Premium
Back Cover: [ 3 H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H 2 Receptor Antagonist (ChemMedChem 1/2015)
Author(s) -
Baumeister Paul,
Erdmann Daniela,
Biselli Sabrina,
Kagermeier Nicole,
Elz Sigurd,
Bernhardt Günther,
Buschauer Armin
Publication year - 2015
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490052
Subject(s) - chemistry , tritium , histamine , antagonist , antagonism , competitive antagonist , stereochemistry , squaramide , receptor , cover (algebra) , biochemistry , pharmacology , biology , enantioselective synthesis , mechanical engineering , physics , organocatalysis , nuclear physics , engineering , catalysis
The back cover picture shows [ 3 H]UR‐DE257, a tritium‐labeled selective histamine H 2 receptor (H 2 R) antagonist identified from a series of piperidinomethylphenoxypropylamines. [ 3 H]UR‐DE257 exhibits high specific binding and comparable K d values at the human, rat, and guinea pig H 2 R. Despite insurmountable antagonism in functional studies and slow dissociation, it is fully displaceable in competition binding studies. Thus, [ 3 H]UR‐DE257 is a valuable tool for the study of H 2 R. For more details, see the Full Paper by Armin Buschauer et al. on p. 83 ff.