438564-53-5Relevant articles and documents
Syntheses of dual-radioisotope-labeled CP-I, a GABAA receptor partial agonist
Zhang, Yinsheng,Greenfield, Laura,Hong, Yang
, p. 411 - 417 (2012/07/13)
CP-I is a potent subtype-selective GABAA receptor partial agonist. Owing to its significant metabolic cleavage at C8 observed in preliminary biotransformation studies with non-radiolabeled CP-I, the syntheses of CP-I labeled at the right or left hand side with 14C or labeled with 3H at the right hand side were required. The two compounds labeled with 14C at the left or right hand side were synthesized in 2 and 5 radio-synthetic steps using [14C]2-chloroacetyl chloride and [ 14C]NaCN as starting radiolabeled materials, respectively. CP-I was labeled with tritium at the right hand side by a tritium de-halogenation method. Batches of radiolabeled CP-I were mixed to give dual-radioisotope-labeled CP-I. An efficient approach to [14C]fluoropyridinyl imidazole was developed, and a short synthesis of iodo-substituted fluoropyridinyl imidazole was also achieved. The details of these syntheses are discussed. Copyright
SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS
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Page 37, (2008/06/13)
Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8, and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
Substituted imidazolylmethyl pyridine and pyrazine deriviatives GABAa receptor ligands
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, (2008/06/13)
Substituted imidazolylmethyl pyridine and pyrazine derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
