For research use only. Not for therapeutic Use.
Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity[1][2][3].
Spiramide retains affinity for 5-HT1A sites (Ki=50 nM) and also binds at dopamine D2 sites (Ki=3 nM), but possesses low affinity for dopamine D1 sites (Ki=2530 nM)[1].
AMI-193 (0.003-0.01 mg/kg; i.m.) dose-dependently decreases response rate in monkeys under a fixed-interval (FI) schedule of stimulus termination[2].
AMI-193 (0.003-0.01 mg/kg; i.m.) attenuates the discriminative-stimulus effects of cocaine in drug-discrimination experiments[2].
AMI-193 (0.003-0.01 mg/kg; i.m.) reduces response rate under a second-order schedule of i.v. self-administration of cocaine (0.1 mg/infusion)[2].
| Catalog Number | I010227 |
| CAS Number | 510-74-7 |
| Synonyms | 8-[3-(4-fluorophenoxy)propyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one |
| Molecular Formula | C22H26FN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H26FN3O2/c23-18-7-9-20(10-8-18)28-16-4-13-25-14-11-22(12-15-25)21(27)24-17-26(22)19-5-2-1-3-6-19/h1-3,5-10H,4,11-17H2,(H,24,27) |
| InChIKey | FJUKDAZEABGEIH-UHFFFAOYSA-N |
| SMILES | C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCOC4=CC=C(C=C4)F |
| Reference | [1]. Ismaiel AM, 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 Aug 20;36(17):2519-25. [2]. Czoty PW, et, al. Behavioral effects of AMI-193, a 5-HT(2A)- and dopamine D(2)-receptor antagonist, in the squirrel monkey. Pharmacol Biochem Behav. 2000 Oct;67(2):257-64. [3]. Kjellberg B, et, al. Partial restoration by a neuroleptic (spiramide) of items of grooming behaviour suppressed by amphetamine. Arch Int Pharmacodyn Ther. 1974 Jul;210(1):61-6. |
