Table 1

Receptor binding assays used to determine the selectivity profile of PD 156982

ReceptorLigandTissue
Cholecystokinin CCKA [125I]BHCCK8sRat pancreas
Cholecystokinin CCKB [125I]BHCCK8sMouse cortex
BB1 [125I][Tyr4]bombesinCloned human
BB2 [125I][Tyr4]bombesinCloned human
Galanin[125I]GalaninRat basal forebrain
Opiate κ[3H]U69593Guinea pig forebrain
Opiate μ[3H]DAGOLGuinea pig forebrain
Na/K ATPase[3H]OuabainRat cortex
Dopamine D1 [3H]SCH23390Pig striatum
5-HT[3H]5HTGuinea pig cortex
5-HT1A [3H]8OH-DPATGuinea pig cortex
5-HT2 [3H]KetanserinRat cortex
K+ channel ATP sensitive[3H]GlibenclamidePig brain
Benzodiazepine[3H]FlunitrazepamMouse brain
L-type Ca2+ channel[3H]NimodepineRat cortex
Histamine H1 [3H]PyrilaminPig cortex
Adrenoceptoralpha-1[3H]PrazosinRat cortex
muscarinic M1 [3H]QNBPig brain
GABA-A[3H]GABARat cortex
GABA-B[3H]GABARat cortex
Glycine[3H]GlycineRat cortex
NMDA[3H]MK801Rat cortex
NMDA[3H]CGP3963Rat cortex
  • List of nontachykinin receptor binding assays performed to determine selectivity of PD 156982 for tachykinin NK1receptors. Assays were carried out using standard methodology as described in the literature. PD 156982 showed <50% inhibition of specific binding at 10 μM in the majority of assays. Of the exceptions, highest affinity was observed at CCKA receptors in the rat pancreas [IC50 value 450 nM (range 270–600)]. IC50 values in the 2 to 10 μM range were obtained for human BB1 and BB2 receptors, CCKB and 5-HT2receptors and calcium channels labeled by [3H]-nimodipine.