[HTML][HTML] The Clinically-tested S1P Receptor Agonists, FTY720 and BAF312, Demonstrate Subtype-Specific Bradycardia (S1P1) and Hypertension (S1P3) in Rat

…, RR Chen, KE Harrington, RM Dinallo… - PLoS …, 2012 - journals.plos.org
Sphingosine-1-phospate (S1P) and S1P receptor agonists elicit mechanism-based effects
on cardiovascular function in vivo. Indeed, FTY720 (non-selective S1P X receptor agonist) …

G protein–coupled bile acid receptor 1 stimulation mediates arterial vasodilation through a KCa1. 1 (BKCa)–dependent mechanism

…, A Muthukumarana, KE Gilpin, RM Dinallo… - … of Pharmacology and …, 2014 - ASPET
Bile acids (BAs) and BA receptors, including G protein–coupled bile acid receptor 1 (GPBAR1),
represent novel targets for the treatment of metabolic and inflammatory disorders. …

Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees

PS Riska, DP Joseph, RM Dinallo, WC Davidson… - Drug metabolism and …, 1999 - ASPET
The study objectives were to characterize the metabolism of nevirapine (NVP) in mouse, rat,
rabbit, dog, monkey, and chimpanzee after oral administration of carbon-14-labeled or -…

Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors

…, SN Mazurek, KE Harrington, RM Dinallo… - … of Pharmacology and …, 2012 - ASPET
We previously reported the discovery of a novel ribosomal S6 kinase 2 (RSK2) inhibitor, (R)-5-Methyl-1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]
indole-8-carboxylic acid [1-(3-…

Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore

…, J Bentzien, RM Dinallo, D Souza, RM Nelson… - Bioorganic & Medicinal …, 2014 - Elsevier
Synthesis and structure–activity relationship (SAR) of a series of alkyl and cycloalkyl containing
non-steroidal dissociated glucocorticoid receptor (GR) agonists is reported. This series …

Strategic integration of in vivo cardiovascular models during lead optimization: predictive value of 4 models independent of species, route of administration, and …

…, RR Chen, KE Harrington, RM Dinallo… - Journal of …, 2012 - journals.lww.com
The strategic integration of in vivo cardiovascular models is important during lead optimization
to enable a wide therapeutic index for cardiovascular safety. However, under what …

BIRM 270: a novel inhibitor of arachidonate release that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils.

…, P Borgeat, M Nadeau, G Hansen, RM Dinallo… - … of Pharmacology and …, 1994 - ASPET
(S)-N-[2-Cyclohexyl-1-(2-pyridinyl)ethyl]-5-methyl-2-benzoxazolamine+ ++ (BIRM 270) was
identified as a potent and enantiomerically selective inhibitor of calcium ionophore A23187-…

Improved thermospray accurate mass measurement using a magnetic sector instrument

WC Davidson, RM Dinallo… - Biological mass …, 1991 - Wiley Online Library
A method permitting accurate mass measurement of full‐scan thermospray mass spectra is
presented. Improved resolution and sensitivity were achieved by the addition of source …

The characterization of synthetic by‐products by B/E linked scanning and high‐resolution thermospray mass spectrometry

RM Dinallo, WC Davidson… - Biological mass …, 1991 - Wiley Online Library
Abstract Characterization of unknown synthetic by‐products from a test synthesis of the
experimental inhibitor of HIV‐1 reverse transcriptase, BI‐RG‐587, is presented. Seven impurities …

Mitigation of Off Target Adrenergic Inhibition and Effects on Cardiovascular Function in the Discovery Novel RSK2 Inhibitors

…, SN Mazurek, KE Harrington, RM Dinallo… - … of Pharmacology and …, 2011 - ASPET
We previously reported the discovery of a novel RSK2 inhibitor, BIX 02565, with high potency
(IC50=1.1 nM) targeted for the treatment of heart failure. In the present study we report that …