Imidazo[1,2-b]pyridazines. XIII. Syntheses and Central Nervous System Activities of Some 2-Benzyl(phenethyl, biphenyl-4'-yl, 6'-methylnaphthalen-2'-yl, t-Butyl and cyclohexyl)-3-methoxy(acylaminomethyl and dimethylaminomethyl)-6-(variously substituted)imidazo[1,2-b]pyridazines

1992 ◽  
Vol 45 (8) ◽  
pp. 1281 ◽  
Author(s):  
GB Barlin ◽  
LP Davies ◽  
SJ Ireland ◽  
JK Zhang
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Rat Brain ◽  
Brain Membrane ◽  
The Central Nervous System

6-(Variously substituted)-3-methoxy(unsubstituted, dimethylaminomethyl, acetamidomethyl and benzamidomethy1)-2-benzyl(phenethyl, biphenyl-4'-yl, 6'-methylnaphthalen-2'-yl, t-butyl and cyclohexyl)imidazo[1,2-b] pyridazines have been prepared and examined for activity in the central nervous system. Of these, 2-benzyl-3-methoxy-6-(3'-methoxybenzylamino) imidazo[1,2-b]pyridazine (IC50 88nM) bound most strongly to rat brain membrane. In general, the order of activity for groups at the 2-position was Ph > PhCH2 > PhCH2CH2 > C6H4Ph-p, 6'-methylnaphthalen-2'-yl, c-C6H11 or But.

Imidazo[1,2-b]pyridazines. XII. Syntheses and Central Nervous System Activities of Some Substituted Imidazo[1,2-b]pyridazines and Related Imidazo[1,2-a]pyridines, Imidazo[1,2-a]pyrimidines and Imidazo[1,2-a]pyrazines

1992 ◽  
Vol 45 (5) ◽  
pp. 877 ◽  
Author(s):  
GB Barlin ◽  
LP Davies ◽  
SJ Ireland ◽  
MML Ngu ◽  
JK Zhang
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Rat Brain ◽  
Alkyl Group ◽  
Significant Loss ◽  
Aryl Group ◽  
Brain Membrane ◽  
Ic50 Values

Syntheses are reported for some 6-chloro(alkoxy,alkylthio and pheny1thio)-3-benzamidomethyl-(acetamidomethyl and methoxy)-2-arylimidazo[1,2-apyridines and some corresponding imidazo- [1,2- b]pyridazines, imidazo[1,2-a[pyrimidines and imidazo[l,2-a]pyrazines. IC50 values (or percentage displacement) are reported and discussed for the displacement of [3H]diazepam from rat brain membrane by each of these compounds. The imidazo[l,2-a[pyridines were generally slightly less potent than the imidazo[l,2- b]pyridazines but considerably more potent than the corresponding imidazo[1,2-a]pyrimidines or imidazo[1,2- a[pyrazines. Substitution of a 2-aryl group by a 2-alkyl group in imidazo[l,2- b]pyridazines led to a significant loss of activity.

scholarly journals Intracellular distribution of pentobarbital sodium in rat brain

1958 ◽  
Author(s):  
◽  
Carol Jean Oen
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Rat Brain ◽  
Major Effect ◽  
Cellular Component ◽  
Intracellular Distribution ◽  
Brain Cells ◽  
Pentobarbital Sodium ◽  
The Central Nervous System ◽  
The Way

"The major effect of the barbiturates is depression of the central nervous system, but the way in which these drugs exert their effect is not yet well understood...As the biochemical functions of the cell and its various parts become better understood, it is of interest to relate the actions of t a drug to some particular function (Reiner and Gellhorn, 1956). If it were found that barbiturate were localized by a particular cellular component, this might mean that its effect was rendered through some function of that particular component. Consequently, this study was undertaken to determine the intracellular distribution of a particular barbiturate, pentobarbital sodium, within rat brain cells."--Introduction

Imidazo[1,2-b]pyridazines. XI. Syntheses and Central Nervous System Activities of Some 6-(N-Benzyl-N-methylamino)-3-methoxy-2-phenyl(and substituted phenyl)imidazo[1,2-b]pyridazines

1992 ◽  
Vol 45 (4) ◽  
pp. 751 ◽  
Author(s):  
GB Barlin ◽  
LP Davies ◽  
SJ Ireland ◽  
JK Zhang
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Rat Brain ◽  
Active Compound ◽  
Brain Membrane ◽  
Ic50 Values

Syntheses are reported for 196-(N-benzyl-N-methylamino )-3-methoxy-2-phenyl(and substituted phenyl or pyridinyl ) imidazo [1,2-b] pyridazines from 6-(N-benzyl-N-methylamino)pyridazin-3- amine 2-oxide. The ability of each of these compounds to displace [3H]diazepam from rat brain membrane preparations was measured and the IC50 values (or percentage displacements) are reported and discussed. 6-(N-Benzyl-N-methylamino )-3-methoxy-2-phenylimido[1,2-b]pyridine was about half as active as its 6-bemylamino analogue, and the most active compound was 6-(N-benzyl-N-methylamino )-2-(2'-fluorophenyl)-3-methoxyimido[1,2-b] pyridazine with IC50 9.8 nM.

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