PRX-07034

SKU: orb1219453

Description

PRX-07034 is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (≥100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors.PRX-07034 is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist ( 100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors. For cyclic AMP quantification, PRX-07034 demonstrated antagonist activity (IC(50) = 19 nM) without an effect on basal levels and did not show any agonist activity up to 10 μM. PRX-07034 at 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination.

Research Area

Neuroscience

Key Properties

• CAS Number: 903580-39-2
• MW: 490.44
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₉Cl₂N₃O₄S
• SMILES: Cl.COc1cc(Cl)cc(C(C)Nc2cc(ccc2S(C)(=O)=O)N2CCNCC2)c1OC
• Target: 5-HT Receptor
• Solubility: In Vitro: DMSO : 31.25 mg/mL (63.72 mM)

Bioactivity

• In Vivo:
  PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination. Animal model: Male Long-Evans rats weighing approximately 350 g. Dosage: 0.1, 1, or 3 mg/kg. Administration: Injected intraperitoneal. Result: 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination.
• In Vitro:
  PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 μM, 71 nM, 0.64 μM, and 0.45 μM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 μM, 2.5 μM, and 3.7 μM, respectively. In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50 = 4.8 μM) and very low agonistic activity for the opioid μ-receptor (EC50 = 19 μM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor