Cyamemazine

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Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class which was introduced by Theraplix in France in 1972 and later in Portugal as well.[1][2][3][4]

Medical use

It is used for the treatment of schizophrenia and, especially, for psychosis-associated anxiety, due to its unique anxiolytic efficacy.[5][6]

It is also used to reduce anxiety associated with benzodiazepine withdrawal syndrome and anxiety in depression with suicidal tendency.[7]

Side effects

Here are some of the most common side effects and related incidence:[8]

Mechanism

Cyamemazine differs from other phenothiazine neuroleptics in that aside from the usual profile of dopamine, α1-adrenergic, H1, and mACh receptor antagonism,[9] it additionally produces potent blockade of several serotonin receptors, including 5-HT2A, 5-HT2C, and 5-HT7.[9][10][11][12] These actions have been implicated in cyamemazine's anxiolytic effects (5-HT2C) and lack of extrapyramidal side effects (5-HT2A),[9][10] and despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.[13]

Site Ki (nM) Species Ref
H1 9.3 Guinea pig [14]
H2 351 Guinea pig [14]
H3 10000+ Rat [14]
M1 13 Human [14]
M2 42 Human [14]
M3 32 Human [14]
M4 12 Human [14]
M5 35 Human [14]
5-HT1A 517 Human [14]
5-HT2A 1.5 Human [14]
5-HT2C 12 Human [14]
5-HT3 2943 Human [14]
5-HT7 22 Human [14]
D1 3.8 Human [14]
D2 5.8 Human [14]
D3 2.5 Human [14]
D4 5.3 Human [14]
α1 2.3 Rat [14]
α2 1320 Rat [14]
GABAA 10000+ Rat [14]
GABAB 10000+ Rat [14]
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Synthesis

File:Cyamemazine synthesis.svg
Synthesis:[15] Patent:[16]

2-Cyanophenothiazine [38642-74-9] (1) 3-Chloro-2-methylpropyl(dimethyl)amine [23349-86-2] (2)

References

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