Chambers, Mark S. published the artcileSpiropiperidines as high-affinity, selective σ ligands., HPLC of Formula: 137419-24-0, the main research area is spiropiperidine selective sigma ligand; tetralin spiropiperidino selective sigma ligand; indan spiropiperidino selective sigma ligand; benzocycloheptane spiropiperidino selective sigma ligand; radioligand displacement spiropiperidinobenzocycloalkane; structure activity spiropiperidinobenzocycloalkane receptor binding.
A variety of achiral conformationally restricted spirocyclic piperidines were prepared in an attempt to investigate the functional role of the central σ recognition site. All compounds possessed a lipophilic N-substituent incorporating either a tetralin (I; n = 2, R = PhCH2, Bu, hexyl, 2-picolyl, cyclohexylmethyl, CH2CH:CH2, 2-furylmethyl, 2-thienylmethyl, CH2CH:CMe2, etc.), indan (I; n = 1, R = PhCH2, PhCH2CH2, CH2CH:CMe2, Bu, etc.), or benzocycloheptane skeleton (I; n = 3, R = PhCH2, Bu). Their in vitro affinity at the σ site was assessed in radioligand displacement experiments with guinea pig cerebellum homogenates using the σ-specific radioligand N,N-di-o-[5-3H]-tolylguanidine (II). A study of the structure-activity relationships identified the N-Bu and N-dimethylallyl substituents as the optimum groups for high affinity and selectivity at the σ site, e.g., I (n = 1, R = CH2CH:CMe2), pIC50 = 8.9 vs II and >10,000-fold selective over the dopamine D2 receptor. Such compounds are amongst the highest affinity σ ligands reported to date, with excellent selectivity over the dopamine D2 receptor, and may serve as a useful tool for exploring the physiol. role of the σ site.
Journal of Medicinal Chemistry published new progress about Antipsychotics. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, HPLC of Formula: 137419-24-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem