AMI-193 |
Catalog No.GC16049
One-Click Copy Product Info
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AMI-193 (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 510-74-7
Sample solution is provided at 25 µL, 10mM.
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AMI-193 is a potent and selective antagonist of 5-HT2A receptor and dopamine D2-receptor with Ki values of 2 and 3 nM, respectively [1].
The 5-HT2A receptor is a G protein-coupled receptor and a subtype of the 5-HT2 receptor. The 5-HT2A receptor plays an important role in the spread of the human polyoma virus. The dopamine D2-receptor is a G protein-coupled receptor that inhibits adenylyl cyclase activity.
AMI-193 is a potent and selective 5-HT2A receptor and dopamine D2-receptor antagonist. AMI-193 was highly selective for 5-HT2A versus 5-HT2C receptor with Ki values of 2 and 4300 nM for 5-HT2A and 5-HT2C receptor, respectively [1]. Also, AMI-193 bound to 5-HT2 receptor with Ki value of 2 nM and exhibited >2000-fold selectivity versus 5-HT1C receptor. In cortical slices, AMI-193 (10-10 - 10-5 M) inhibited GABA release in a dose-dependent way and increased 5-HT outflow [3].
In rats, AMI-193 behaved as an antagonist with ED50 value of 0.003 mg/kg [2].
References:
[1]. Czoty PW, Howell LL. Behavioral effects of AMI-193, a 5-HT(2A)- and dopamine D(2)-receptor antagonist, in the squirrel monkey. Pharmacol Biochem Behav, 2000, 67(2): 257-264.
[2]. Ismaiel AM, De Los Angeles J, Teitler M, et al. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. J Med Chem, 1993, 36(17): 2519-2525.
[3]. Luparini MR, Garrone B, Pazzagli M, et al. A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone. Prog Neuropsychopharmacol Biol Psychiatry, 2004, 28(7): 1117-1127.
| Cas No. | 510-74-7 | SDF | |
| Chemical Name | 8-(3-(4-fluorophenoxy)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one | ||
| Canonical SMILES | FC1=CC=C(C=C1)OCCCN2CC[C@]3(CC2)N(C4=CC=CC=C4)CNC3=O | ||
| Formula | C22H26FN3O2 | M.Wt | 383.46 |
| Solubility | <28.76mg/ml in DMSO | Storage | Store at RT |
| 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 | 2.6078 mL | 13.0392 mL | 26.0783 mL |
| 5 mM | 521.6 μL | 2.6078 mL | 5.2157 mL |
| 10 mM | 260.8 μL | 1.3039 mL | 2.6078 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)