1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Nelotanserin

Nelotanserin (Synonyms: APD125)

Cat. No.: HY-10559 Purity: 99.79%
Handling Instructions

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

For research use only. We do not sell to patients.

Nelotanserin Chemical Structure

Nelotanserin Chemical Structure

CAS No. : 839713-36-9

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Based on 1 publication(s) in Google Scholar

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Description

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

IC50 & Target

5-HT2A Receptor

1.7 nM (IC50)

5-HT2C Receptor

79 nM (IC50)

5-HT2B Receptor

791 nM (IC50)

In Vitro

Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT2A full inverse agonist (IC50=1.7 nM), a moderately potent 5-HT2C partial inverse agonist (IC50=79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT2B inverse agonist (IC50=791 nM). Nelotanserin displays high affinity for recombinant human 5-HT2A receptors (Ki=0.35 nM), moderate affinity for human 5-HT2C receptors (Ki=100 nM), and low affinity for human 5-HT2B receptors (2000 nM) stably expressed in HEK293 cells. The results suggest that Nelotanserin has a 262-fold higher affinity for human 5-HT2A than 5-HT2C receptors and a 6610-fold higher affinity for human 5-HT2A than 5-HT2B receptors[1].

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

In Vivo

Each compound is tested in a minimum of five rats by oral gavage with administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that persist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the number of NREM bouts decrease during the first hour for Nelotanserin (p<0.01) as well as for compound 15 (p<0.05)[2].

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

Clinical Trial
Molecular Weight

437.24

Formula

C₁₈H₁₅BrF₂N₄O₂

CAS No.

839713-36-9

SMILES

COC1=C(C2=C(Br)C=NN2C)C=C(NC(NC3=C(F)C=C(F)C=C3)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (73.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2871 mL 11.4354 mL 22.8707 mL
5 mM 0.4574 mL 2.2871 mL 4.5741 mL
10 mM 0.2287 mL 1.1435 mL 2.2871 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.79%

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Keywords:

NelotanserinAPD125APD 125APD-1255-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Nelotanserin
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