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Antagonists of A2B Receptors Improve Insulin Sensitivity

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
54441
Program Year/Program:
2001 / SBIR
Agency Tracking Number:
1R43DK059677-01
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
ADENOSINE THERAPEUTICS, LLC
310 FOURTH STREET NE SUITE 201 CHARLOTTESVILLE, VA 22902
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2001
Title: Antagonists of A2B Receptors Improve Insulin Sensitivity
Agency: HHS
Contract: N/A
Award Amount: $100,000.00
 

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

Principal Investigator:

Robert A. Figler

Business Contact:


4349716800
RSCAPON@AOL.COM
Small Business Information at Submission:

ADENOSINE THERAPEUTICS, LLC
300 PRESTON AVE, 5TH FLOOR CHARLOTTESVILLE, VA 22902

EIN/Tax ID: 541932209
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No