2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. WAY 163909

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

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WAY 163909

WAY 163909 Chemical Structure

CAS No. : 428868-32-0

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WAY 163909 Related Antibodies

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Description

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

IC50 & Target[2]

5-HT2C Receptor

8 nM (EC50)

In Vitro

WAY 163909 (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 (1-10 μM) results significant depletion of in incubations with cDNA-expressed CYP2D6 but not other tested CYP isoforms[1].
WAY 163909 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.

WAY 163909 Related Antibodies
In Vivo

WAY 163909 (3-100 mg/kg; i.p., p.o.; once daily; 10 days) 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) 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) 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) 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) 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) 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.

Animal Model: Sprague-Dawley (SD) rats; obese Zuker rats; diet-induced obese mice[1]
Dosage: 3 mg/kg (acute i.p.); 30 mg/kg (acute p.o., SD rat); 3-100→75 mg/kg (chronic p.o., SD rat)
Administration: i.p. (acute); p.o. (acute, SD rat); p.o.; once daily; 10 days (chronic SD rat)
Result: Produced dose-dependent decreases in food intake, with a minimal effective dose (MED) of 3 mg/kg i.p. across all models, and an oral MED of 30 mg/kg in SD rats.
Produced dose-dependent reductions in food intake and body weight gain; by study end, mean body weights were ~101, 97.5, 88.3, and 83.1% of control for 3, 10, 30, and 100→75 mg/kg groups respectively.
Reduced triglyceride levels by ~40 and ~54% at 30 and 100→75 mg/kg, respectively, at study end.
Animal Model: Sprague-Dawley (SD) rats; Wistar-Kyoto (WKY) rats; rats (resident-intruder, learned helplessness, olfactory bulbectomy models)[1]
Dosage: 10 mg/kg (i.p., forced swim test); 0.3 mg/kg (s.c., resident-intruder model); 30 mg/kg/day (i.p., learned helplessness model); 3 mg/kg (i.p., olfactory bulbectomy model)
Administration: i.p.; s.c.; once daily; 5 days (learned helplessness, olfactory bulbectomy); once daily; 21 days (olfactory bulbectomy)
Result: Significantly decreased immobility with an MED of 10 mg/kg i.p. in SD and WKY rats; in SD rats, increased swimming without affecting climbing, and effects in WKY rats were reversed by a 5-HT2C/2B receptor antagonist.
Selectively reduced aggressive behavior with an MED of 0.3 mg/kg s.c., with no motor impairment.
Produced dose-dependent decreases in escape latency and escape failures in learned helplessness model.
Effectively decreased hyperactivity in bulbectomized rats without affecting activity in sham-operated rats following both 5-day and 21-day treatment.
Animal Model: Wistar (male, 300-350 g at study start; resident rats from Charles River UK, intruder rats from Bath University stock)[2]
Dosage: 0.33 mg/kg; 1.0 mg/kg; 3.0 mg/kg
Administration: s.c.; single dose 30 min pre-test
Result: Significantly reduced aggressive behavior at all three doses (p<0.05 for all).
Achieved an ID50 of 0.33 mg/kg s.c. for aggression reduction (95% CI: 0.055-0.719 mg/kg s.c.).
Achieved an ID50 of 0.967 mg/kg s.c. for reducing total behaviors (95% CI: 0.755-1.234 mg/kg s.c.).
Significantly affected investigation, sexual behavior, and flight escape behaviors at 1 or 3 mg/kg.
Molecular Weight

214.31

Formula

C14H18N2
CAS No.
SMILES

[H][C@@]12[C@@](N3CCNCC4=CC=CC2=C43)([H])CCC1
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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WAY 163909 Related Classifications

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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.

Keywords:

WAY 163909428868-32-0WAY163909WAY-1639095-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorrodent obesity modelshuman peripheral blood lymphocytes5-HT2B receptorsSD rats5-HT2A receptors5-HT2C receptorCYP2D6olfactory bulbectomy modelhuman liver microsomesWKY ratsInhibitorinhibitorinhibit

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