compounds Kappa-opioid receptor agonists Tetrahydrofurans Acetamides Benzofuranethanamines Spiro compounds Abandoned drugs {{Psychoactive-stub