1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Cyamemazine

Cyamemazine 

Cat. No.: HY-14264
Handling Instructions

Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.

For research use only. We do not sell to patients.

Cyamemazine Chemical Structure

Cyamemazine Chemical Structure

CAS No. : 3546-03-0

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10 mM * 1 mL in DMSO USD 210 In-stock
Estimated Time of Arrival: December 31
5 mg USD 295 In-stock
Estimated Time of Arrival: December 31
10 mg USD 495 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].

IC50 & Target[1]

5-HT2A Receptor

1.5 nM (Ki)

5-HT2C Receptor

12 nM (Ki)

5-HT3 Receptor

75 nM (Ki)

In Vitro

Cyamemazine exhibits a high affinity for dopamine receptors, which is consistent with its antipsychotic activity. The antagonist activity of Cyamemazine at muscarinic receptors is consistent with its affinity for M1 (Ki = 13 nM), M2 (Ki = 42 nM), M3 (Ki = 321 nM), M4 (Ki = 12 nM), and M5 (Ki = 35 nM) receptors[1].

In Vivo

Cyamemazine behaves as an antagonist at the 5-HT3, 5-HT2C, and 5-HT2A receptors in 5-HT3-dependent contraction of isolated guinea pig ileum and bradycardic responses in rats, in 5-HT2C-dependent phospholipase C stimulation in the rat brain membrane, and in 5-HT2A-dependent contraction of isolated rat aorta rings and isolated guinea pig trachea. Cyamemazine antagonizes 5-HT3 and 5-HT2C receptors and that this effect is partially involved in its therapeutic activity in anxiety disorders. Acute administration of low doses of Cyamemazine can reduces extracellular dopamine and metabolite concentrations in rat striatum[1].

Molecular Weight

323.46

Formula

C₁₉H₂₁N₃S

CAS No.

3546-03-0

SMILES

CN(C)CC(C)CN1C2=C(C=CC(C#N)=C2)SC3=CC=CC=C31

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Cyamemazine5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorPhenothiazinechromophoreneurolepticanxiolyticsedativeserotonindopaminehistaminemuscarineInhibitorinhibitorinhibit

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Cyamemazine
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