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5-HT6 inverse agonist 1

5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL) -induced rat model[1].

Product Specifications

CAS Number

[2727088-38-0]

UNSPSC

12352005

Target

5-HT Receptor; CDK; mTOR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein; Neuronal Signaling; PI3K/Akt/mTOR

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/5-ht6-inverse-agonist-1.html

Smiles

O=C(NC1CCNCC1)C2=C(N(C=C2)S(=O)(C3=CC=CC(Cl)=C3)=O)C4=CC=C(C=C4)F.Cl

Molecular Formula

C22H22Cl2FN3O3S

Molecular Weight

498.40

References & Citations

[1]Drop M, et al., Neuropathic pain-alleviating activity of novel 5-HT6 receptor inverse agonists derived from 2-aryl-1H-pyrrole-3-carboxamide. Bioorg Chem. 2021 Oct;115:105218.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MLAG-3; MUC2; MUC3; α-1 microglobulin

Curated Selection

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