Antagonists of A2B Receptors Improve Insulin Sensitivity

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$100,000.00
Award Year:
2001
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Award Id:
54441
Agency Tracking Number:
1R43DK059677-01
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
300 PRESTON AVE, 5TH FLOOR, CHARLOTTESVILLE, VA, 22902
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
ROBERT FIGLER
() -
Business Contact:
(434) 971-6800
RSCAPON@AOL.COM
Research Institution:
n/a
Abstract
DESCRIPTION (Scanned from the Applicant's Abstract): Blockade of A2B adenosine receptors (A2BARs) increases insulin sensitivity in insulin resistant obese Zucker rats by an effect on skeletal muscle. We have synthesized and characterized the first potent and selective antagonists of A2B receptors. The goal of this phase I SBIR proposal is to develop improved A2BAR antagonists as new candidate drugs for the treatment of insulin resistance. Aim 1 is to synthesize additional A2BAR structures that have improved aqueous solubility but that maintain high potency and selectivity for human and rat A2BARs. Aim 2 is to determine pharmacokinetics of candidate compounds in rats. Preliminary data indicate that MRS1754, a prototype selective A2B antagonist, and BWA1433, a nonselective Al and A2B antagonist, are able to improve insulin sensitivity in insulin resistant Zuker rats. These findings cannot be replicated using the A1AR-selective antagonist, cyclopentyl-1,3-dipropyl-xanthine (CPX). Aims 3 and 4 of this proposal are designed to prove that A2B adenosine receptor blockade improves insulin sensitivity in rat models of insulin resistance. There is a great need for improved therapies to treat type II diabetes and insulin resistance that commonly accompany obesity. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE

* information listed above is at the time of submission.

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