《Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning》 was written by Stewart, Andrew O.; Cowart, Marlon D.; Moreland, Robert B.; Latshaw, Steve P.; Matulenko, Mark A.; Bhatia, Pramila A.; Wang, Xueqing; Daanen, Jerome F.; Nelson, Sherry L.; Terranova, Marc A.; Namovic, Marian T.; Donnelly-Roberts, Diana L.; Miller, Loan N.; Nakane, Masaki; Sullivan, James P.; Brioni, Jorge D.. Category: piperazines And the article was included in Journal of Medicinal Chemistry on April 22 ,2004. The article conveys some information:
A series of subtype selective dopamine D4 receptor ligands from the heteroarylmethylphenylpiperazine class have been discovered that exhibit a remarkable structure-activity relation (SAR), revealing a substituent effect in which regiosubstitution on the terminal arylpiperazine ring can modulate functional or intrinsic activity. Other structure-dependent efficacy studies in the dopamine D4 field have suggested a critical interaction of the heteroarylmethyl moiety with specific protein microdomains in controlling intrinsic activity. The authors studies indicate that for some binding orientations, the phenylpiperazine moiety also plays a key role in determining efficacy. These data also implicate a kinetic or efficiency term, contained within measured functional affinities for agonists, which support a sequential binding and conformational stabilization model for receptor activation. The structural similarity between partial agonist and antagonist, within this subset of ligands, and lack of bioisosterism for this substituent effect are key phenomena for these hypotheses. In the experimental materials used by the author, we found Abt-724(cas: 70006-24-5Category: piperazines)
Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics