Pharmacology in translation: the preclinical and early clinical profile of the novel α2/3 functionally selective GABAA receptor positive allosteric modulator PF-06372865-Reference-Cited by-同舟云学术

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Pharmacology in translation: the preclinical and early clinical profile of the novel α2/3 functionally selective GABAA receptor positive allosteric modulator PF-06372865

Published:2018-01-18 Issue:4 Volume:175 Page:708-725
ISSN:0007-1188
Container-title:British Journal of Pharmacology
language:en
Short-container-title:British Journal of Pharmacology

Author:

Nickolls Sarah A¹²,Gurrell Rachel¹^ORCID,van Amerongen Guido³,Kammonen Juha¹,Cao Lishuang¹,Brown Adam R¹,Stead Clara¹,Mead Andy⁴⁵,Watson Christine⁶,Hsu Cathleen⁴,Owen Robert M¹,Pike Andy¹,Fish Rebecca L¹,Chen Laigao⁴,Qiu Ruolun⁴,Morris Evan D⁷,Feng Gang¹,Whitlock Mark¹,Gorman Donal¹,van Gerven Joop³,Reynolds David S¹,Dua Pinky¹,Butt Richard P¹

Affiliation:

1. Pfizer Inc.; Cambridge UK

2. GSK Medicines Research Centre; Stevenage UK

3. Centre for Human Drug Research; Leiden The Netherlands

4. Pfizer Worldwide Research and Development; Groton CT USA

5. Drug Safety & Metabolism, AstraZeneca; Cambridge UK

6. Department of Worldwide Medicinal Chemistry; Pfizer Global Research and Development, Sandwich Laboratories; Sandwich Kent UK

7. Department of Radiology and Biomedical Imaging; Yale University; New Haven CT USA

Funder

Pfizer

Publisher

Wiley

Subject

Pharmacology

Link

http://onlinelibrary.wiley.com/wol1/doi/10.1111/bph.14119/fullpdf

Reference52 articles.

1. The Concise Guide to PHARMACOLOGY 2017/18: ligand-gated ion channels;Alexander;Br J Pharmacol,2017

2. Subtype-selective GABAA receptor modulation yields a novel pharmacological profile: the design and development of TPA023;Atack;Adv Pharmacol (San Diego, Calif),2009

3. The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates;Atack;Br J Pharmacol,2009

4. Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist;Atack;J Psychopharmacol (Oxford, England),2011a

5. MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans;Atack;J Psychopharmacol (Oxford, England),2011b

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