1977-07-7
1977-07-7 structure
- Name: Dopamine serotonin antagonist-1
- Chemical Name: 6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine
- CAS Number: 1977-07-7
- Molecular Formula: C18H20N4
- Molecular Weight: 292.37800
- Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
- Create Date: 2017-02-09 06:35:01
- Modify Date: 2025-08-22 10:45:53
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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.
| Name | 6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine |
|---|---|
| Synonyms |
Dechloroclozapine
Dopamine serotonin antagonist-1 |
| 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 |
| 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℃ |