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Kappa agonists, Analgesic, Opioid metabolites, Mu-opioid agonists

Categories

Analgesics (2)
Delta-opioid agonists (2)
Drugs acting on the nervous system (2)
Ethers (2)
Euphoriants (2)
Nociceptin receptor agonists (2)
Opioid receptor ligands (2)
Opioids (2)
Psychoactive drugs (2)


Related Results:
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.
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.
Nalorphine hydrochloride (57-29-4)  
Nalorphine  ·  Allylnormorphine  ·  Lethidrone
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.
Etorphine (14521-96-1)  
M99  ·  Ethorphine
Pravadoline (92623-83-1)  
Pravadoline (WIN 48,098) is an antiinflammatory and analgesic drug with an IC50 of 4.9 µM and a Ki of 2511 nM at CB1, related in structure to nonsteroidal anti-inflammtory drugs (NSAIDs) such as indometacin. It was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX). However, pravadoline was found to exhibit unexpectedly strong analgesic effects, which appeared at doses ten times smaller than the effective anti-inflammatory dose and so could not be explained by its action as a COX inhibitor.
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.
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.
naloxone (465-65-6)  
Narcan  ·  Naloxone Hydrochloride  ·  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.
Ro 48-8071 (161582-11-2)  
Ro 48-8071hydrochloride  ·  (4'-(6-allylmethylaminohexyloxy)-2'-fluorophenyl)-4-(4-bromophenyl)methanone fumarate  ·  Ro-48-8071
CYCLAZOCINE (3572-80-3, 63903-61-7, 7346-09-0)  
Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity for the DOR.
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.
Nikethamide (59-26-7)  
Coramine  ·  Coramin  ·  Cordiamine
Nikethamide is a stimulant which mainly affects the respiratory cycle. Widely known by its former trade name of Coramine, it was used in the mid-twentieth century as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. It is no longer commonly considered to be of value for such purposes.
baclofen (62594-36-9, 1134-47-0)  
Lioresal  ·  Genpharm  ·  beta-(p-Chlorophenyl)-gamma-aminobutyric Acid
Baclofen, sold under the brand name Lioresal among others, is a medication used to treat spasticity. It is used as a central nervous system depressant and skeletal muscle relaxant although its effectiveness has not been clearly shown. It is also used in topical creams to help with pain.
Gepirone (83928-76-1)  
Gepirone is an antidepressant and anxiolytic drug of the azapirone group that was synthesized by Bristol-Myers Squibb in 1986 and has been under development for the treatment of depression but has yet to be marketed. It has been under development in the U.S. in an extended release form (referred to as gepirone ER), but despite completing phase III clinical trials and demonstrating efficacy, it has been rejected multiple times by the Food and Drug Administration (FDA) during the drug approval process.
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
Opioid metabolites
Mu-opioid agonists
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