127984-93-4Relevant articles and documents
Anxiolytic drugs
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, (2008/06/13)
The present invention relates to an anxiolytic drug comprising as an active ingredient a 1-amino-5-halogenouracil represented by formula [I]: STR1 wherein X represents a halogen atom, or pharmaceutically acceptable salt thereof.
Novel uracil derivatives: Newly synthesized centrally acting agents
Imaizumi,Kano,Sakata
, p. 1808 - 1813 (2007/10/02)
A series of 1-amino-5-substituted uracils and their 4-thio or 2,4-dithio substituted analogues were synthesized and assayed for anti-conflict activity in rats and anesthetic activity in mice. 1-Amino-5-halogenouracils 3b-e, 1-amino-4-thiouracil (9a), and 1-amino-5-halogeno-4-thiouracils 9c, d showed both anti-conflict and anesthetic activities. The most active compound was 1-amino-5-chloro-4-thiouracil (9d) which showed anxiolytic activity at 2 mg/kg of oral administration (p.o.) on a modified Geller-Seifter conflict schedule. Its minimum effective dose (MED) was lower than that of diazepam. The 50 percent effective dose (ED50) for anesthetic activity in mice of the compound (9d) was 32.9 mg/kg, p.o.