Dopamine serotonin antagonist-1

Modify Date: 2024-01-05 01:21:25

Dopamine serotonin antagonist-1 Structure
Dopamine serotonin antagonist-1 structure
Common Name Dopamine serotonin antagonist-1
CAS Number 1977-07-7 Molecular Weight 292.37800
Density N/A Boiling Point N/A
Molecular Formula C18H20N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dopamine serotonin antagonist-1


Dopamine serotonin antagonist-1 is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.

 Names

Name 6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine
Synonym More Synonyms

 Dopamine serotonin antagonist-1 Biological Activity

Description Dopamine serotonin antagonist-1 is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
Related Catalog
Target

Ki: 200 nM (Dopamne D1), 2500 nM (Dopamne D2), 420 nM (Dopamne D4), 39 nM (Serotonin S2A), 84 nM (Serotonin S2C), 200 nM (Serotonin S3)[1]

Kinase Assay To measure the affinity for the serotonin 5-3 (6-HTs) receptor, membranes from confluent NG108-15 cell monolayers are prepared and stored. The assay tubes, in triplicate, receive 100 μL of 1 nM [3H]GR65630, 50 μL of test compound (include Dopamine serotonin antagonist-1) or 10 pM metoclopramide for nonspecific binding, 200 μL membrane suspension (0.1 to 0.2 mglassay tube) in a final volume of 500 μL. Incubation proceeds at 37°C for 30 min and is terminated by filtration of the mixture through GF/B glass fiber filters, presoaked in 0.1% polyethylenimine, using a Brandel cell harvester. The filters are rinsed with two 5-mL portions of ice-cold HEPES-KOH, pH 7.4, buffer. The filters are transferred to scintillation vials to which 4 mL of Beckman Ready Protein is added, and the radioactivity is determined by liquid scintillation spectrometry[1].
References

[1]. Phillips ST, et al. Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. J Med Chem. 1994 Aug 19;37(17):2686-96.

 Chemical & Physical Properties

Molecular Formula C18H20N4
Molecular Weight 292.37800
Exact Mass 292.16900
PSA 30.87000
LogP 2.51870
Vapour Pressure 1.48E-08mmHg at 25°C
Storage condition 2-8℃

 Synonyms

Dechloroclozapine
Dopamine serotonin antagonist-1