伪-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one was written by Zareba, Paula;Dudek, Magdalena;Lustyk, Klaudia;Siwek, Agata;Starowicz, Gabriela;Bednarski, Marek;Nowinski, Leszek;Razny, Katarzyna;Sapa, Jacek;Malawska, Barbara;Kulig, Katarzyna. And the article was included in Bioorganic & Medicinal Chemistry in 2015.SDS of cas: 27469-60-9 This article mentions the following:
This study focused on a series of pyrrolidin-2-one derivatives connected via two or four methylene units to arylpiperazine fragment. The compounds obtained for 伪1– and 伪2-adrenoceptors were assessed. The compound with highest affinity for the 伪1-adrenoceptors was 1-{4-[4-(2-chloro-phenyl)-piperazin-1-yl]-butyl}-pyrrolidin-2-one I with pKi = 7.30. Compound with pKi (伪1) 鈮?.44 were evaluated in functional bioassays for intrinsic activity at 伪1A– and 伪1B-adrenoceptors. All compounds tested were antagonists of the 伪1B-adrenoceptors. Addnl., compounds II and I were 伪1A-adrenoceptors antagonist. The dual 伪1A-/伪1B-adrenoceptors antagonists, compounds II and I were also tested in vivo for their hypotensive activity in rats. These compounds, when dosed of 1.0 mg/kg iv in normotensive, anesthetized rats, significantly decreased systolic and diastolic pressure and their hypotensive effects lasted for longer than one hour. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9SDS of cas: 27469-60-9).
4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.SDS of cas: 27469-60-9
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics