Synthesis and radioreceptor binding activity of N-0437, a new, extremely potent and selective D2 dopamine receptor agonist

Pharm Weekbl Sci. 1985 Oct 25;7(5):208-11. doi: 10.1007/BF02307578.

Abstract

The synthesis of a new, potent and selective D2 dopamine receptor agonist, N-0437, of the 2-aminotetralin group is described. The results of a radioreceptor binding assay using a homogenate of porcine anterior pituitary as a tissue source for D2 dopamine receptors and 3H-spiperone as radioligand demonstrate that this compound is one of the most potent compounds so far evaluated in this test system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive
  • In Vitro Techniques
  • Naphthalenes / chemical synthesis*
  • Radioligand Assay
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine / metabolism
  • Receptors, Dopamine D2
  • Spiperone / metabolism
  • Structure-Activity Relationship
  • Swine
  • Tetrahydronaphthalenes / chemical synthesis*
  • Tetrahydronaphthalenes / pharmacology
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology
  • Tritium

Substances

  • Naphthalenes
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Tetrahydronaphthalenes
  • Thiophenes
  • Tritium
  • Spiperone
  • rotigotine