Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes
摘要:
Thirteen [(aryl/heteroaryl-piperazinyl)alkyl]benzotriazoles were prepared as potential trazodone- and buspirone-like drugs. The synthesized compounds displayed from moderate to good affinity to the serotonin 5-HT1A receptor and only modest or poor affinity to the dopamine D-2 receptor, similar to buspirone. The introduction of substituents on the benzotriazole ring did,not improve the affinity to the 5-HT1A receptor, compared to the previously described unsubstituted derivatives. In a general pharmacological screening, which concerned only three of these compounds so far (5, 7 and 13), several in vitro and in vivo activities were observed.The guinea pig ileum contractions, induced either electrically or by several agonists, were strongly inhibited; at higher concentrations also the spontaneous tone of the guinea pig trachea was reduced. Compound 13 exhibited good analgesic activity in mice in the formalin-induced algesia and in the writhing test. The same at 30 mg kg(-1) p.o. also displayed antihypertensive activity probably related to calcium channel blockade and adrenergic alpha(1) antagonism. In binding assays, 13 showed a IC50 = 580 nM for displacing [H-3]prazosin from alpha(1) receptor.Finally, compound 5 (and, to a minor extent, compound 13) protected mice against potassium cyanide induced hypoxia. (C) 2001 Elsevier Science S.A. All rights reserved.
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes
摘要:
Thirteen [(aryl/heteroaryl-piperazinyl)alkyl]benzotriazoles were prepared as potential trazodone- and buspirone-like drugs. The synthesized compounds displayed from moderate to good affinity to the serotonin 5-HT1A receptor and only modest or poor affinity to the dopamine D-2 receptor, similar to buspirone. The introduction of substituents on the benzotriazole ring did,not improve the affinity to the 5-HT1A receptor, compared to the previously described unsubstituted derivatives. In a general pharmacological screening, which concerned only three of these compounds so far (5, 7 and 13), several in vitro and in vivo activities were observed.The guinea pig ileum contractions, induced either electrically or by several agonists, were strongly inhibited; at higher concentrations also the spontaneous tone of the guinea pig trachea was reduced. Compound 13 exhibited good analgesic activity in mice in the formalin-induced algesia and in the writhing test. The same at 30 mg kg(-1) p.o. also displayed antihypertensive activity probably related to calcium channel blockade and adrenergic alpha(1) antagonism. In binding assays, 13 showed a IC50 = 580 nM for displacing [H-3]prazosin from alpha(1) receptor.Finally, compound 5 (and, to a minor extent, compound 13) protected mice against potassium cyanide induced hypoxia. (C) 2001 Elsevier Science S.A. All rights reserved.
Uv-resistant hot-melt contact adhesive, a method for producing the same and adhesive objects produced therefrom
申请人:——
公开号:US20040014863A1
公开(公告)日:2004-01-22
The invention relates to a hot-melt contact adhesive, containing at least one unsaturated polymer and a particulate inorganic compound which has an average particle diameter d50 of between 0.05 and 300 &mgr;m. The invention also relates to a method for producing the same and to the use of inorganic particulate compounds of this type for producing a hot-melt contact adhesive. In addition, The invention relates to adhesive objects which are produced using a hot-melt contact adhesive of this type.