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Medchemexpress LLC SB-277011 (hydrochloride) | 215804-67-4 | 99.6% | 475.02 | 25 MG
SDP

Supplier:  Medchemexpress LLC 25MGHY10847B

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SB-277011 hydrochloride is a potent, selective, orally bioavailable, and brain-penetrant dopamine D3 receptor (D3R) antagonist. It demonstrates 80- to 100-fold selectivity over other dopamine receptors.

  • Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively.
  • Selectivity over D2, 5-HT1B, and 5-HT1D receptors.
  • Oral bioavailability of 43% and a half-life of 2.0 h in rats.
  • High brain-penetrant (brain:blood ratio of 3.6:1).
  • Reverses quinelorane effects in the nucleus accumbens at 3 mg/kg (p.o.) in rats.
  • Reduces intravenous cocaine self-administration in rats (12.5-25 mg/kg, i.p.).
  • Inhibits basal and cocaine-enhanced locomotion in rats at 50 mg/kg.

Catalog No. 50-003-47663


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