alexa Development Of Orally Bioavailable, Blood-brain Barrier Penetrant Antidotes To Replace 2-PAM As An Antidote In Organophosphate Exposure
ISSN: 1948-593XX

Journal of Bioanalysis & Biomedicine
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Share This Page

Additional Info

Loading
Loading Please wait..
 

8th World congress on Bioavailability & Bioequivalence: Pharmaceutical R & D Summit
June 26-27, 2017 San Diego, USA

Palmer Taylor
University of California, USA
Keynote: J Bioanal Biomed
DOI: 10.4172/1948-593X-C1-028
Abstract
Current antidotes to organophosphate exposure from pesticides and the more insidious nerve agents of terrorism are limited by their inability to cross the blood-brain barrier, their rapid clearance and lack of oral bioavailability. To enhance antidote activity, we have developed a library of zwitterion antidotes with measured in vitro reactivation capabilities and capacity to cross the blood-brain barrier and reactivate cholinesterase in the central and peripheral nervous system. Lead compounds show good protection ratios in mice and have led to more detailed pharmacokinetic and tissue disposition studies in mice and macaques. Antidotes, in contrast to therapeutic agents in treatment of chronic disease, require immediate absorption and distribution to the target tissue of action. To this end, we have developed a small molecule intramuscular loading doseoral maintenance dose scheme for the treatment of organophosphate poisoning from nerve agents used in terrorism and pesticides used in agriculture and home/gardens. By virtue of the ionization equilibria transitioning at physiological pH values between amine cation and oximate anion, both with pKa values between 8 and 9, a cationic or zwitterion species is available for reactivation of organophosphate conjugated AChE within the active center gorge in target tissues and a neutral species, that can readily cross the blood-brain barrier and exhibit oral bioavailability, treatment immediately after exposure by subcutaneous organophosphates or inhaled sarin vapor reverses toxicity in mice and macaques. The presentation will review the pharmacokinetics and tissue disposition required for successful antidote treatment of terrorism-inspired events.
Biography

Palmer Taylor is a PhD holder and the Sandra and Monroe Trout Chair Person of Pharmacology at the University of California, San Diego. He served as Founding Dean of the Skaggs School of Pharmacy and Pharmaceutical Sciences (2002-2014) and previously as Chair Person of the Department of Pharmacology in the School of Medicine (1987-2002). His research is directed to molecular pharmacology and neurotransmission, through study of the structures and functions of acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChRs). His particular interests are molecular recognition and design of selective therapeutic agents, directed to the α7-nAChR subtype and to antidotes that reactivate the organophosphate-conjugated AChE. The soluble acetylcholine binding protein has been the template for design of agonists and antagonists of the α7-nAChR subtype potentially useful in treatment of disorders of nervous system development and aging. His group has also been responsible for development of small zwitterion antidotes that serve as reactivators for organophosphate poisoning.

Email: [email protected]

image PDF   |   image HTML
 
Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri & Aquaculture Journals

Dr. Krish

[email protected]

1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

General Science

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001Extn: 9042

 
© 2008- 2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version
adwords