The renin–angiotensin–aldosterone system is the well established endocrine system having significant role in preserving hemodynamic stability. Renin is secreted from the juxtaglomerular cells of the kidney. Phenylpiperazine derivatives have been reported as human renin inhibitor. To perform predictive QSAR modeling for 27 phenylpiperazine derivatives as renin enzyme inhibitors. The IC50 values ...

α1-Adrenergic receptors (α1-ARs), as one of the most important members of G protein-coupled receptors (GPCRs), can mediate lots of physiological responses of the sympathetic nervous system. Until now, α1-ARs have been divided into at least three subtypes, α1A, α1B, and α1D, which distribute in various tissues and organs. In this research, we designed and synthesized several napthalimide-based s...

Human epidermal growth factor receptor (EGFR) is an important drug target that plays a fundamental role in signal transduction pathways in oncology. We report herein the discovery of a novel class of phenylpiperazine derivatives with improved potency toward EGFR. The biological activity of compound 3p as inhibitor of EGFR was further investigated both in vitro and in vivo. Notably, compound 3p ...

Dopamine constitutes about 80% of the content of central catecholamines and has a crucial role in the etiology of several neuropsychiatric disorders, including Parkinson's disease, depression and schizophrenia. Several dopaminergic drugs are used to treat these pathologies, but many problems are attributed to these therapies. Within this context, the search for new more efficient dopaminergic a...

New arylpiperazines with a four-methylene spacer containing a terminal pyrimido[2,1-f] theophylline fragment were synthesized, and their 5-HT1A and 5-HT2A receptor affinities were determined. All these compounds displayed a high affinity for 5-HT1A receptors (Ki=0.5-21.5 nM), and low affinity for 5-HT2A ones. The results of in vivo experiments showed that compounds revealed potential agonistic ...

After discarding eight items in the Dutch translation of Livesley's DAPP-BQ that showed item-total correlations < 0.20 in a sample of 223 normal subjects. Cronbach's alpha coefficients were calculated for the remaining items in the 18 scales of this instrument. The 'Dutch' alpha coefficients proved to be satisfactory. Furthermore, the Dutch DAPP-BQ scales were factor analyzed, retaining four fa...