510-74-7 Usage
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.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 510-74-7 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 5,1 and 0 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 510-74:
(5*5)+(4*1)+(3*0)+(2*7)+(1*4)=47
47 % 10 = 7
So 510-74-7 is a valid CAS Registry Number.
InChI:InChI=1/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)
510-74-7Relevant articles and documents
Target-specific ligands and gadolinium-based complexes for imaging of dopamine receptors: Synthesis, binding affinity, and relaxivity
Zigelboim, Isaac,Weissberg, Avi,Cohen, Yoram
, p. 7001 - 7012 (2013/08/23)
Magnetic resonance imaging (MRI) and positron emission tomography (PET) are two extremely important imaging modalities with unlimited tissue penetration. Molecular imaging is a field by which specific targets or biological processes are imaged. MRI, which is used for functional imaging and for the diagnosis of a broad range of pathologic conditions, suffers from limited specificity and intrinsically low sensitivity. One possibility to alleviate partially these limitations is to use contrast agents (CAs) and more importantly target-specific CAs. We have developed a modular synthesis of novel ligands and gadolinium(III)-based target-specific MRI CAs with high relaxivity and high binding affinity toward the dopamine receptors. The prepared ligands and MRI CAs are based on spiperone as targeting moiety. The prepared target-specific CAs can potentially be used for in vitro and possibly in vivo MR imaging of dopaminergic receptors. Importantly the ligands prepared using the modular approach presented in this paper may also be useful for other imaging modalities such as PET (or SPECT) by just replacing, at the last stage of the synthesis, the gadolinium cation by other metal cations having relatively long half-lives, such as 64Cu, 89Zr, 11In, and more.
