5-HT7/5-HT2A receptor antagonist 1
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases.
For research use only. We do not sell to patients.
- CAS No.: 851375-22-9
- Formula: C16H20FN3
- Molecular Weight:273.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
In Vitro
5-HT7/5-HT2A receptor antagonist 1 (Compound 4j) behaves as an antagonist at 5-HT2A with a pKB = 8.1 based on an in vitro functional assay using calcium mobilization[1].
5-HT7/5-HT2A receptor antagonist 1 is also an inverse agonist at 5-HT7 in a functional assay for 5-HT7 (cAMP, pIC50 = 7.0)
5-HT7/5-HT2A receptor antagonist 1 shows >50-fold selectivity over a panel of 50 mono-amine and peptide hormone receptors, ion channels, and neurotransmitter uptake sites[1].
5-HT7/5-HT2A receptor antagonist 1 shows in vitro affinity for the h5-HT2B and 5-HT2C receptors with pKi 7.6 and 7.3, respectively[1].
5-HT7/5-HT2A receptor antagonist 1 binds to plasma proteins was found to be below to moderate, with unbound fractions determined to be 30%fu and 20%fu in human and rat plasma, respectively[1].
The metabolic stability of 5-HT7/5-HT2A receptor antagonist 1 is high in both rat and human liver microsomes (t1/2 > 60 min)[1].
5-HT7/5-HT2A receptor antagonist 1 (10 μM) shows no inhibition of cytochrome P450 enzymes, suggesting that the potential liability for any drug-drug interactions are minimal[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Clearance (CL) | T1/2 | Tmax | Cmax |
|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 0.4 L/h | 3.4 h | / | / |
| Rat | 3 mg/kg | p.o. | 0.4 L/h | 4.3 h | 1.7 h | 190 ng/mL |
| Rat | 3 mg/kg | s.c. | 0.4 L/h | 3.9 h | 0.75 h | 260 ng/mL |
In Vivo
5-HT7/5-HT2A receptor antagonist 1 (0.03-1 mg/kg, p.o., once) is a potent central 5-HT7 receptor antagonist that blocks 5-CT-induced hypothermia in rats[1].
4J (0.001-10 mg/kg, p.o., s.c., 20min, 40 min) is an effective central 5-HT2A receptor antagonist with high oral bioavailability, exerting functional inhibitory effects in the central nervous system in mice[1].
5-HT7/5-HT2A receptor antagonist 1 (0.01-10 mg/kg, p.o., 1 h) occupies 5-HT2A receptor binding sites found in the frontal cortex area of the rat brain with an ED50 in good agreement with the ED50 value for central functional effect mediated by 5-HT2A receptor in rats (ED50 = 0.8 mg/kg)[1].
5-HT7/5-HT2A receptor antagonist 1 shows only weak activity in the blockade of phenylephrine-induced mydriasis in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats implanted with a telemetry device capable of measuring various data streams, including body temperature[1].
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
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Administration:Oral gavage, p.o. 20 min before 5-CT administration.
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Result:Showed efficacy at very low doses with an established of ED50 = 0.05 mg/kg for the blockade of induced by 5-CT hypothermia.
The maximal efficacy was observed at 0.3 mg/kg p.o., corresponding to a plasma concentration of 27 ng/ml.
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Animal Model:2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice[1].
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Dosage:0.001 mg/kg, 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg
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Administration:DOI-Induce after s.c. (20 min) or oral (60 min)
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Result:Showed efficacy at low doses with an established ED50 = 0.3 mg/kg p.o.
Chemical Information
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CAS No. 851375-22-9
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Molecular Weight 273.35
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Formula C16H20FN3
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SMILES
CC(C)N1C(C2=CC=C(F)C=C2)=C3C(CCNCC3)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5-HT7/5-HT2A receptor antagonist 1 Related Classifications
HY-134483 Related Classifications
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