Receptor | Ligand | Tissue |
---|---|---|
Cholecystokinin CCKA | [125I]BHCCK8s | Rat pancreas |
Cholecystokinin CCKB | [125I]BHCCK8s | Mouse cortex |
BB1 | [125I][Tyr4]bombesin | Cloned human |
BB2 | [125I][Tyr4]bombesin | Cloned human |
Galanin | [125I]Galanin | Rat basal forebrain |
Opiate κ | [3H]U69593 | Guinea pig forebrain |
Opiate μ | [3H]DAGOL | Guinea pig forebrain |
Na/K ATPase | [3H]Ouabain | Rat cortex |
Dopamine D1 | [3H]SCH23390 | Pig striatum |
5-HT | [3H]5HT | Guinea pig cortex |
5-HT1A | [3H]8OH-DPAT | Guinea pig cortex |
5-HT2 | [3H]Ketanserin | Rat cortex |
K+ channel ATP sensitive | [3H]Glibenclamide | Pig brain |
Benzodiazepine | [3H]Flunitrazepam | Mouse brain |
L-type Ca2+ channel | [3H]Nimodepine | Rat cortex |
Histamine H1 | [3H]Pyrilamin | Pig cortex |
Adrenoceptoralpha-1 | [3H]Prazosin | Rat cortex |
muscarinic M1 | [3H]QNB | Pig brain |
GABA-A | [3H]GABA | Rat cortex |
GABA-B | [3H]GABA | Rat cortex |
Glycine | [3H]Glycine | Rat cortex |
NMDA | [3H]MK801 | Rat cortex |
NMDA | [3H]CGP3963 | Rat 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.