27296-60-2Relevant academic research and scientific papers
Chromeno[3,4-c]pyridin-5-ones: Selective human dopamine D4 receptor antagonists as potential antipsychotic agents
Unangst, Paul C.,Capiris, Thomas,Connor, David T.,Heffner, Thomas G.,MacKenzie, Robert G.,Miller, Steven R.,Pugsley, Thomas A.,Wise, Lawrence D.
, p. 2688 - 2693 (2007/10/03)
The discovery of a series of chromeno[3,4-c]pyridin-5-ones with selective affinity for the dopamine D4 receptor is described. Target compounds were tested for binding to cloned human dopamine D2, D3 and D4 receptor subtypes expressed in Chinese hamster ovary (CHO) K-1 cells. Several compounds demonstrated single digit nanomolar K(i) values for binding to the D4 receptor with several hundred-fold selectivities toward the D2 and D3 receptors. A limited SAR study of this series is discussed. In a mitogenesis assay measuring [3H]thymidine uptake, the target compounds showed antagonist to weak, partial agonist activity at the D4 receptor, with intrinsic activities ranging from 0 to 35%. Compound 6, 3-benzyl-8-methyl-1,2,3,4- tetrahydrochromeno[3,4-c]pyridin-5-one, increased DOPA (L-3 4- dihydroxyphenylalanine) synthesis 84% in the hippocampus and 10% in the striatum of rat brain when dosed orally at 10 mg/kg.
Evaluation of Some Naturally Occurring and Synthetic Coumarins for Hypotensive Activity
Joshi, B. S.,Viswanathan, N.,Kaul, C. L.,Grewal, R. S.
, p. 495 - 499 (2007/10/02)
A number of synthetic as well as natural coumarins have been screened for their hypotensive activity.Most of the compounds show fall of blood pressure lasting for short duration.
Drugs derived from cannabinoids. 1. Nitrogen analogs, benzopyranopyridines and benzopyranopyrroles
Pars,Granchelli,Razdan,Keller,Teiger,Rosenberg,Harris
, p. 445 - 454 (2007/10/05)
Various nitrogen analogs of Δ(6a,10a) tetrahydrocannabinol were synthesized by a general procedure described in an earlier communication. Minimum effective doses (MED(50's)) and lethal doses (LD(50's)) were determined by a modified Irwin mouse screen afte
