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Photoaffinity Labelling of the Benzodiazepine Receptor Compromises the Recognition Site but Not Its Effector Mechanism
Author(s) -
Brown Chloë L.,
Martin Ian L.
Publication year - 1984
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1984.tb06707.x
Subject(s) - photoaffinity labeling , benzodiazepine , chemistry , labelling , flunitrazepam , diazepam , receptor , affinity label , gabaa receptor , membrane , effector , biochemistry , biophysics , pharmacology , biology
When subjected to ultraviolet light flunitrazepam could be irreversibly attached to brain membrane preparations such that the affinity of the benzodiazepinereceptor for certain ligands, such as diazepam, becomes markedly reduced. However, the apparent affinity for diazepam is increased by the addition of y‐aminobutyricacid and sodium chloride, to the same extent in this membrane preparation as in membranes not so pretreated. This observation suggests that photoaffinity labelling ofthe benzodiazepine receptor with flunitrazepam modifiesthe recognition characteristics of the receptor but not itseffector mechanism.