1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. PRX-07034 hydrochloride

PRX-07034 hydrochloride 

Cat. No.: HY-14559
Handling Instructions

PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.

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

PRX-07034 hydrochloride Chemical Structure

PRX-07034 hydrochloride Chemical Structure

CAS No. : 903580-39-2

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Description

PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility[1].

IC50 & Target[1]

5-HT6 Receptor

4-8 nM (Ki)

5-HT6 Receptor

19 nM (IC50)

5-HT1B Receptor

260 nM (Ki)

5-HT1A Receptor

420 nM (Ki)

5-HT1D Receptor

2.8 μM (Ki)

5-HT2A Receptor

2.5 μM (IC50)

5-HT2B Receptor

2.5 μM (IC50)

5-HT2C Receptor

3.7 μM (IC50)

Dopamine D3 Receptor

71 nM (Ki)

Opioid μ Receptor

0.45 μM (Ki)

Histamine H2 Receptor

0.64 μM (Ki)

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[1].
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) [1].

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

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[1].

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

Animal Model: Male Long-Evans rats weighing approximately 350 g[1]
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.
Molecular Weight

490.44

Formula

C₂₁H₂₉Cl₂N₃O₄S

CAS No.

903580-39-2

SMILES

O=S(C1=CC=C(N2CCNCC2)C=C1NC(C)C3=CC(Cl)=CC(OC)=C3OC)(C)=O.[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:

PRX-07034PRX07034PRX 070345-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT6workingmemorycognitiveflexibilityInhibitorinhibitorinhibit

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Product Name:
PRX-07034 hydrochloride
Cat. No.:
HY-14559
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