1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. WAY 163909 (hydrochloride)

WAY 163909 hydrochloride is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 hydrochloride exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 hydrochloride induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 hydrochloride alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 hydrochloride can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.

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WAY 163909 (hydrochloride)

WAY 163909 (hydrochloride) Chemical Structure

CAS No. : 428868-35-3

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Description

WAY 163909 hydrochloride is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 hydrochloride exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 hydrochloride induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 hydrochloride alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 hydrochloride can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia[1][2][3].

IC50 & Target

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

5-HT7 Receptor

 

In Vitro

WAY 163909 hydrochloride (1-10 μM) has high metabolic clearance in dogs, moderate clearance in rats and monkeys, and low clearance in human liver microsomes, with no meaningful metabolism by small intestinal microsomes across tested species[1].
WAY 163909 hydrochloride (1-10 μM) results significant depletion of in incubations with cDNA-expressed CYP2D6 but not other tested CYP isoforms[1].
WAY 163909 hydrochloride is not mutagenic in the Ames assay and does not induce chromosomal aberrations in human peripheral blood lymphocytes[1].

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

In Vivo

WAY 163909 (3-100 mg/kg; i.p., p.o.; once daily; 10 days) hydrochloride produces dose-dependent reductions in food intake and body weight gain in rodent obesity models, with significant triglyceride-lowering effects at higher chronic doses[1].
WAY 163909 (0.1-30 mg/kg; i.p., p.o., s.c.; once daily; 21 days) hydrochloride exhibits atypical antipsychotic-like activity in rodent models, with selective effects on mesolimbic dopamine pathways and no extrapyramidal side effect liability up to 30 mg/kg i.p[1].
WAY 163909 (10 mg/kg; i.p.; three time points: 15 min post-pretest, 5 h pre-test, 1 h pre-test) hydrochloride reduces immobility and increases swimming behavior in SD rats in the forced swim test, mirroring the profile of SSRIs[2].
WAY 163909 (0.33-3.0 mg/kg; s.c.; single dose 30 min pre-test) hydrochloride selectively reduces aggressive behavior in resident rats in the resident-intruder model, with an ID50 of 0.33 mg/kg s.c[2].
WAY 163909 (10 mg/kg; i.p.; daily; 14 days) hydrochloride reduces noncontact penile erections in male SD rats, indicating sexual dysfunction liability at doses higher than those needed for antidepressant-like effects[2].
WAY 163909 (0.3-3 mg/kg; i.p.; single injection; 15 minutes pre-ketamine) hydrochloride pretreatment at 1 mg/kg and 3 mg/kg significantly attenuates ketamine-induced hypothermia in male Swiss-Webster mice via activation of 5-HT2C receptors, with the 1 mg/kg dose being the most effective[3].

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

Molecular Weight

250.77

Formula

C14H19ClN2

CAS No.
SMILES

[H][C@@]1(CCC2)[C@@]2([H])C3=CC=CC4=C3N1CCNC4.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
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  • 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:
WAY 163909 (hydrochloride)
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HY-15401A
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