5-HT1A modulator 1 |
| Catalog No.GC31234 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 142477-34-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[1]. Taverne T, et al. Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. J Med Chem. 1998 Jun 4;41(12):2010-8.
Kinase experiment: | 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]. |
Animal experiment: | 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. |
References: [1]. Taverne T, et al. Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. J Med Chem. 1998 Jun 4;41(12):2010-8. | |
| Cas No. | 142477-34-7 | SDF | |
| Canonical SMILES | O=C1SC2=CC(CCN3CCN(C4=CC=CC=C4OC)CC3)=CC=C2N1C | ||
| Formula | C21H25N3O2S | M.Wt | 383.51 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6075 mL | 13.0375 mL | 26.0749 mL |
| 5 mM | 0.5215 mL | 2.6075 mL | 5.215 mL |
| 10 mM | 0.2607 mL | 1.3037 mL | 2.6075 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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