THIS IS A NOTICE OF INTENT TO AWARD A SOLE SOURCE ORDER AND NOT A REQUEST FOR QUOTATIONS. The National Center For Advancing Transltional Sciences (NCATS), Rockville, MD intends to negotiate on a sole source basis and issue an order with Eurofins Panlabs, Inc.under the authority of Federal Acquisition Regulation (FAR) 13.106-1(b). Only one responsible source and no other supplies or services will satisfy agency requirements. This purchase is for Lab Testing Services, Evaluation of Binding Affinity for twelve Lead D3 Antagonists in D2L and D3 Radioligand Binding Assays, IC50 determination. TDB at NCATS in collaboration with the investigators at NIDA has embarked on a journey to find novel D3R antagonists while displaying significant selectivity from the highly homologous D2 receptors. Working on the bitopic ligands identified by earlier investigations, the team has identified several lead molecules that display around a 1000-fold selectivity over D2R in the binding assays. These lead molecules occupy an orthosteric binding site (OBS) at D3R and connect to a secondary binding pocket (SBP), via a 4-carbon linker, responsible for achieving selectivity amongst the dopamine receptor subtypes. The lead molecules from this series, identified by the team, has displayed efficacy in various rat and non-human primate models of addiction and are being considered for development.

In this study, we will be evaluating D2/D3 selectivity for twelve lead antagonists in the in-vitro radio ligand binding assays. D2L and D3 Human Dopamine GPCR binding assays were chosen for this purpose. The ability of the new antagonist leads to inhibit the binding of the radio labeled ligand will be measured and reported. These assays will be performed at 5 antagonist concentrations and the IC50 will be reported. This data will help guide the in-vivo campaign for these lead antagonists. Award is subject to approval of the Sole Source Justification. This notice of intent is not a request for competitive proposals or quotations; however, an interested party may submit a statement of capabilities if they believe they can meet the above requirement. The statement of capabilities must be submitted in writing and contain sufficient detail to allow the Government to determine if the party can provide the requirement. A determination by the Government not to compete this proposed action based upon responses to this notice is solely with the discretion of the Government. All responses must be received within 10 days from the date of publication of this synopsis. Information received will normally be considered for the purpose of determining whether to conduct a competitive procurement. If no affirmative responses are received within 10 days of this notice, an award will be made to Eurofins Panlabs, Inc. The NAICS Code/Size is 541380/16.5M. This procurement is to be processed using Simplified Acquisition Procedures. There is no solicitation package available. No faxed documents will be accepted. For any questions regarding this announcement, please contact Robert McFarland via email: mcfarlar@mail.nih.gov, or Rhanda Lopez via email: rhanda.lopez@nih.gov.