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

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Analgesics (1)
Cyclic compounds (1)
Five-membered rings (1)
Opioids (1)
Pharmaceuticals (1)
Psychoactive drugs (1)
Pyrrolidines (1)
Synthetic opioids (1)

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.

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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.
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.
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.
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.
15532-75-9 (15532-75-9)  
TFMPP  ·  1-(m-trifluoromethylphenyl)piperazine  ·  1-(3-trifluoromethylphenyl)piperazine
3-Trifluoromethylphenylpiperazine (TFMPP) is a recreational drug of the piperazine chemical class. Usually in combination with its analogue benzylpiperazine (BZP), it is sold as an alternative to the illicit drug MDMA ("Ecstasy") under the name "Legal X".
Etorphine (14521-96-1)  
M99  ·  Ethorphine
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.
WIN VI (98034-30-1)  
Win 52035  ·  WIN 52035-2  ·  5-(5-(4-(4,5-dihydro-2-oxazolyl)phenoxy)pentyl)-3-methylisoxazole
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.
tizanidine (51322-75-9)  
Tizanidine (trade names Zanaflex (Acorda Therapeutics), Sirdalud (Novartis), Relentus (Beximco Pharma) Is a centrally acting α2 adrenergic agonist used as a muscle relaxant. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant.
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
BENPERIDOL (2062-84-2)  
Benperidol-neuraxpharm  ·  Glianimon  ·  Frenactil
Benperidol is a drug which is a highly potent butyrophenone derivative. It is the most potent neuroleptic on the European market, with chlorpromazine equivalency as high as 75 to 100 (about 150 to 200% potency in terms of dose compared to haloperidol). It is an antipsychotic, which can be used for the treatment of schizophrenia, but it is primarily used to control antisocial hypersexual behaviour, and is sometimes prescribed to sex offenders as a condition of their parole, as an alternative to anti-androgen drugs such as cyproterone acetate.
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.
Etifoxine (21715-46-8)  
Etifoxine (INN, also known as etafenoxine; trade name Stresam) is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. It is sold in approximately 40 countries for anxiety disorders, without the sedation and ataxia associated with benzodiazepine drugs. It has similar anxiolytic effects to benzodiazepine drugs, but is structurally distinct and does not bind to the benzodiazepine receptor.
Ro 48-8071 (161582-11-2)  
Ro 48-8071hydrochloride  ·  (4'-(6-allylmethylaminohexyloxy)-2'-fluorophenyl)-4-(4-bromophenyl)methanone fumarate  ·  Ro-48-8071
clonidine (4205-90-7)  
Catapres  ·  Clonidine Hydrochloride  ·  Dixarit
Clonidine (trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist that has been in clinical use since 1966.
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Kappa agonists
Opioid receptor ligands
Drugs acting on the nervous system
Analgesic
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