Valerie J Whiterock
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Explore the profile of Valerie J Whiterock including associated specialties, affiliations and a list of published articles.
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8
Citations
38
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Recent Articles
1.
Luo G, Jiang X, Chen L, Conway C, Gulianello M, Kostich W, et al.
Bioorg Med Chem Lett
. 2021 May;
43:128077.
PMID: 33932522
In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available azepinone derivatives that unfortunately also exhibited the unwanted property of potent...
2.
Mercer S, Chaturvedula P, Conway C, Cook D, Davis C, Pin S, et al.
Bioorg Med Chem Lett
. 2020 Oct;
31:127624.
PMID: 33096162
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP K ...
3.
Hill M, Fang H, Brown J, Molski T, Easton A, Han X, et al.
ACS Med Chem Lett
. 2016 Dec;
7(12):1082-1086.
PMID: 27994742
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the -methyl-d-aspartate receptor (NMDAR)....
4.
Degnan A, Maxwell D, Balakrishnan A, Brown J, Easton A, Gulianello M, et al.
Bioorg Med Chem Lett
. 2016 Nov;
26(24):5871-5876.
PMID: 27856084
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5...
5.
Huang H, Degnan A, Balakrishnan A, Easton A, Gulianello M, Huang Y, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(17):4165-9.
PMID: 27496211
Herein we describe the structure activity relationships uncovered in the pursuit of an mGluR5 positive allosteric modulator (PAM) for the treatment of schizophrenia. It was discovered that certain modifications of...
6.
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5
Yang F, Snyder L, Balakrishnan A, Brown J, Sivarao D, Easton A, et al.
ACS Med Chem Lett
. 2016 Mar;
7(3):289-93.
PMID: 26985317
Positive allosteric modulators (PAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5) are of interest due to their potential therapeutic utility in schizophrenia and other cognitive disorders. Herein we describe...
7.
Whiterock V, Morgan D, Lentz K, Orcutt T, Sinz M
Drug Metab Dispos
. 2011 Nov;
40(2):228-31.
PMID: 22074769
Phenacetin is widely used as an in vitro probe to measure CYP1A2 activity across species. To investigate whether phenacetin can be used as an in vivo probe substrate to phenotype...
8.
Whiterock V, Delmonte T, Hui L, Orcutt T, Sinz M
Drug Metab Lett
. 2009 Apr;
1(2):163-5.
PMID: 19356037
A single nucleotide polymorphism in the dog CYP1A2 gene causes these animals to be CYP1A2 deficient (i.e., lack functional CYP1A2 enzyme activity). Genotyping a colony of 79 dogs revealed 77%...