Mu-opioid receptor: nootropics and compounds | sci-wiki

Dermorphin

Dermorphin is a naturally occurring opioid peptide, a chain of seven amino acids first isolated from the skin of South American frogs of the genus Phyllomedusa. It is among the most potent and selective mu-opioid agonists known, reported to be many times stronger than morphine, and it is one of very few peptides made by a vertebrate to contain a D-amino acid, a D-alanine residue installed by post-translational epimerization that is essential to its potency and its resistance to protease breakdown. Dermorphin is not an approved medicine; it is used in research and is known for its illicit use as a doping agent in horse racing.

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Cannabinoid

Rimonabant

The first CB1 cannabinoid-receptor blocker; a withdrawn anti-obesity drug (Acomplia) that curbed appetite and cleaned up metabolic markers, but was pulled worldwide for serious psychiatric risk.

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Opioid

SR-17018

SR-17018 is an experimental synthetic opioid; a G-protein-biased partial agonist of the mu-opioid receptor studied for pain relief and opioid withdrawal, not approved for human medical use.

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Opioid

Morphine

Morphine is a potent opioid analgesic and the principal alkaloid of opium, the dried latex of the opium poppy (Papaver somniferum). It relieves moderate to severe pain by activating opioid receptors in the brain and spinal cord, and it has been a mainstay of pain medicine since it was first isolated in the early nineteenth century. A controlled substance on the World Health Organization's list of essential medicines, morphine is highly effective but carries substantial risks of dependence, addiction and potentially fatal respiratory depression.

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Opioid

Codeine

Codeine is an opioid medication and a naturally occurring alkaloid found in the opium poppy, used to relieve mild to moderate pain, to suppress coughing and to treat diarrhoea [1]. It is a prodrug: the body converts a portion of it into morphine, which produces most of its pain-relieving effect by acting on mu-opioid receptors [1][3]. First isolated in 1832, it remains one of the most widely used opioids and appears on the World Health Organization's list of essential medicines, but it is a controlled substance with real risks of dependence and, in some people, dangerous sensitivity [1][2].

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Opioid

Oxycodone

Oxycodone is a semi-synthetic opioid analgesic used to treat moderate to severe pain. Derived from the opium alkaloid thebaine and first synthesized in 1916, it acts on the mu-opioid receptor to relieve pain but carries a high potential for tolerance, dependence, and misuse. It is a controlled substance in most countries and is available in immediate-release and controlled-release forms, sometimes combined with non-opioid analgesics.

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Opioid

Hydrocodone

Hydrocodone is a semisynthetic opioid derived from the naturally occurring alkaloids codeine and thebaine, used medically to relieve moderate to severe pain and to suppress cough. It is most often taken by mouth, frequently combined with a non-opioid analgesic such as acetaminophen or ibuprofen in products like Vicodin and Norco. Like other opioids it carries a substantial risk of dependence, addiction, and life-threatening respiratory depression, and it is tightly controlled as a scheduled substance.

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Opioid

Fentanyl

Fentanyl is a powerful synthetic opioid used medically for anesthesia and for severe pain, including breakthrough cancer pain. It acts on mu-opioid receptors in the nervous system and is estimated to be roughly 50 to 100 times more potent than morphine. In recent years, illicitly manufactured fentanyl has become a leading cause of drug overdose deaths.

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Opioid

Tramadol

Tramadol is a centrally acting opioid analgesic used to treat moderate to moderately severe pain, set apart from typical opioids by a dual mechanism [1][2]. In addition to weakly activating the mu-opioid receptor, it inhibits the reuptake of the neurotransmitters serotonin and norepinephrine, so it also behaves somewhat like an antidepressant [2]. First marketed in the late 1970s and sold under names such as Ultram, it is a scheduled controlled substance in many countries.

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Opioid

Heroin

Heroin (diacetylmorphine, or diamorphine in medicine) is a fast-acting semisynthetic opioid made by acetylating morphine. It is a prodrug; the body strips the acetyl groups off to release 6-monoacetylmorphine and morphine, which switch on mu-opioid receptors to produce pain relief, a rush of euphoria, and dangerous slowing of breathing.

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Opioid

Buprenorphine

Buprenorphine is a semisynthetic opioid that acts as a partial agonist at the mu-opioid receptor. It is widely used to treat opioid use disorder and is also used for acute and chronic pain. First developed in the 1960s from the poppy alkaloid thebaine, it is often combined with naloxone in formulations intended to discourage misuse.

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Opioid

Methadone

Methadone is a synthetic opioid medication that acts mainly as an agonist at the mu-opioid receptor, with additional activity as an antagonist at the NMDA glutamate receptor. It is used both to treat opioid use disorder, where long-acting daily doses prevent withdrawal and reduce cravings, and to manage chronic and cancer pain. First synthesized in Germany in the late 1930s, methadone is distinguished among opioids by its long and variable duration of action, and it is listed as an essential medicine by the World Health Organization.

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