2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Dopamine D3 receptor antagonist-3

Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kb of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder.

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Dopamine D3 receptor antagonist-3

Dopamine D3 receptor antagonist-3 Chemical Structure

CAS No. : 2894793-37-2

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Dopamine D3 receptor antagonist-3 Related Antibodies

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Description

Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kb of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder[1].

IC50 & Target[1]

Dopamine D3 receptor

0.49 μM (Kd)

In Vitro

Dopamine D3 receptor antagonist-3 (Compound 6a) exhibits good microsomal stability microsome stability (human/mouse/rat) and lacks activity at the hERG channel with estimated IC50 values >10 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dopamine D3 receptor antagonist-3 Related Antibodies
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 40 mg/kg i.p. Tmax 1.0 h
Mice 40 mg/kg i.p. Cmax 28 μM
Mice 40 mg/kg i.p. T1/2 3.97 h
Mice 40 mg/kg i.p. AUClast 72681 ng·h/mL
Mice 40 mg/kg i.p. AUCinf 97638 ng·h/mL
In Vivo

Dopamine D3 receptor antagonist-3 (Compound 6a) (40 mg/kg, i.p., single dose) is brain penetrant and exhibits brain half-lives of 3.65 h and brain Cmaxs value of 3183 ng/g (6.5 μM), respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

485.86

Formula

C18H17ClF5N3O3S
CAS No.
SMILES

ClC(C=C1NS(C(C(C(N(C2)CCC2(F)F)=O)=C3C)=C(N3)C)(=O)=O)=C(C=C1)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Dopamine D3 receptor antagonist-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dopamine D3 receptor antagonist-32894793-37-2Dopamine ReceptorPositive Allosteric Modulator-Antagonistβ-Arrestin RecruitmentRadioligand Binding AssaysPharmacokineticsStructure-Activity RelationshipInhibitorinhibitorinhibit

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