[Preparation and characteristics of a tritiated derivative of CP-96,345--a nonpeptide antagonist of the substance P receptor with a high specific radioactivity].
[3H]CP-96.345 with the specific radioactivity of 84.2 Ci/mmol has been prepared from CP-96.345 by the high-temperature solid state isotopic exchange. The tritiated compound was equipotent with the parent antagonist in inhibiting the iodinated substance P binding to brain membranes from various species. Direct binding of [3H]CP-96.345 was detected by radioligand analysis using the striatum-enriched membranes from the guinea-pig brain.
Kasheverov
I E
IE
Zaĭtsev
D A
DA
Utkin
Iu N
IuN
Tsetlin
V I
VI
D000818:Animals; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D064729:Neurokinin-1 Receptor Antagonists; D014316:Tritium
D001713:Biphenyl Compounds; D006993:Hypnotics and Sedatives; D064729:Neurokinin-1 Receptor Antagonists; D014316:Tritium; C066892:CP 96345
Poluchenie i kharakteristika tritirovannogo proizvodnogo CP-96,345-- nepeptidnogo antagonista retseptora veshchestva P--s vysokoĭ udel'noĭ radioaktivnost'iu.