83393-32-2Relevant academic research and scientific papers
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+
Sikazwe, Donald M. N.,Li, Shouming,Lyles-Eggleston, Margaret,Ablordeppey, Seth Y.
, p. 3779 - 3782 (2003)
We have previously proposed that haloperidol's debilitating extrapyramidal symptoms (EPS) may be associated with its quaternary BCPP+ (an MPP+ like species) metabolite formed in vivo. However, recent work on D2 knock out mice suggest
Synthesis and evaluation of ligands for D2-like receptors: The role of common pharmacophoric groups
Sikazwe, Donald M.N.,Nkansah, Nancy T.,Altundas, Ramazan,Zhu, Xue Y.,Roth, Bryan L.,Setola, Vincent,Ablordeppey, Seth Y.
experimental part, p. 1716 - 1723 (2009/08/07)
Arylcycloalkylamines, such as phenyl piperidines and piperazines and their arylalkyl substituents, constitute pharmacophoric groups exemplified in several antipsychotic agents. A review of previous reports indicates that arylalkyl substituents can improve
Synthesis and monoamine transporter affinity of 3α-arylmethoxy-3β-arylnortropanes
Kaur, Harneet,Izenwasser, Sari,Verma, Abha,Wade, Dean,Housman, Amy,Stevens, Edwin D.,Mobley, David L.,Trudell, Mark L.
supporting information; experimental part, p. 6865 - 6868 (2010/06/16)
A series of 3-arylnortrop-2-enes and 3α-arylmethoxy-3β-arylnortropanes were synthesized and evaluated for binding affinity at monoamine transporters. The 3-(3,4-dichlorophenyl)nortrop-2-ene (6e) exhibited high affinity for the SERT (Ki = 0.3 nM
Haloperidol: Towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors
Sikazwe, Donald M.N.,Li, Shouming,Mardenborough, Leroy,Cody, Vivian,Roth, Brian L.,Ablordeppey, Seth Y.
, p. 5739 - 5742 (2007/10/03)
An attempt to understand the pharmacophore-relevant position of the alcoholic moiety in haloperidol and the contributions of other pharmacophoric elements led to the re-synthesis of its tropane analogue (compound 2). An analysis of the binding data sugges
