[HTML][HTML] On the discovery and development of pimavanserin: a novel drug candidate for Parkinson's psychosis

U Hacksell, ES Burstein, K McFarland, RG Mills… - Neurochemical …, 2014 - Springer
Parkinson’s disease psychosis (PDP) is a condition that may develop in up to 60 % of
Parkinson’s patients, and is a major reason for nursing home placement for those affected. There …

Pharmacology of N-desmethylclozapine

J Lameh, ES Burstein, E Taylor, DM Weiner… - Pharmacology & …, 2007 - Elsevier
Currently available treatments for schizophrenia have limited efficacy and are generally poorly
tolerated. However, among these antipsychotic agents, clozapine stands apart in having …

The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine

…, M Lee, AI Levey, U Hacksell, ES Burstein… - …, 2004 - Springer
Rationale Clozapine is a unique antipsychotic, with efficacy against positive symptoms in
treatment-resistant schizophrenic patients, and the ability to improve cognition and treat the …

5-hydroxytryptamine2A receptor inverse agonists as antipsychotics

DM Weiner, ES Burstein, N Nash, GE Croston… - … of Pharmacology and …, 2001 - ASPET
We have used a cell-based functional assay to define the pharmacological profiles of a wide
range of central nervous system active compounds as agonists, competitive antagonists, …

Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl) carbamide (2R, 3R) …

…, F Piu, HH Schiffer, TR Ott, ES Burstein… - … of Pharmacology and …, 2006 - ASPET
The in vitro and in vivo pharmacological properties of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide
(2R,3R)-…

Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial …

ES Burstein, J Ma, S Wong, Y Gao, E Pham… - … of Pharmacology and …, 2005 - ASPET
Drugs that antagonize D 2 -like receptors are effective antipsychotics, but the debilitating
movement disorder side effects associated with these drugs cannot be dissociated from …

Discovery of an Ectopic Activation Site on the M1Muscarinic Receptor

…, N Skjærbæk, TL Messier, EA Currier, ES Burstein… - Molecular …, 2002 - ASPET
Receptors have well-conserved regions that are recognized and activated by hormones and
neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native …

Trazodone kinetics: effect of age, gender, and obesity

DJ Greenblatt, H Friedman, ES Burstein… - Clinical …, 1987 - Wiley Online Library
Single 25 mg intravenous and 50 mg oral doses of trazodone were given to 43 healthy subjects,
divided into young men and women (aged 18 to 40 years) and elderly men and women (…

Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson's disease

…, JN Ma, R Olsson, ES Burstein - ACS chemical …, 2013 - ACS Publications
Nurr1 is a nuclear hormone receptor (NucHR) strongly implicated in the growth, maintenance,
and survival of dopaminergic neurons. Nurr1 may be unable to bind ligands directly, but it …

[HTML][HTML] The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein coupling

ES Burstein, TA Spalding, MR Brann - Journal of Biological Chemistry, 1998 - ASBMB
We have completed a systematic search of the intracellular loops of a muscarinic acetylcholine
receptor for domains that govern G-protein coupling. A unique feature of the second …