1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. SB-277011 dihydrochloride

SB-277011 dihydrochloride (Synonyms: SB-277011A dihydrochloride)

Cat. No.: HY-10847A
Handling Instructions

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

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

SB-277011 dihydrochloride Chemical Structure

SB-277011 dihydrochloride Chemical Structure

CAS No. : 1226917-67-4

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Based on 1 publication(s) in Google Scholar

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Description

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

IC50 & Target

pKi: 8.0 (D3 receptor), 6.0 (D2 receptor), <5.2 (5-HT1B receptor), 5.9 (5-HT1D receptor)[1]

In Vitro

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1].

In Vivo

SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].
SB-277011A (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011A can significantly inhibit basal and cocaine-enhanced locomotion in rats[2].

Molecular Weight

511.49

Formula

C₂₈H₃₂Cl₂N₄O

CAS No.

1226917-67-4

SMILES

O=C(C1=CC=NC2=CC=CC=C12)N[[email protected]]3CC[[email protected]](CCN4CC5=C(C=C(C#N)C=C5)CC4)CC3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

SB-277011SB-277011ASB277011SB 277011Dopamine Receptornucleus accumbencocaine locomotiondopamine receptorInhibitorinhibitorinhibit

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SB-277011 dihydrochloride
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