The regulation in expression of human 5-hydroxytryptamine1A (5-HT1A) receptors by agonists and antagonists was studied in a stable transfected Chinese hamster ovary cell line expressing the human 5-HT1A receptor. Receptor density and affinity were measured with [125I]4-(2'-methoxyphenyl)-1-[2'-[N-(2'-pyridinyl)-p-iodobenzamido ]ethyl]piperazine ([125I]p-MPPI), a selective antagonist of 5-HT1A r...

In the liver microsome cyanide (CN)-trapping assays, piperazinecontaining compounds formed significant N-methyl piperazine CN adducts. Two pathways for the N-methyl piperazine CN adduct formation were proposed: 1) The a-carbon in the N-methyl piperazine is oxidized to form a reactive iminium ion that can react with cyanide ion; 2) N-dealkylation occurs followed by condensation with formaldehyde...

1. Tetramisole (100 mug/ml) paralysed live Ascaris in 3 min.2. Tetramisole (10 mug/ml) caused a sustained contraction of the isolated somatic muscles of the worm. This contraction was not blocked by curare nor by piperazine.3. Tetramisole reduced the resting potential of Ascaris muscle from 34+/-4 to 10+/-1 mV.4. Tetramisole caused contraction of Ascaris muscle previously depolarized with high ...

In the title compound, (C(7)H(18)N(2))[ZnCl(4)], the Zn atom adopts a slightly distorted tetra-hedral geometry. The diprotonated piperazine ring adopts a chair conformation. In the crystal structure, the cations and anions are linked by inter-molecular N-H⋯Cl hydrogen bonds into a chain along [001].

1-Benzyl-N-(2,6-dimethylphenyl)piperidine-3-carboxamide and 4-benzyl-N-(2,6-dimethylphenyl)piperazine-2-carboxamide, two conformationally restricted analogues of tocainide, were designed and synthesized as voltage-gated skeletal muscle sodium channel blockers. They showed, with respect to tocainide, a marked increase in both potency and use-dependent block.

The crystal structure of the title compound, (C(5)H(14)N(2))[ZnCl(4)]·0.5H(2)O, is built up from discrete 1-methyl-piperazine-diium cations with chair conformation, tetrahedral tetrachloridozincate anions and uncoordinated solvent water mol-ecules linked together by three types of inter-molecular hydrogen bonds, viz. N-H⋯Cl, N-H⋯O and O-H⋯Cl.

In the title N-Mannich bases, 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-[(4-phenyl-piperazin-1-yl)meth-yl]-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C29H34FN5S) (I), and 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-{[4-(2-meth-oxyphen-yl)piperazin-1-yl]-meth-yl}-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C30H36FN5OS) (II), fluoro-phenyl, adamantane and piperazine moieties are linked to a planar triaz...

In the title salt, C11H17N2O2S(+)·CF3COO(-), the cation is protonated at the secondary piperazine N atom. The dihedral angle between the benzene ring and the piperazine mean plane is 85.54 (10)°. In the crystal, cations and anions are connected by two types of strong N-H⋯O hydrogen bonds into chains extending along [101]. The chains are further assembled into (10-1) layers via stacking inter-ac...