1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. GSK-163090 dihydrochloride

GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.

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GSK-163090 dihydrochloride

GSK-163090 dihydrochloride Chemical Structure

CAS No. : 844903-52-2

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Description

GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities[1].

IC50 & Target[1]

5-HT1A Receptor

9.4 (pKi)

5-HT1B Receptor

8.5 (pKi)

5-HT1D Receptor

9.7 (pKi)

In Vivo

GSK163090 (dihydrochloride) (compound 36) shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA) in male Sprague-Dawley rats, with ED50 values ranging from 0.03 to 1 mg/kg[1].

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

Molecular Weight

488.45

Formula

C25H31Cl2N5O

CAS No.
SMILES

O=C1NCCN1C2=CC=CC(CCN3CCN(C4=C5C=CC(C)=NC5=CC=C4)CC3)=C2.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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GSK-163090 dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GSK-163090 dihydrochloride
Cat. No.:
HY-14349
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