Cyamemazine

 ( Alpha-1 Blockers ) 

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

(1996). 9780412466304, Chapman & Hall/CRC. . ISBN 9780412466304

(1988). 9780815511441, Noyes Publications. . ISBN 9780815511441

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Medical use It is used for the treatment of schizophrenia and, especially, for psychosis-associated anxiety, due to its unique anxiolytic efficacy.

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

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Side effects Here are some of the most common side effects and related incidence:

• Sedation (20%)
• Vertigo (7.9%)
• Constipation (4%)
• Dyskinesia (4.4%)
• Dryness of mouth (5.9%)
• Hypotension (7.4%)
• Tachycardia (3.2%)

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Mechanism Cyamemazine differs from other phenothiazine neuroleptics in that aside from the usual profile of dopamine, α₁-adrenergic, H₁, and mACh receptor antagonism, it additionally produces potent blockade of several serotonin receptors, including 5-HT_2A, 5-HT_2C, and 5-HT₇. These actions have been implicated in cyamemazine's anxiolytic effects (5-HT_2C) and lack of extrapyramidal (5-HT_2A), and despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.

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

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Synthesis

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

Categories: Alpha-1 Blockers, Dimethylamino Compounds, Dopamine Antagonists, H1 Receptor Antagonists, M1 Receptor Antagonists, M2 Receptor Antagonists, M3 Receptor Antagonists, M4 Receptor Antagonists, M5 Receptor Antagonists, Nitriles, Phenothiazines, Serotonin Receptor Antagonists, Typical Antipsychotics

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