Nitrile is any organic compound with a −C≡N functional group. 105-34-0, formula is C4H5NO2, Name is Methyl 2-cyanoacetate.The prefix cyano- is used interchangeably with the term nitrile in literature. Electric Literature of 105-34-0.
Pedersen, Mie Fabricius;Wrobel, Tomasz Marcin;Marcher-Roersted, Emil;Pedersen, Daniel Sejer;Moeller, Thor Christian;Gabriele, Federica;Pedersen, Henrik;Matosiuk, Dariusz;Foster, Simon Richard;Bouvier, Michel;Brauner-Osborne, Hans research published 《 Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics》, the research content is summarized as follows. Here we provide a comprehensive kinetic pharmacol. comparison of clin. relevant μ-opioid receptor agonists, including the novel biased agonist oliceridine (TRV130) which is in clin. trial for pain management. We demonstrate that the bias profile observed for the selected agonists is not time-dependent and that agonists with dramatic differences in their binding kinetic properties can display the same degree of bias. Binding kinetics analyses demonstrate that buprenorphine has 18-fold higher receptor residence time than oliceridine. This is thus the largest pharmacodynamic difference between the clin. approved drug buprenorphine and the clin. candidate oliceridine, since their bias profiles are similar. Further, we provide the first pharmacol. characterization of (S)-TRV130 demonstrating that it has a similar pharmacol. profile as the (R)-form, oliceridine, but displays 90-fold lower potency than the (R)-form. This difference is driven by a significantly slower association rate. GRK2 and GRK5 overexpression greatly increased μ-opioid receptor internalization induced by morphine, but only had modest effects on buprenorphine and oliceridine-induced internalization. Overall, our data reveal that the clin. available drug buprenorphine displays a similar pharmacol. bias profile in vitro compared to the clin. candidate drug oliceridine and that this bias is independent of binding kinetics suggesting a mechanism driven by receptor-conformations.
105-34-0, Methyl cyanoacetate is an alkyl cyanoacetate ester.
Methyl cyanoacetate is the intermediate product in pharmaceutical organic synthesis as well as in the synthesis of some biologically active compounds used in agriculture. It undergoes calcite or fluorite catalyzed Knövenagel condensation with aromatic aldehydes, giving the corresponding arylidenemalononitriles and (E)-α -cyanocinnamic esters.
Methyl Cyanoacetate is often used as a nucleophile in the electrochemical oxidation of catechols. Methyl Cyanoacetate is also a reagent in the synthesis of Methyl 2-Amino-4-trifluoromethylthiophene-3-carboxylate (M287290); a compound used in the synthesis of DPP-IV inhibitors for treating type 2 diabetes., Electric Literature of 105-34-0
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts