title: Receptor screening technologies in the evaluation of Amazonian ethnomedicines with potential applications to cognitive deficits.
abstract: BACKGROUND
  Amazonian peoples utilize a variety of psychoactive plants that may contain novel biologically active compounds. Efforts to investigate such remedies in terms of neuropharmacology have been limited.
  
  
  OBJECTIVE
  This study identified Amazonian ethnomedicines with potential for the treatment of cognitive deficits in schizophrenia and dementias, and characterized their interactions with CNS neurotransmitter receptors in vitro.
  
  
  METHODS
  Approximately 300 Amazonian species with folk uses or constituents indicative of central nervous system activity were incorporated into a database constructed from literature searches, herbarium surveys, and interviews with traditional practitioners. Approximately 130 of these targeted species were collected in Loreto province, Peru, and 228 fractions derived from them were screened in 31 radioreceptor assays via the resources of the NIMH Psychoactive Drug Screening Program. A subset was also screened in functional assays at selected serotonin, muscarinic, and adrenergic receptors.
  
  
  RESULTS
  Ninety-one samples displayed ≥60% inhibition of radioligand binding activity in receptor assays; 135 samples displayed agonist or antagonist activity (or both) in functional assays.
  
  
  CONCLUSIONS
  Potential CNS activity was detected in about 40% of the samples screened, with some correlations to both folk uses and phytochemical constituents. These results may point to novel and potentially therapeutic CNS active compounds.
authors.affiliation: Center for Spirituality and Healing, Academic Health Center, University of Minnesota, MMC505, 420 Delaware St. SE, Minneapolis, MN 55455, USA. mcken031@umn.edu
authors.forename: Dennis J
authors.initials: DJ
authors.lastname: McKenna
authors.forename: Juan M
authors.initials: JM
authors.lastname: Ruiz
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Hoye
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
authors.forename: Alan T
authors.initials: AT
authors.lastname: Shoemaker
mesh_terms: D003072:Cognition Disorders / Q000188:drug therapy* / Q000378:metabolism; D003704:Dementia / Q000188:drug therapy; D055808:Drug Discovery / Q000379:methods*; D020834:Ethnopharmacology / Q000379:methods; D006801:Humans; D007407:Interviews as Topic; D008519:Medicine, Traditional; D018377:Neurotransmitter Agents / Q000494:pharmacology* / Q000627:therapeutic use; D010568:Peru; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use; D010946:Plants, Medicinal; D011619:Psychotropic Drugs / Q000494:pharmacology / Q000627:therapeutic use; D017981:Receptors, Neurotransmitter / Q000378:metabolism; D012559:Schizophrenia / Q000188:drug therapy
chemical_list: D018377:Neurotransmitter Agents; D010936:Plant Extracts; D011619:Psychotropic Drugs; D017981:Receptors, Neurotransmitter