2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2A&5-HT2C agonist-3

5-HT2A&5-HT2C agonist-3 (compound 4e) is an orally bioavailable and blood-brain barrier penetrant agonist of 5-HT2A and 5-HT2C. 5-HT2A&5-HT2C agonist-3 increases intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used for the research of neuropsychiatric disorders.

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5-HT2A&5-HT2C agonist-3

5-HT2A&5-HT2C agonist-3 Chemical Structure

CAS No. : 3082429-35-1

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5-HT2A&5-HT2C agonist-3 Related Antibodies

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Description

5-HT2A&5-HT2C agonist-3 (compound 4e) is an orally bioavailable and blood-brain barrier penetrant agonist of 5-HT2A and 5-HT2C. 5-HT2A&5-HT2C agonist-3 increases intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used for the research of neuropsychiatric disorders[1].

In Vitro

5-HT2A&5-HT2C agonist-3 (compound 4e) acts as a selective partial agonist at human 5-HT2A and 5-HT2C receptors expressed in CHO-K1 cells, with no measurable efficacy at 5-HT2B receptors, exhibiting a pEC50 of 7.79 at 5-HT2A and 7.10 at 5-HT2C[1].

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

5-HT2A&5-HT2C agonist-3 Related Antibodies
Parmacokinetics
Species Dose Route AUC Cmax Tmax
Mice[1] 20 mg/kg p.o. 8903 ng·h/mL 5426 ng/mL 0.25 h
In Vivo

5-HT2A&5-HT2C agonist-3 (compound 4e) (3 mg/kg; p.o.; single dose) induces significantly attenuated psychedelic-like head-twitch responses in male C57BL/6 mice relative to psilocybin at an equivalent 3 mg/kg oral dose[1].

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

Animal Model: C57BL/6 (male)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose
Result: Induced a significantly lower total number of head-twitch responses compared to both 1 mg/kg and 3 mg/kg doses of psilocybin.
Did not elicit an early peak response; instead, showed a delayed and attenuated profile, with a modest increase in head-twitch responses observed primarily in intermediate and later 10-minute intervals of the 45-minute observation period.
Molecular Weight

365.78

Formula

C15H19ClF3N3O2
CAS No.
SMILES

C[NH+](C)CCC1=CNC2=CC=CC(OC(NCC(F)(F)F)=O)=C21.[Cl-]
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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5-HT2A&5-HT2C agonist-3 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.

Keywords:

5-HT2A&5-HT2C agonist-33082429-35-15-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorS9 fractionshuman plasmaCHO-K1 cellsmale C57BL/6 mice5-HT2C receptorshuman liver microsomes5-HT2B receptors5-HT2A receptorsneuropsychiatric conditionspsilocinInhibitorinhibitorinhibit

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