1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. 5-HT1A modulator 1

5-HT1A modulator 1 

Cat. No.: HY-100290
Handling Instructions

5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

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

5-HT1A modulator 1 Chemical Structure

5-HT1A modulator 1 Chemical Structure

CAS No. : 142477-34-7

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Description

5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

IC50 & Target[1]

sPLA2

2 nM (IC50)

5-HT1B Receptor

300 nM (IC50)

5-HT2A Receptor

500 nM (IC50)

5-HT2C Receptor

4000 nM (IC50)

α1 receptor

10 nM (IC50)

D2 receptor

40 nM (IC50)

In Vitro

5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT1B, 5-HT2A and 5-HT2C receptor with IC50s of 300±55 nM, 500±75 nM, and 4000±440 nM, respectively[1].

In Vivo

5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01)[1].

Molecular Weight

383.51

Formula

C₂₁H₂₅N₃O₂S

CAS No.

142477-34-7

SMILES

O=C1SC2=CC(CCN3CCN(C4=CC=CC=C4OC)CC3)=CC=C2N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[1]

Binding is determined using membranes prepared from bovine hippocampus. The receptor is labeled with 0.5 nM [3H]-8-hydroxydipropylaminotetralin (8-OH-DPAT) by incubation at 25°C for 30 min with 11 concentrations of the test compounds (1-105 nM). Nonspecific binding is determined using 10-5 Mbuspirone. Competition experiments are analyzed using the iterative nonlinear least-squares curve-fitting program Inplot 4, graphpad; IC50 values are calculated using the Cheng-Prusoff equation[1].

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

Animal Administration
[1]

Rats[1]
Wistar rats (n=6) are used. 5-HT1A modulator 1 is tested at pharmacological doses (1 and 2 mg/kg ip, respectively) and at high doses (32 and 64 mg/kg ip) in rats. The intensity of forepaw treading is expressed as percentage of the maximal possible score. The 5HT1A agonist 8-OH-DPAT induces forepaw treading and is used as a reference compound.
Mice[1]
Swiss mice are injected with the test compound (e.g., 5-HT1A modulator 1, 0.25 and 1 mg/kg ip) before an injection of 5HTP (400 mg/kg ip). The number of head twiches occurring in a 10 min period starting 10 min after the injection of 5HTP is counted. Cyproheptadine is used as reference compound.

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

References
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Keywords:

5-HT1A modulator 15-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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