Kumar, Vivek published the artcileSynthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R), Safety of 1-(3-Cyanophenyl)piperazine, the publication is Journal of Medicinal Chemistry (2017), 60(4), 1478-1494, database is CAplus and MEDLINE.
The development of bitopic ligands directed toward D2-like receptors has proven to be of particular interest to improve the selectivity and/or affinity of these ligands and as an approach to modulate and bias their efficacies. The structural similarities between dopamine D3 receptor (D3R)-selective mols. that display bitopic or allosteric pharmacol. and those that are simply competitive antagonists are subtle and intriguing. Herein the authors synthesized a series of mols. in which the primary and secondary pharmacophores were derived from the D3R-selective antagonists SB269,652 and SB277011A whose structural similarity and pharmacol. disparity provided the perfect templates for SAR investigation. Incorporating a trans-cyclopropylmethyl linker between pharmacophores and manipulating linker length resulted in the identification of two bivalent noncompetitive D3R-selective antagonists, I and II, which further delineates SAR associated with allosterism at D3R and provides leads toward novel drug development.
Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Safety of 1-(3-Cyanophenyl)piperazine.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics