TY - JOUR
T1 - Typical antipsychotics exhibit inverse agonist activity at rat dopamine D1-like receptors expressed in Sf9 cells
AU - Martin, Michael W.
AU - Scott, Allelia W.
AU - Johnston, Douglas E.
AU - Griffin, Suzy
AU - Luedtke, Robert R.
PY - 2001/5/25
Y1 - 2001/5/25
N2 - The baculovirus system has been used to express the rat dopamine D1 receptors in Spodoptera frugiperda (Sf9) cells. A panel of typical antipsychotics including, α-flupenthixol, fluphenazine and thioridizine were found to inhibit dopamine-dependent stimulation of adenylyl cyclase. However, these compounds were also found to inhibit adenylyl cyclase activity in the absence of agonist in Sf9 cells expressing dopamine D1-like receptors. Therefore, these nonselective dopamine receptor compounds displayed negative intrinsic or inverse agonist activity. None of the compounds tested were neutral antagonists.
AB - The baculovirus system has been used to express the rat dopamine D1 receptors in Spodoptera frugiperda (Sf9) cells. A panel of typical antipsychotics including, α-flupenthixol, fluphenazine and thioridizine were found to inhibit dopamine-dependent stimulation of adenylyl cyclase. However, these compounds were also found to inhibit adenylyl cyclase activity in the absence of agonist in Sf9 cells expressing dopamine D1-like receptors. Therefore, these nonselective dopamine receptor compounds displayed negative intrinsic or inverse agonist activity. None of the compounds tested were neutral antagonists.
KW - Adenylyl cyclase stimulation
KW - Antipsychotic
KW - Baculovirus expression
KW - Dopamine D1 receptor
KW - Dopamine receptor
KW - Inverse agonist
UR - http://www.scopus.com/inward/record.url?scp=0035946931&partnerID=8YFLogxK
U2 - 10.1016/S0014-2999(01)00982-7
DO - 10.1016/S0014-2999(01)00982-7
M3 - Article
C2 - 11408027
AN - SCOPUS:0035946931
VL - 420
SP - 73
EP - 82
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 2-3
ER -