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5-HT1AR/5-HT6R ligand-1

5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively) . 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM[1].

Product Specifications

UNSPSC

12352005

Target

5-HT Receptor; Dopamine Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=S(C1=C2C=CC=CC2=CC=C1Cl)(NCCCCCCNC3=NC4=C(C=CC=C4)C(C)N3)=O

Molecular Formula

C25H29ClN4O2S

Molecular Weight

485.04

References & Citations

[1]Zaręba P, et al., Long-Chain Cyclic Arylguanidines as Multifunctional Serotonin Receptor Ligands with Antiproliferative Activity. ACS Omega. 2025 Feb 11;10 (7) :6446-6469.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

5-HT6 Receptor;5-HT7 Receptor; D2 Receptor

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