Binding properties of dipropyltryptamine at the human 5-HT1a receptor.
Dipropyltryptamine (DPT) is a synthetic indolealkylamine first characterized in the 1960s. Largely forgotten since the discovery of multiple serotonin receptor subtypes, some of the properties of DPT at the cloned human 5-HT1a receptor are described here. When [3H]8-OH-DPAT is bound to the receptor, DPT inhibits the interaction with an IC50 of 0.1 micromol/l. This interaction is shown to be competitive when double-reciprocal plots of the DPT/agonist interaction are analyzed. DPT's effects in the signal transduction system are complex. While DPT alone (0.1-1,000 micromol/l) activates Gi when both cAMP and gamma-S-GTP incorporation are measured, in the presence of 5-HT (0.1-10 micromol/l), DPT blocks the agonist effect. In combination, the findings suggest that DPT is a moderate affinity partial agonist at the human 5-HT1a receptor. These results provide evidence that DPT has potential as a versatile experimental tool at 5-HT1a receptors.
Thiagaraj
Harish V
HV
Department of Biomedical and Pharmaceutical Sciences, The COBRE Center for Structural and Functional Neuroscience, School of Pharmacy and Allied Health Sciences, The University of Montana, Missoula, Montana 59812-1552, USA.
Russo
Ethan B
EB
Burnett
Andrea
A
Goldstein
Eric
E
Thompson
Charles M
CM
Parker
Keith K
KK
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D000242:Cyclic AMP / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D011869:Radioligand Assay; D044282:Receptor, Serotonin, 5-HT1A / Q000235:genetics / Q000378:metabolism*; D012701:Serotonin / Q000494:pharmacology; D013462:Sulfur Radioisotopes; D014162:Transfection; D014316:Tritium; D014363:Tryptamines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
D013462:Sulfur Radioisotopes; D014363:Tryptamines; D014316:Tritium; D044282:Receptor, Serotonin, 5-HT1A; D012701:Serotonin; D016244:Guanosine 5'-O-(3-Thiotriphosphate); C007528:dipropyltryptamine; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000242:Cyclic AMP