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Kappa agonists, Opioids, Dissociative drugs

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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.
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.
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.
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.
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.
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.
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).
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.
SPIRADOLINE (87151-85-7)  
Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist. It has analgesic, diuretic and antitussive effects, and produces subjective effects in animals similar to those of ketazocine and alazocine. The main effect in humans is sedation, along with analgesic and diuretic effects, but significant side effects such as dysphoria and hallucinations have stopped it from being used clinically.
CYCLORPHAN (4163-15-9)  
Cyclorphan is an opioid analgesic of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) weak partial agonist or antagonist, κ-opioid receptor (KOR) full agonist, and, to a much lesser extent, δ-opioid receptor (DOR) agonist (75-fold lower affinity relative to the KOR). The drug was first synthesized in 1964 by scientists at Research Corporation.
Racemorphan (297-90-5)  
Racemorphan, or morphanol, is the racemic mixture of the two stereoisomers of 17-methylmorphinan-3-ol, each with differing pharmacology and effects: Dextrorphan - an antitussive and dissociative hallucinogen (NMDA receptor antagonist) Levorphanol - an opioid analgesic Racemorphan itself is under international control per the Single Convention on Narcotic Drugs 1961 and is therefore listed as a Schedule II Narcotic controlled substance in the US Controlled Substances Act 1970; it has an ACSCN of 9733 and in 2014 it had an aggregate annual manufacturing quota of zero. The salts in use are hydrobromide (free base conversion ratio 0.741), hydrochloride (0.876), and tartrate (0.632).
Tifluadom (83386-35-0)  
KC 5103  ·  KC 5911  ·  KC-5911
Tifluadom is a benzodiazepine derivative with an unusual activity profile. Unlike most benzodiazepines, tifluadom has no activity at the GABAA receptor, but instead is a selective agonist for the κ-opioid receptor. In accordance, it has potent analgesic and diuretic effects in animals, and also has sedative effects and stimulates appetite.
Oxilorphan (42281-59-4)  
oxilorphan hydrochloride, (9alpha,13alpha,14alpha)-isomer  ·  oxilorphan, (14alpha)-(+-)-isomer  ·  L-N-cyclopropylmethyl-3,14-dihydroxymorphinan
Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation.
125-73-5 (125-73-5)  
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.
Xorphanol (77287-89-9)  
Xorphanol (INN) (developmental code name TR-5379 or TR-5379M), also known as xorphanol mesylate (USAN), is an opioid analgesic of the morphinan family that was never marketed. Xorphanol is a mixed agonist–antagonist of opioid receptors, acting preferentially as a high-efficacy partial agonist/near-full agonist of the κ-opioid receptor (Ki = 0.4 nM; EC50 = 3.3 nM; Imax = 49%; IA = 0.84) and to a lesser extent as a partial agonist of the μ-opioid receptor (Ki = 0.25 nM; IC50 = 3.4 nM; Imax = 29%) with lower relative intrinsic activity and marked antagonistic potential (including the ability to antagonize morphine-induced effects and induce opioid withdrawal in opioid-dependent individuals). The drug has also been found to act as an agonist of the δ-opioid receptor (Ki = 1.0 nM; IC50 = 8 nM; Imax = 76%).

Related Results:
DL-Methamphetamine (4846-07-5, 7632-10-2, 51-57-0)  
Methamphetamine  ·  Desoxyn  ·  Methylamphetamine
Methamphetamine (contracted from N-methylamphetamine) is a strong central nervous system (CNS) stimulant that is mainly used as a recreational drug and less commonly as a second-line treatment for attention deficit hyperactivity disorder and obesity. Methamphetamine was discovered in 1893 and exists as two enantiomers: levo-methamphetamine and dextro-methamphetamine. Methamphetamine properly refers to a specific chemical, the racemic free base, which is an equal mixture of levomethamphetamine and dextromethamphetamine in their pure amine forms.
Naloxone hydrochloride (357-08-4)  
Naloxone  ·  Narcan  ·  Nalone
Naloxone, sold under the brandname Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone may be combined within the same pill as an opioid to decrease the risk of misuse. When given intravenously, naloxone works within two minutes, and when injected into a muscle, it works within five minutes; it may also be sprayed into the nose.
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Kappa agonists
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