AMI-193
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.
Physical Appearance | White solid |
Storage | Store at RT |
M.Wt | 383.46 |
Cas No. | 510-74-7 |
Formula | C22H26FN3O2 |
Solubility | <28.76mg/ml in DMSO |
Chemical Name | 8-(3-(4-fluorophenoxy)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one |
SDF | Download SDF |
Canonical SMILES | FC1=CC=C(C=C1)OCCCN2CC[C@]3(CC2)N(C4=CC=CC=C4)CNC3=O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet