Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Convulsants, Four-membered rings
Cyclic compounds (1)
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%).
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".
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.
WIN VI (98034-30-1)
Win 52035 · WIN 52035-2 · 5-(5-(4-(4,5-dihydro-2-oxazolyl)phenoxy)pentyl)-3-methylisoxazole
Epibatidine is a putative alkaloid that is secreted by the Ecuadoran frog Epipedobates anthonyi. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated until 1992.
nicotinanilide · nicotinanilide monohydrochloride
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.
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.
phenylpiperazine · phenylpiperazine monohydrochloride · phenylpiperazine dihydrobromide
1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. A number of phenylpiperazine derivatives are drugs, including: Pharmaceuticals: Research chemicals: Designer drugs:
Mesulergine is a psychoactive drug of the ergoline chemical class that acts on serotonin and dopamine receptors. The compound had entered clinical trials for the treatment of Parkinson's disease; however, further development was halted due to adverse histological abnormalities in rats.
Spiroperidol · Spiroperone
Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class. It is licensed for clinical use in Japan as a treatment for schizophrenia. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis.
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.
TENOCYCLIDINE (21500-98-1, 1867-65-8)
Tenocyclidine (TCP) was discovered by a team at Parke Davis in the late 1950s. It is a dissociative anesthetic drug with psychostimulant and hallucinogenic effects. It is similar in effects to phencyclidine (PCP) but is considerably more potent.
isoguvacine hydrochloride · isoguvacine hydrobromide
Isoguvacine is a GABAA receptor agonist used in scientific research.
Quipazine is a piperazine drug used in scientific research. It is a moderately selective serotonin receptor receptor agonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3.
m-CPP · 1-(3-chlorophenyl)piperazine dihydrochloride · m-chlorophenylpiperazine
meta-Chlorophenylpiperazine (mCPP) is a psychoactive drug of the phenylpiperazine class. It was initially developed in the late-1970s and used in scientific research before being sold as a designer drug in the mid-2000s. It has been detected in pills touted as legal alternatives to illicit stimulants in New Zealand and pills sold as "ecstasy" in Europe and the United States.