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Kappa agonists, Analgesic, Delta-opioid agonists

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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.
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
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.
Hemorphin 4 (103930-64-9)  
Hemorphin-4 is an endogenous opioid peptide of the hemorphin family which possesses antinociceptive properties and is derived from the β-chain of hemoglobin in the bloodstream. It is a tetrapeptide with the amino acid sequence Tyr-Pro-Trp-Thr. Hemorphin-4 has affinities for the μ-, δ-, and κ-opioid receptors that are in the same range as the structurally related β-casomorphins, although affinity to the κ-opioid receptor is markedly higher in comparison.
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).
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%).

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Bremazocine (83829-76-9, 75684-07-0, 79665-42-2)  
bremazocine hydrochloride, (2R)-isomer  ·  bremazocine hydrochloride, (+-)-isomer  ·  2-(1-hydroxy-cyclopropylmethyl)-5-ethyl-9,9-dimethyl-2'-hydroxy-6,7-benzomorphan
Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress breathing.
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.
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.
Ro 48-8071 (161582-11-2)  
Ro 48-8071hydrochloride  ·  (4'-(6-allylmethylaminohexyloxy)-2'-fluorophenyl)-4-(4-bromophenyl)methanone fumarate  ·  Ro-48-8071
Spiroxatrine (1054-88-2)  
Spiroxatrine is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects.
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Kappa agonists
Analgesic
Delta-opioid agonists
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