title: Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.
abstract: Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer's disease, Parkinson's disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective molecules that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel negative allosteric modulators of human α4β2 (Hα4β2) and human α3β4 (Hα3β4) nicotinic receptors. The effects of novel sulfonylpiperazine analogues that act as negative allosteric modulators on both Hα4β2 nAChRs and Hα3β4 nAChRs were investigated. This work, through structure-activity relationship (SAR) studies, describes the chemical features of these molecules that are important for both potency and selectivity on Hα4β2 nAChRs.
authors: Division of Pharmacology, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210, United States.
authors: Brandon J
authors: BJ
authors: Henderson
authors: Daniel J
authors: DJ
authors: Carper
authors: Tatiana F
authors: TF
authors: González-Cestari
authors: Bitna
authors: B
authors: Yi
authors: Kiran
authors: K
authors: Mahasenan
authors: Ryan E
authors: RE
authors: Pavlovicz
authors: Martin L
authors: ML
authors: Dalefield
authors: Robert S
authors: RS
authors: Coleman
authors: Chenglong
authors: C
authors: Li
authors: Dennis B
authors: DB
authors: McKay
mesh_terms: D000494:Allosteric Regulation; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D006801:Humans; D009474:Neurons / Q000378:metabolism*; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D010879:Piperazines; D011978:Receptors, Nicotinic; D013450:Sulfones; C403530:nicotinic receptor alpha3beta4; C403531:nicotinic receptor alpha4beta2; D002118:Calcium