α-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 α1– and α2-adrenoceptors were assessed. The compound with highest affinity for the α1-adrenoceptors was 1-{4-[4-(2-chloro-phenyl)-piperazin-1-yl]-butyl}-pyrrolidin-2-one I with pKi = 7.30. Compound with pKi (α1) ≥6.44 were evaluated in functional bioassays for intrinsic activity at α1A– and α1B-adrenoceptors. All compounds tested were antagonists of the α1B-adrenoceptors. Addnl., compounds II and I were α1A-adrenoceptors antagonist. The dual α1A-/α1B-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