ProHealth health Vitamin and Natural Supplement Store and Health
Home  |  Log In  |  My Account  |  View Cart  View Your ProHealth Vitamin and Supplement Shopping Cart
800-366-6056  |  Contact Us  |  Help
Facebook Google Plus
Fibromyalgia  Chronic Fatigue Syndrome & M.E.  Lyme Disease  Natural Wellness  Supplement News  Forums  Our Story
Store     Brands   |   A-Z Index   |   Best Sellers   |   New Products   |   Deals & Specials   |   Under $10   |   SmartSavings Club

Trending News

Scientifically-designed fasting diet lowers risks for major diseases

More evidence for calorie restriction’s longevity effect

Supplementation with vitamin D associated with improved testosterone, erectile function among middle...

A Little Zinc Goes a Long Way

Vitamin D deficiency increases risk of chronic headache

VIDEO: The Best Brain Foods That Help Increase Your Memory!

Get the Most From Your Green Tea

Iron (And More) For Lasting, Natural Energy

Metabolic syndrome increases the need for vitamin E

Supplement combo improves bone density, mood, in postmenopausal women

 
Print Page
Email Article

Abstract: Mediation of Highly Concentrative Uptake of Pregabalin by L-Type Amino Acid Transport in CHO and Caco-2 Cells

  [ 64 votes ]   [ Discuss This Article ]
www.ProHealth.com • March 17, 2005


J Pharmacol Exp Ther. 2005 Mar 15; [Epub ahead of print] Su TZ, Feng MR, Weber ML. Pfizer Global R & D. Pregabalin (PGB) is a novel drug under development for the treatment of epilepsy, neuropathic pain, fibromyalgia and generalized anxiety disorder. In this study we investigated PGB transport in rats, mammalian cell lines and Xenopus leavis oocytes. In contrast to gabapentin (GBP), PGB absorption in rats showed unique linear pharmacokinetics. PGB entered CHO and Caco-2 cells predominately via Na(+)-independent processes. Uptake of PGB was mutually exclusive with leucine, GBP and BCH, the substrates preferential for system L. The preloaded PGB in CHO cells was exchangeable with leucine, but at a lower exchange rate than that of leucine and GBP. Dixon plots showed competitive inhibition of leucine uptake by PGB with a Ki value very close to the Km value for PGB uptake (377 vs. 363 microM). At an extracellular concentration of 300 microM, the intracellular PGB concentration in CHO cells reached 1.5- and 23-fold higher than that of GBP and leucine, respectively. By contrast, at clinically relevant concentrations, PGB appeared not to interact with GABA transport in GAT1, GAT2 and GAT3 cell lines, system y(+), b(0,+) , B(0,+) and B(0) transport activities in Caco-2 and NBL-1 cells, and the b(0,+)-like transport activity in rBAT cRNA-injected Xenopus leavis oocytes. Taken together, these results suggest that L-type transport is the major transport route for PGB and GBP uptake in mammalian cells. The differential affinity of PGB and GBP at L-type system leads to more concentrative accumulation of PGB than GBP, which may facilitate PGB transmembrane absorption in vivo. PMID: 15769862 [PubMed - as supplied by publisher]




Post a Comment

Featured Products From the ProHealth Store
Optimized Curcumin Longvida® Ultra EPA  - Fish Oil Vitamin D3 Extreme™

Looking for Vitamins, Herbs and Supplements?
Search the ProHealth Store for Hundreds of Natural Health Products


Article Comments



Be the first to comment on this article!

Post a Comment


 
NAD+ Ignite with Niagen

Featured Products

Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils
Optimized Curcumin Longvida® Optimized Curcumin Longvida®
Supports Cognition, Memory & Overall Health
Vitamin D3 Extreme™ Vitamin D3 Extreme™
50,000 IU Vitamin D3 - Prescription Strength
Mitochondria Ignite™ with NT Factor® Mitochondria Ignite™ with NT Factor®
Reduce Fatigue up to 45%
Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium

Natural Remedies

Sleep Like a Baby in Nature's Cradle Sleep Like a Baby in Nature's Cradle
Enhance Eyelashes Naturally Enhance Eyelashes Naturally
Restoring Gut Health: How to Create a Firewall Against Toxins Entering the Gut Wall Restoring Gut Health: How to Create a Firewall Against Toxins Entering the Gut Wall
Red Yeast Rice - Natural Option for Supporting Healthy Cholesterol Red Yeast Rice - Natural Option for Supporting Healthy Cholesterol
Break Free From Fibromyalgia Break Free From Fibromyalgia

CONTACT US
ProHealth, Inc.
555 Maple Ave
Carpinteria, CA 93013
(800) 366-6056  |  Email

· Become a Wholesaler
· Vendor Inquiries
· Affiliate Program
SHOP WITH CONFIDENCE
Credit Card Processing
SUBSCRIBE TO OUR NEWSLETTERS
Get the latest news about Fibromyalgia, M.E/Chronic Fatigue Syndrome, Lyme Disease and Natural Wellness

CONNECT WITH US ProHealth on Facebook  ProHealth on Twitter  ProHealth on Pinterest  ProHealth on Google Plus

© 2017 ProHealth, Inc. All rights reserved. Pain Tracker App  |  Store  |  Customer Service  |  Guarantee  |  Privacy  |  Contact Us  |  Library  |  RSS  |  Site Map