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Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Analgesic

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Analgesics (55)
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morphine (64-31-3, 57-27-2)  
Morphia  ·  Morphine Sulfate  ·  MS Contin
Morphine is a pain medication of the opiate variety which is found naturally in a number of plants and animals. It acts directly on the central nervous system (CNS) to decrease the feeling of pain. It can be taken for both acute pain and chronic pain.
Levomethorphan (510-53-2, 125-71-3, 125-70-2)  
Dextromethorphan  ·  Dextromethorphan Hydrobromide  ·  Delsym
Methorphan comes in two isomeric forms, each with differing pharmacology and effects: Dextromethorphan - An over-the-counter cough suppressant, as well as dissociative hallucinogen. Levomethorphan - A potent opioid analgesic that was never clinically developed; the codeine analogue of the powerful opioid agonist analgesic levorphanol (Levo-Dromoran). Racemethorphan refers to the racemic mixture of both of these stereoisomers.
dextromethorphan (510-53-2, 125-71-3, 125-70-2)  
Dextromethorphan Hydrobromide  ·  Delsym  ·  Levomethorphan
Methorphan comes in two isomeric forms, each with differing pharmacology and effects: Dextromethorphan - An over-the-counter cough suppressant, as well as dissociative hallucinogen. Levomethorphan - A potent opioid analgesic that was never clinically developed; the codeine analogue of the powerful opioid agonist analgesic levorphanol (Levo-Dromoran). Racemethorphan refers to the racemic mixture of both of these stereoisomers.
meperidine (57-42-1)  
Demerol  ·  Dolin  ·  Pethidine
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1939 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, Germany. Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines (piminodine, anileridine and others), the prodines (alphaprodine, MPPP, etc.), bemidones (ketobemidone, etc.) and others more distant, including diphenoxylate and analogues.
levorphanol (77-07-6, 297-90-5)  
Levorphanol Tartrate  ·  Levorphan  ·  LevoDromoran
Levorphanol (INN; brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain. It is one of four enantiomers of the compound racemorphan, and was first described in Germany in 1948 as an orally active, morphine-like analgesic. The drug has been in clinical use in the United States since 1953.
Etorphine (14521-96-1)  
M99  ·  Ethorphine
Nalorphine (62-67-9)  
Allylnormorphine  ·  Nalorphine Hydrochloride  ·  Lethidrone
Nalorphine (INN) (brand names Lethidrone, Nalline), also known as N-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence. It acts at two opioid receptors — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM; EC50 = 483 nM; Emax = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics.
butorphanol (42408-82-2, 58786-99-5)  
Stadol  ·  Butorphanol Tartrate  ·  Stadol NS
Butorphanol (BC 2627) is a morphinan-type synthetic agonist–antagonist opioid analgesic developed by Bristol-Myers. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Ben Venue Laboratories.
Salvinorin A (83729-01-5)  
Salvinorin A is the main active psychotropic molecule in Salvia divinorum, a Mexican plant which has a long history of use as an entheogen by indigenous Mazatec shamans. Salvinorin A is considered a dissociative. It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psilocybin, and mescaline) because it contains no nitrogen atoms; hence, it is not an alkaloid (and cannot be rendered as a salt) but a terpenoid.
ENADOLINE (124378-77-4)  
Enadoline is a drug which acts as a highly selective κ-opioid agonist. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist.
nalbuphine (20594-83-6)  
Nubain  ·  Nalbuphine Hydrochloride  ·  EN-2234A
Nalbuphine is a semi-synthetic opioid agonist-antagonist used commercially as an analgesic under a variety of trade names, including Nubain and Manfine.
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).
Diprenorphine (14357-78-9)  
Revivon  ·  Diprenorphine Hydrochloride
Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) that is employed in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans.
DEXTRORPHAN (297-90-5, 125-73-5)  
(+-)-17-Methylmorphinan-3-ol
Dextrorphan (DXO) is a psychoactive drug of the morphinan class which acts as an antitussive or cough suppressant and dissociative hallucinogen. It is the dextrorotatory-stereoisomer of racemorphan, the levo-half being levorphanol. Dextrorphan is produced by O-demethylation of dextromethorphan by CYP2D6.
norketamine (35211-10-0)  
Norketamine, or N-desmethylketamine, is the major active metabolite of ketamine, which is formed mainly by CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor antagonist (Ki = 1.7 µM and 13 µM for (S)-(+)-norketamine and (R)-(–)-norketamine, respectively), but is about 3–5 times less potent as an anesthetic in comparison. Also, similarly again to ketamine, norketamine binds to the μ- and κ-opioid receptors.
Asimadoline (153205-46-0)  
Asimadoline (EMD-61753) is a drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist. Because of its poor ability to cross the blood–brain barrier, asimadoline lacks the psychotomimetic effects of centrally acting KOR agonists, and consequently has more potential for medical use, and has been researched as a possible treatment for irritable bowel syndrome, with reasonable efficacy seen in clinical trials.
Matrine (519-02-8)  
Matrine is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, as well as κ-opioid and μ-opioid receptor agonism. Matrine possesses strong antitumor activities in vitro and in vivo.
PHENAZOCINE (127-35-5)  
Narphen  ·  Phenazocine Hydrobromide  ·  Phenbenzorphan
Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at high doses, most likely due to action at κ-opioid and σ receptors. Phenazocine appears to be a much stronger analgesic with fewer side effects than pentazocine, probably due to a more favorable μ/κ binding ratio.
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Kappa agonists
Opioid receptor ligands
Drugs acting on the nervous system
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