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Mu-opioid agonists


Analgesics (168)
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ALFENTANIL (71195-58-9)  
Alfentanil (R-39209, trade name Alfenta, Rapifen in Australia) is a potent but short-acting synthetic opioid analgesic drug, used for anaesthesia in surgery. It is an analogue of fentanyl with around 1/4 to 1/10 the potency of fentanyl and around 1/3 of the duration of action, but with an onset of effects 4x faster than fentanyl. Alfentanil has a pKa of approximately 6.5, which leads to a very high proportion of the drug being uncharged at physiologic pH.
ANILERIDINE (144-14-9)  
Anileridine (trade name: Leritine) is a synthetic analgesic drug and is a member of the piperidine class of analgesic agents developed by Merck & Co. in the 1950s. It differs from pethidine (meperidine) in that the N-methyl group of meperidine is replaced by an N-aminophenethyl group, which increases its analgesic activity.
Desomorphine (427-00-9)  
Desomorphine is a synthetic opioid developed by Roche. With powerful, fast-acting effects, such as sedation and analgesia. First synthesized in 1932 and patented in 1934 in the United States, desomorphine was used in Switzerland under the brand name Permonid and was described as having a fast onset and a short duration of action, with relatively little nausea compared to equivalent doses of morphine.
Ketobemidone (469-79-4)  
cetobemidon  ·  1-(4-(m-hydroxyphenyl)-1-methyl-4-piperidyl)-1-propanone  ·  ketobemidone hydrochloride
Ketobemidone, sold under the brand name Ketogan among others, is a powerful opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its metabolite norketobemidone. This may make it useful for some types of pain that do not respond well to other opioids.
REMIFENTANIL (132875-61-7)  
Remifentanil is a potent, short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications for use in general anesthesia.
Levomethadyl acetate (1477-40-3)  
Levacetylmethadol (INN), levomethadyl acetate (USAN), OrLAAM (trade name) or levo-α-acetylmethadol (LAAM) is a synthetic opioid similar in structure to methadone. It has a long duration of action due to its active metabolites. It was approved in 1993 by the U.S.
levallorphan (152-02-3)  
Lorfan  ·  Naloxiphan
Levallorphan (INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartrate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia. Levallorphan was formerly widely used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia (via KOR agonism).
Ethylmorphine (76-58-4)  
Dionine  ·  Ethylmorphine, (5alpha,6beta)-Isomer  ·  Ethylmorphine Hydrochloride, (5alpha,6alpha)-Isomer
Ethylmorphine (also known as codethyline, dionine, and ethyl morphine) is an opioid analgesic and antitussive.
Alphaprodin (468-59-7, 77-20-3)  
Alphaprodine  ·  Nisentil  ·  Alphaprodine Hydrochloride
Prodine (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was developed in Germany in the late 1940s. Several 1-alkyl-4-phenyl-4-acyloxypiperidines have been prepared and found to possess significant analgesic action.
ALPHAPRODINE (77-20-3)  
Nisentil  ·  Alphaprodine Hydrochloride  ·  Prodine
Prodine (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was developed in Germany in the late 1940s. Several 1-alkyl-4-phenyl-4-acyloxypiperidines have been prepared and found to possess significant analgesic action.
Dihydromorphine (1421-28-9, 509-60-4)  
Paramorfan  ·  Paramorphan
Levopropoxyphene (2338-37-6)  
Levopropoxyphene is an antitussive. It is an optical isomer of dextropropoxyphene. The racemic mixture is called propoxyphene.
dihydrocodeine bitartrate  ·  Paracodin  ·  DF 118
Dihydrocodeine is a semi-synthetic opioid analgesic prescribed for pain or severe dyspnea, or as an antitussive, either alone or compounded with paracetamol (as in co-dydramol) or aspirin. It was developed in Germany in 1908 and first marketed in 1911. Commonly available as tablets, solutions, elixirs, and other oral forms, dihydrocodeine is also available in some countries as an injectable solution for deep subcutaneous and intra-muscular administration.
Difenoxin (28782-42-5, 35607-36-4)  
diphenoxylic acid  ·  difenoxin hydrochloride  ·  difenoxin hydrochloride, 14C-labeled
Difenoxin (Motofen, R-15403) is an opioid drug used, often in combination with atropine, to treat diarrhea. It is the principal metabolite of diphenoxylate. Difenoxin crosses the blood brain barrier and induces some euphoria; it is often sold with or administered with atropine to reduce the potential for abuse and overdose.
Mefentanyl (42045-86-3)  
3-Methylfentanyl (3-MF, mefentanyl) is an opioid analgesic that is an analog of fentanyl. 3-Methylfentanyl is one of the most potent drugs that has been widely sold on the black market, estimated to be between 400 and 6000 times stronger than morphine, depending on which isomer is used (with the cis isomers being the more potent ones). 3-Methylfentanyl was first discovered in 1974 and subsequently appeared on the street as an alternative to the clandestinely produced fentanyl analog α-methylfentanyl.
CARFENTANIL (59708-52-0)  
Carfentanil or carfentanyl is an analog of the synthetic opioid analgesic fentanyl. A unit of carfentanil is 100 times as potent as the same amount of fentanyl, 5,000 times as potent as a unit of heroin and 10,000 times as potent as a unit of morphine. The toxicity of carfentanil in humans and its ready commercial availability has aroused concerns over its potential use as a weapon of mass destruction by rogue nations and terrorist groups.
Piritramide (302-41-0)  
Dipydolor  ·  Piritramid  ·  Pirinitramide
Piritramide (R-3365, trade names Dipidolor, Piridolan, Pirium and others) is a synthetic opioid analgesic (narcotic painkiller) that is marketed in certain European countries including: Austria, Belgium, Czech Republic, Germany and the Netherlands. It comes in free form, is about 0.75x times as potent as morphine and is given parenterally (by injection) for the treatment of severe pain. Nausea, vomiting, respiratory depression and constipation are believed to be less frequent with piritramide than with morphine (the gold standard opioid against which other opioids are compared and contrasted), and it produces more rapid-onset analgesia (pain relief) when compared to morphine and pethidine.
Methadyl acetate (509-74-0)  
LAAM  ·  Acetylmethadol  ·  Levomethadyl
Acetylmethadol, also known as methadyl acetate, is a synthetic opioid analgesic. It is a racemic mixture of alphacetylmethadol (α-acetylmethadol) and betacetylmethadol (β-acetylmethadol), which are in turn racemic mixtures of levacetylmethadol (LAAM; L-α-acetylmethadol) and D-α-acetylmethadol and L-β-acetylmethadol and D-β-acetylmethadol, respectively. Hence, acetylmethadol has four possible optical isomers.
3-Methylthiofentanyl (86052-04-2)  
3-Methyl-thiofentanyl is an opioid analgesic and analogue of fentanyl. 3-Methyl-thiofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural similarity rather than scheduling each drug individually as they appeared. 3-Methyl-thiofentanyl has similar effects to fentanyl.
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