| Identification | Back Directory | [Name]
AMI-193 | [CAS]
510-74-7 | [Synonyms]
R 5808
AMI-193
spiramide
Fluroxyspiramine
8-[3-(4-FLUOROPHENOXY)PROPYL]-1-PHENYL-1,3,8-TRIAZASPIRO[4.5]-DECANONE
8-[3-(4-FLUOROPHENOXY)PROPYL]-1-PHENYL-1,3,8-TRIAZASPIRO[4.5]DECAN-4-ONE
1-Phenyl-8-[3-(4-fluorophenoxy)propyl]-1,3,8-triazaspiro[4.5]decane-4-one
1,3,8-Triazaspiro[4.5]decan-4-one, 8-[3-(4-fluorophenoxy)propyl]-1-phenyl- | [Molecular Formula]
C22H26FN3O2 | [MDL Number]
MFCD00673878 | [MOL File]
510-74-7.mol | [Molecular Weight]
383.46 |
| Chemical Properties | Back Directory | [Melting point ]
176 - 179°C | [storage temp. ]
Store at RT | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
White solid. | [color ]
Off-White to Pale Yellow |
| Hazard Information | Back Directory | [Uses]
AMI-193 is a selective 5-HT2A and D2DR receptor antagonist. Endoplasmic reticulum (ER) stress inducer; Also, it is derived from 4-Fluorophenol (F595325), which is a fluorinated phenolic compound with various applications as an starting reagent for the synthesis of pharmaceutical goods. | [Definition]
ChEBI: An azaspiro compound that consists of 1,3,8-triazaspiro[4.5]decan-4-one having a phenyl group attached to N-1 and a 3-(4-fluorophenoxy)propyl attached to N-8. Selective 5-HT antagonist, which binds to 5-HT2 sites as potently as spipero
e but has lower affinity for 5-HT2C receptors. Also a high affinity D2 receptor antagonist (Ki = 3 nM). Lacks the disruptive effect of spiperone on animal behaviour. | [Biological Activity]
Selective 5-HT antagonist, which binds to 5-HT 2 sites as potently as spiperone but has lower affinity for 5-HT 2C receptors. Also a high affinity D 2 receptor antagonist (K i = 3 nM). Lacks the disruptive effect of spiperone on animal behavior. | [in vivo]
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]. | Animal Model: | Adult male squirrel monkeys (850-1300 g)[2] | | Dosage: | 0.003, 0.01 mg/kg | | Administration: | I.m. on Tuesday, Wednesday, and Thursday the following week | | Result: | Decreased the response rate.
The rate-decreasing effects were reversed by cocaine.
|
| [IC 50]
5-HT2 Receptor: 2 nM (Ki); D2 Receptor: 3 nM (Ki); 5-HT1A Receptor: 50 nM (Ki); D1 Receptor: 2530 nM (Ki); 5-HT1C Receptor: 4300 nM (Ki) | [storage]
Store at RT | [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. |
|
| Company Name: |
Shaanxi Dideu Medichem Co. Ltd
|
| Telephone: |
+86-29-87569266 +86-17392581500 |
| Website: |
https://www.chemicalbook.com/manufacturer/shaanxi-dideu-medichem-220/ |
| Company Name: |
Energy Chemical
|
| Telephone: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|