Substituted hexahydrobenzodipyrans as 5-HT2A/2C receptor probes.
A pair of substituted hexahydrobenzodipyrans was designed as molecular probes for determining the steric restrictions of the agonist binding site of serotonin 5-HT2A and 5-HT2C receptors. The rationale for the design of these receptor ligands, their chemical synthesis, rat behavioral pharmacology in the two-lever drug discrimination assay using LSD-trained rats, affinity for cloned rat 5-HT2A and 5-HT2C receptors and agonist functional activities are reported.
Whiteside
Michael S
MS
Department of Chemistry, University of Wisconsin-La Crosse, La Crosse, WI 54601, USA.
Kurrasch-Orbaugh
Deborah
D
Marona-Lewicka
Danuta
D
Nichols
David E
DE
Monte
Aaron
A
D016475:3T3 Cells; D000818:Animals; D001665:Binding Sites; D006213:Hallucinogens / Q000008:administration & dosage / Q000494:pharmacology; D008024:Ligands; D008238:Lysergic Acid Diethylamide / Q000008:administration & dosage / Q000494:pharmacology; D051379:Mice; D015335:Molecular Probes / Q000138:chemical synthesis; D010716:Phosphatidylinositols / Q000378:metabolism; D011714:Pyrans / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000378:metabolism*; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology
D006213:Hallucinogens; D008024:Ligands; D015335:Molecular Probes; D010716:Phosphatidylinositols; D011714:Pyrans; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D008238:Lysergic Acid Diethylamide