LIGAND DETERMINATION WITH SPIN LABELED COMPOUNDS BY RECEPTOR DISPLACEMENT

• US 3,690,834 A
• Filed: 05/10/1971
• Issued: 09/12/1972
• Est. Priority Date: 01/11/1971
• Status: Expired due to Term

• Current Assignee: Edwin F. Ullman, Goldstein Avram, Richard K. Leute
• Original Assignee: Edwin F. Ullman, Goldstein Avram, Richard K. Leute
• Inventors: GOLDSTEIN AVRAM, Leute, Richard K., Ullman, Edwin F.
• Application Number:
  US05/141,516
• Time in Patent Office: 491 Days
• US Class Current: 436/537
• CPC Class Codes: C07D 207/46 with hetero atoms directly attached to the ring nitrogen atom
• CPC Class Codes: G01N 24/088 Assessment or manipulation of a chemical or biochemical reaction, e.g. verification whether a chemical reaction occurred or whether a ligand binds to a receptor in drug screening or assessing reaction kinetics
• CPC Class Codes: G01N 33/58 involving labelled substances G01N33/53 takes precedence
• CPC Class Codes: G01N 33/946 CNS-stimulants, e.g. cocaine, amphetamines
• CPC Class Codes: G01N 33/9486 Analgesics, e.g. opiates, aspirine
• CPC Class Codes: G01R 33/281 Means for the use of in vitro contrast agents G01R33/282 takes precedence; involving use of a contrast agent in MR imaging G01R33/5601; in vivo contrast agents A61K49/0002
• CPC Class Codes: Y10S 436/803 Stabe free radicals, e.g. spin immunoassay
• CPC Class Codes: Y10S 436/816 Alkaloids, amphetamines, and barbiturates
• CPC Class Codes: Y10S 436/817 Steroids or hormones

Abstract

ORGANIC COMPOUNDS OF BIOLOGICAL INTEREST CAN BE DETERMINED A EXTREMELY LOW CONCENTRATIONS BY COMBINING IN A MEDIUM, THE COMPOSITION TO BE DETERMINED, HEREINAFTER REFEREED TO AS LIGAND, A HIGH MOLECULAR WEIGHT MATERIAL OF AT LEAST 10,000 MOLECULAR WEIGHT, WHICH HAS A SITE SPATIALLY CHARACTERISITIC OF THE LIGAND, HEREINAFTER REFERRED TO AS RECEPTOR, AND AN ANALOG OF THE LIGAND HAVING A FREE RADICAL FUNCTIONALITY, HEREINAFTER REFERRED TO AS "LIGAND ANALOG." THE LIGAND ANALOG AND LIGAND IN THE MEDIUM COMPETE FOR THE RECEPTOR SITE, THE AMOUNT OF LIGAND ANALOG BOND TO THE RECEPTOR, BEING DEPENDENT ON

THE AMOUNT OF LIGAND PRESENT IN THE MEDIUM. BY FOLLOWING THE CHANGE IN ELECTRON SPIN RESONANCE SPECTRUM OF THE LIGAND ANALOG AND COMPARING IT TO THE CHANGE IN SPECTRUM WHICH WOULD BE OBTAINED IN THE ABSENCE OF ANY LIGAND, THE AMOUNT OF LIGAND CAN BE DETERMINED. COMPOUNDS ARE PROVIDED WHICH ARE LIGAND ANALOGS FOR USE IN THE ASSAY.

Claims