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.

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter

Research Areas >> Neurological Disease

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]

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].

[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.

Fluoxetine Hydrochloride | CB-154 mesylate | SCH 23390 hydrochloride | Levodopa | Cabergoline | Paroxetine HCl | Sertraline hydrochloride | Thioridazine hydrochloride | Brexpiprazole | Domperidone | Trifluoperazine dihydrochloride | Fluvoxamine maleat | pimozide | Risperidone | SKF38393 HCl