Recommanded Product: tert-Butyl 2-cyanoacetate. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: tert-Butyl 2-cyanoacetate, is researched, Molecular C7H11NO2, CAS is 1116-98-9, about The GABAB receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Author is Ferlenghi, Francesca; Maccioni, Paola; Mugnaini, Claudia; Brizzi, Antonella; Fara, Federica; Mostallino, Rafaela; Paola, Castelli M.; Colombo, Giancarlo; Mor, Marco; Vacondio, Federica; Corelli, Federico.
We report an in vitro phase I metabolism study on COR659 (1), a 2-acylaminothiophene derivative able to suppress alc. and chocolate self-administration in rats, likely via pos. allosteric modulation of the GABAB receptor and antagonism/inverse agonism at the cannabinoid CB1 receptor. High performance liquid chromatog. coupled to tandem and high resolution mass spectrometry was employed for the characterization of in vitro metabolism and in vivo pharmacokinetics of COR659 in rats. In vitro [35S]GTPĪ³S binding assays on stimulated GABAB and CB1 receptors, in combination with alc. and chocolate self-administration experiments in rats, were employed to assess the pharmacol. profile of this novel set of analogs, using COR659 as reference compound Eight metabolites of COR659 were discovered in liver microsomal incubates; two of them (M1, M2) were identified by comparison with synthetic reference standards In the novel set of COR659 analogs, those bearing branched alkyl substituents on the ester group, showed an improved in vitro metabolic stability (2-4), had an in vitro GABAB PAM (2-4) and/or CB1 partial agonist/antagonist profile (2-3) and maintained the ability to reduce alc. (2-4) and/or chocolate (4) self-administration in rats. Both PK and PD data ruled out any involvement of metabolite M1 in the in vivo potency of COR659 and 4. The present results, therefore, highlight the importance to design and synthesize novel compounds endowed with the dual activity profile and devoid of metabolic liabilities.
Although many compounds look similar to this compound(1116-98-9)Recommanded Product: tert-Butyl 2-cyanoacetate, numerous studies have shown that this compound(SMILES:O=C(OC(C)(C)C)CC#N), has unique advantages. If you want to know more about similar compounds, you can read my other articles.
Reference:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem