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PRX-07034 hydrochloride

Catalog No. T8720   CAS 903580-39-2
Synonyms: PRX-07034

PRX-07034 hydrochloride 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 hydrochloride 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.

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PRX-07034 hydrochloride Chemical Structure
PRX-07034 hydrochloride, CAS 903580-39-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 40.00
5 mg In stock $ 64.00
10 mg In stock $ 105.00
25 mg In stock $ 198.00
50 mg In stock $ 328.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.17%
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Biological Description
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Description PRX-07034 hydrochloride 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 hydrochloride 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.
Targets&IC50 5-HT2A receptor:2.5 μM (IC50), 5-HT2C receptor:3.7 μM (IC50), 5-HT6 receptor:19 nM (IC50), 5-HT6 receptor:4-8 nM (Ki), H2 receptor:0.64 μM (Ki), D3 receptor:71 nM (Ki), μ opioid receptor:0.45 μM (Ki), 5-HT2B receptor:2.5 μM (IC50), 5-HT1A receptor:420 nM (Ki), 5-HT1B receptor:260 nM (Ki), 5-HT1D receptor:2.8 μM (Ki)
In vitro 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.
Synonyms PRX-07034
Molecular Weight 490.44
Formula C21H29Cl2N3O4S
CAS No. 903580-39-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (20.39 mM)

TargetMolReferences and Literature

1. Mohler E G , Baker P M , Gannon K S , et al. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats[J]. Psychopharmacology, 2012, 220(4):687-696. 2. Abraham R , Nirogi R , Shinde A , et al. Low-dose prazosin in combination with 5-HT6 antagonist PRX-07034 has antipsychotic effects[J]. Canadian Journal of Physiology & Pharmacology, 2015, 93(1):13-21.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Angiogenesis related Compound Library ReFRAME Related Library Neuronal Signaling Compound Library NO PAINS Compound Library

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Keywords

PRX-07034 hydrochloride 903580-39-2 GPCR/G Protein Neuroscience 5-HT Receptor flexibility PRX-07034 Hydrochloride PRX 07034 PRX-07034 5-HT6 working Serotonin Receptor cognitive Inhibitor PRX07034 PRX 07034 Hydrochloride inhibit PRX 07034 hydrochloride memory PRX07034 Hydrochloride 5-hydroxytryptamine Receptor PRX07034 hydrochloride inhibitor

 

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