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Nervous system drug, Bases (chemistry)


Drugs acting on the nervous system (34)
Amines (32)
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methadone (76-99-3)  
Dolophine  ·  Methadone Hydrochloride  ·  Amidone
Methadone, sold under the brand name Dolophine, among others, is an opioid used to treat pain and as maintenance therapy or to help with tapering in people with opioid dependence. Detoxification using methadone can either be done relatively rapidly in less than a month or gradually over as long as six months. While a single dose has a rapid effect, maximum effect can take five days of use.
BENACTYZINE (302-40-9)  
Amizil  ·  Amizyl  ·  Lucidil
Benactyzine is an anticholinergic drug that was used as an antidepressant in the treatment of depression and associated anxiety before it was pulled from the U.S. market by the FDA due to its ineffectiveness. Its use for these indications was limited by side effects such as dry mouth and nausea, and at high doses it can cause more severe symptoms such as deliriant and hallucinogenic effects.
Chlorphenoxamine (77-38-3)  
Chlorphenoxamine (Phenoxene) is an antihistamine and anticholinergic used as an antipruritic and antiparkinsonian agent. It is an analog of diphenhydramine.
1,3-Di-o-tolylguanidine (97-39-2)  
1,3-ditolylguanidine hydrochloride  ·  1,3-di-ortho-tolyl-guanidine  ·  N,N'-bis(2-methylphenyl)guanidine
Ditolylguanidine is a sigma receptor agonist. It is somewhat selective for sigma receptors, but non-selective between the two sigma receptor subtypes, binding to both σ1 and σ2 with equal affinity. It has neuroprotective and antidepressant effects, and potentiates the effects of NMDA antagonists.
Desmethylsertraline (87857-41-8)  
Desmethylsertraline (DMS), also known as norsertraline, is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline acts as a monoamine reuptake inhibitor, and may be responsible for some of its parent's therapeutic benefits. However, DMS is significantly less potent relative to sertraline as a serotonin reuptake inhibitor (Ki = 76 nM vs.
Levomethadone (125-58-6)  
Levomethadone (INN; L-Polamidon, L-Polamivet, Levadone, Levothyl), or levamethadone, is a synthetic opioid analgesic and antitussive which is marketed in Europe and is used for pain management and in opioid maintenance therapy. In addition to being used as a pharmaceutical drug itself, levomethadone, or R-(−)-methadone, is the active enantiomer of methadone, having approximately 50x the potency of the S-(+)-enantiomer as well as greater μ-opioid receptor selectivity. Accordingly, it is about twice as potent as methadone by weight and its effects are virtually identical in comparison.
Bifemelane (62232-46-6, 90293-01-9)  
MCI-2016  ·  2-(4-methylaminobutoxy)diphenylmethane  ·  Celeport
Bifemelane (INN) (Alnert, Celeport), or bifemelane hydrochloride (JAN), also known as 4-(O-benzylphenoxy)-N-methylbutylamine, is an antidepressant and cerebral activator that is widely used in the treatment of cerebral infarction patients with depressive symptoms in Japan, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma. Bifemelane acts as a monoamine oxidase inhibitor (MAOI) of both isoenzymes, with competitive (reversible) inhibition of MAO-A (Ki = 4.20 μM) (making it a reversible inhibitor of monoamine oxidase A (RIMA)) and non-competitive (irreversible) inhibition of MAO-B (Ki = 46.0 μM), and also acts (weakly) as a norepinephrine reuptake inhibitor.
S-Methadone (5653-80-5)  
Dextromethadone is an antitussive opioid. It is the (S)-enantiomer of methadone. Dextromethadone acts as a N-methyl-D-aspartate NMDA receptor antagonist similar to ketamine.
5,6-Dehydronorketamine (57683-62-2)  
Dehydronorketamine (DHNK), or 5,6-dehydronorketamine, is a minor metabolite of ketamine which is formed by dehydrogenation of its metabolite norketamine. Though originally considered to be inactive, DHNK has been found to act as a potent and selective negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 = 55 nM). For this reason, similarly to hydroxynorketamine (HNK), it has been hypothesized that DHNK may have the capacity to produce rapid antidepressant effects.
Ebrotidine (100981-43-9)  
Ebrotidine is an H2 receptor antagonist with gastroprotective activity against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine, and approximately 10-fold greater than those of cimetidine. Ebrotidine has anti-Helicobacter pylori activity via inhibition of the urease enzyme and the proteolytic and mucolytic activities of the bacterium.
N-Isopropylbenzylamine (102-97-6)  
N-benzylisopropylamine  ·  N-benzyl-N-isopropylamine
Isopropylbenzylamine is a chemical compound used as an intermediate in the pharmaceutical industry as a precursor to the manufacture of some drugs. It has recently come to the attention of the DEA due to its use by illicit methamphetamine manufacturers as a diluting agent.This amine's ammonium salt is very similar in appearance and physical properties to methamphetamine and is cheap and not currently illegal. Isopropylbenzylamine is a structural isomer of methamphetamine, and has the same molar mass.
Fenozolone (15302-16-6)  
Fenozolone (Ordinator) was developed by Laboratoires Dausse in the 1960s and is a psychoactive drug and stimulant related to pemoline and 4-methylaminorex which acts as a norepinephrine-dopamine releasing agent (NDRA).
Amylocaine (644-26-8)  
Stovaine  ·  amylocaine hydrochloride  ·  Dolodent
Amylocaine was the first synthetic local anesthetic. It was synthesized and patented under the name Stovaine by Ernest Fourneau at the Pasteur Institute in 1903. It used to be used mostly in spinal anesthesia.
Adafenoxate (82168-26-1)  
Adafenoxate is a compound related to centrophenoxine, that has been found to act as a nootropic in rats.
Exp 561 (10206-89-0)  
EXP-561 is an investigational drug that acts as an inhibitor of the reuptake of serotonin, dopamine, and norepinephrine. It was developed in the 1960s by Du Pont and was suggested as a potential antidepressant but failed in trials and was never marketed.
FLUCINDOLE (40594-09-0)  
Flucindole is an antipsychotic with a tricyclic structure that was never marketed. It is the 6,8-difluoro derivative of cyclindole.
CP 122288 (143321-74-8)  
CP-122,288 is a drug which acts as a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin receptor subtypes. It is a derivative of the migraine medication sumatriptan, but while CP-122,288 is 40,000 times more potent than sumatriptan as an inhibitor of neurogenic inflammation and plasma protein extravasation, it is only twice as potent as a constrictor of blood vessels. In human trials, CP-122,288 was not found to be effective as a treatment for migraine, but its selectivity for neurogenic anti-inflammatory action over vasoconstriction has made it useful for research into the underlying causes of migraine.
Binedaline (60662-16-0)  
Binedaline (Ixprim), also called binodaline, is a drug that was being investigated as an antidepressant in the 1980s but never marketed. It acts as a selective norepinephrine reuptake inhibitor (Ki = 25 nM), with relatively insignificant influence on the serotonin (Ki = 847 nM) and dopamine (Ki >= 2 µM) transporters. It has negligible affinity for the α-adrenergic, mACh, H1, or 5-HT2 receptors.
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