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GABA receptor antagonists

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Analgesics (7)
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Delta-opioid agonists (7)
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GABA receptor ligands (7)
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Nociceptin receptor agonists (7)
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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.
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.
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.

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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.
isoguvacine (64603-90-3)  
isoguvacine hydrochloride  ·  isoguvacine hydrobromide
Isoguvacine is a GABAA receptor agonist used in scientific research.
ampa (77521-29-0)  
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid  ·  AMPA, (R)-Isomer, Monohydrobromide  ·  alpha Amino 3 hydroxy 5 methyl 4 isoxazolepropionic Acid
AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) is a compound that is a specific agonist for the AMPA receptor, where it mimics the effects of the neurotransmitter glutamate. There is several types of glutamatergic ion channels in the central nervous system including AMPA, kainic acid and N-methyl-D-aspartic acid (NMDA) channels. In the synapse, these receptors serve very different purposes.
3-Apmpa (127729-35-5)  
SKF-97,541 is a compound used in scientific research which acts primarily as a selective GABAB receptor agonist. It has sedative effects in animal studies and is widely used in research into potential treatment of various types of drug addiction.
Ifenprodil (23210-56-2, 23210-58-4)  
4-benzyl-alpha-(p-hydroxyphenyl)-beta-methyl-1-piperidineethanol  ·  ifenprodil tartrate (2:1), (R-(R*,R*))-isomer  ·  ifenprodil, (R*,S*)-(+-)-isomer
Ifenprodil is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. NMDA receptors are multimeric ionotropic glutamate receptors composed of four subunits.
bicuculline (485-49-4)  
6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)furo(3,4-e)1,3-benzodioxol-8(6H)one
Gyki-52466 (102771-26-6)  
GYKI 52466  ·  1-(p-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
GYKI-52466 is a 2,3-benzodiazepine that acts as an ionotropic glutamate receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively), orally-active anticonvulsant, and skeletal muscle relaxant. Unlike conventional 1,4-benzodiazepines, GYKI-52466 and related 2,3-benzodiazepines do not act on GABAA receptors. Like other AMPA receptor antagonists, GYKI-52466 has anticonvulsant and neuroprotective properties.
ritanserin (87051-43-2)  
Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.
CGP-20712A (137888-49-4)  
2-hydroxy-5-(2-(hydroxy-3-(4-((1-methyl-4-trifluoromethyl)-1H-imidazol-2-yl)phenoxy)propyl)aminoethoxy)benzamide  ·  CGP-20712  ·  CGP 20712A
Xanthinol nicotinate (437-74-1)  
Xantinol Nicotinate  ·  Xanthinol Niacinate  ·  Xavin
Xanthinol is a drug prepared from theophylline used as a vasodilator. It is most often used as the salt with niacin (nicotinic acid), known as xantinol nicotinate.
XANOMELINE (131986-45-3)  
Xanomeline (LY-246,708; Lumeron, Memcor) is a muscarinic acetylcholine receptor agonist with reasonable selectivity for the M1 and M4 subtypes, though it is also known to act as a M5 receptor antagonist. It has been studied for the treatment of both Alzheimer's disease and schizophrenia, particularly the cognitive and negative symptoms, although gastrointestinal side effects led to a high drop-out rate in clinical trials. Despite this, xanomeline has been shown to have reasonable efficacy for the treatment of schizophrenia symptoms, and one recent human study found robust improvements in verbal learning and short-term memory associated with xanomeline treatment.
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