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At least 73 records · Page 4Linked to original sources
PubMed2004

Diacetato-kappa2O-bis[(S)-1-(4-fluorophenyl)ethylamine-kappaN]palladium(II) and di-mu-acetato-kappa4O:O'-bis[[(S)-2-(1-aminoethyl)-5-fluorophenyl-kappa2C1,N]palladium(II)] benzene hemisolvate.

Complexes of the composition trans-[Pd(L)2(OAc)2] have been postulated as intermediates during cyclopalladation. The first structural characterization of such a precursor has now been achieved and its role in the reaction sequence has been established. Diacetato-kappa2O-bis[(S)-1-(4-fluorophenyl)ethylamine-kappaN]palladium(II), [Pd(O2CMe)2(4-FC6H3CHMeNH2)2] or [Pd(C2H3O2)2(C8H10FN)2], (I), was obtained from palladium(II) acetate and (S)-NH2CHMeC6H3F-4 in a 1:2 molar ratio. The intermediate was then reacted with additional palladium(II) acetate to give the acetate-bridged dinuclear complex di-mu-acetato-kappa4O:O'-bis[[(S)-2-(1-aminoethyl)-5-fluorophenyl-kappa2C1,N]palladium(II)] benzene hemisolvate, [Pd(4-FC6H3CHMeNH2)2(mu-O2CMe)]2.0.5C6H6 or [Pd2(C8H9FN)2(C2H3O2)2].0.5C6H6, (II).

Journal Article↗
PubMed1982

Effects of impromidine, a specific H2-receptor agonist and 2(2-pyridyl)-ethylamine, an H1-receptor agonist, on stimulation-induced release of [3H]-noradrenaline in guinea-pig isolated atria.

1 The specific histamine H2-receptor agonist, impromidine (3-100 nmol/l), increased the rate and force of beating of guinea-pig isolated atria. These effects were blocked by the H2-receptor antagonist, cimetidine (30 mumol/l), but not by the H1-receptor antagonist, mepyramine (0.1 mumol/l). 2 In atria that had previously been incubated in [3H]-noradrenaline, impromidine (3-100 nmol/l) had no effect on the resting efflux of radioactivity, but concentrations of 50 and 100 nmol/l significantly increased the efflux induced by electrical stimulation (2 Hz for 10 s) of the intramural sympathetic nerves by approximately 38%; lower concentrations (3, 10 and 25 nmol/l) had no effect. 3 The effect of impromidine in enhancing stimulation-induced efflux of radioactivity was abolished by cimetidine (30 mumol/l) and by mepyramine (0.1 mumol/l). It was unaffected by the alpha-adrenoceptor antagonist, phentolamine (30 mumol/l). 4 Impromidine produced some inhibition of the uptake of [3H]-noradrenaline, but this did not account for the enhancement of the stimulation-induced efflux of radioactivity, since impromidine (50 mumol/l) still increased release in the presence of cocaine (30 mumol/l). 5 The specific H1-receptor agonist, 2-(2-pyridyl)-ethylamine (10-100 mumol/l), increased both the resting and stimulation-induced efflux of radioactivity. These effects were not blocked by mepyramine (0.1 mumol/l) or the beta-adrenoceptor antagonist, metoprolol (0.1 mumol/l). 6 The prejunctional inhibitory histamine receptors in guniea-pig atria are not classifiable into H1- or H2-type by the use of relatively specific postjunctional histamine H1- or H2-receptor agonists and antagonists.

Animals↗
PubMed2003

Differences in cytochrome P450 forms involved in the metabolism of N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine monohydrochloride (NE-100), a novel sigma ligand, in human liver and intestine.

N,N-Dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine monohydrochloride (NE-100) has been developed to treat subjects with schizophrenia. This drug is mainly excreted in the form of oxidative metabolites. In the present study, identification of p450 forms involved in the metabolism was carried out using human livers and intestinal microsomes (HLM and HIM). Eadie-Hofstee plots for NE-100 disappearance in HLM were biphasic, thus indicating the involvement of at least two p450 forms. The metabolism of NE-100 was mediated with recombinant CYP1A1, CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. A significant correlation was observed between activities of NE-100 metabolism and dextromethorphan O-demethylation (a specific activity for CYP2D6) or testosterone 6beta-hydroxylation (a specific activity for CYP3A4) in HLM. The activity of NE-100 metabolism was inhibited by approximately 80% by an anti-CYP2D6 antibody and only by quinidine among the p450-selective inhibitors at a low substrate concentration (0.1 microM). In contrast, with a high substrate concentration (10 microM), the activity was inhibited by an anti-CYP3A4 antibody and by ketoconazole. On the other hand, in HIM, the Eadie-Hofstee plots for NE-100 disappearance were monophasic, and the metabolism was strongly inhibited by an anti-CYP3A4 antibody and by ketoconazole but not by other inhibitors used. These results strongly suggest that NE-100 has different profiles regarding metabolism between liver and intestine. During absorption, NE-100 is mainly metabolized by CYP3A4 in the intestine and thereafter by CYP2D6 in the liver in the presence of therapeutic doses.

Anisoles↗
PubMed1995

Preliminary preformulation studies of a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration at an exploratory stage of new drug development.

Preliminary preformulation studies of a 2-(3,4-dimethoxyphenyl)ethylamine derivative were investigated. The hydrochloride form showed incompatibility with the excipients used for oral dosage forms. There were several crystal forms of the free base, namely, alpha-anhydrate, beta-anhydrate, monohydrate, and trihydrate. The trihydrate form was unstable. The degree of crystallinity of the beta-anhydrate form was difficult to control. The monohydrate form was difficult to manufacture with constant quality. The serum levels of the compounds in rats were almost related to the dissolution rates in the JP 1st disintegration medium from the discs. The serum level of alpha-anhydrate was the lowest. However, the dissolution rates from the formulations of alpha-anhydrate were improved. After oral administration of the improved formulation, the serum level of alpha-anhydrate in beagle dogs was almost triple that after the oral administration of the capsule of the hydrochloride form.

Administration, Oral↗
PubMed2000

Stereoselective reactions. XXXII. Enantioselective deprotonation of 4-tert-butylcyclohexanone by fluorine-containing chiral lithium amides derived from 1-phenylethylamine and 1-(1-naphthyl)ethylamine.

Enantioselective deprotonation of 4-tert-butylcyclohexanone was examined using 1-phenylethylamine- and 1-(1-naphthyl)ethylamine-derived chiral lithium amides having an alkyl or a fluoroalkyl substituent at the amide nitrogen. The lithium amides having a 2,2,2-trifluoroethyl group on the amide nitrogen are easily accessible in both enantiomeric forms, and were found to induce good enantioselectivity in the present reaction.

Amides↗
PubMed1977

Metabolic products of N-ethyl-beta-methoxy-beta-(3'-trifluoromethylphenyl)ethylamine (SKF 40652A).

The metabolsim of N-ethyl-beta-methoxy-beta-(3'-trifluoromethylphenyl)ethylamine (SKF 40652A, I) in vitro with 9000 g supernatants and washed microsomes of rabbit liver gave N-dealkylation, and N-oxidation of the parent secondary amine and the derived primary amine, anti and syn beta-methoxy-beta-(3'-trifluoromethylphenyl)acetaldoximes (V), and the beta-methoxy-beta-(3'-trifluoromethylphenyl(ethyl alcohol (VI). The identification and the physicochemical properties of these compounds are reported.

Animals↗
PubMed1988

Synthesis and dopamine receptors binding affinity of 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N-alkyl derivatives.

The 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N,N-dialkyl derivatives were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. No compound proved effective in displacing [3H]SCH 23390. Two derivatives are selective displacers of [3H]spiperone.

Animals↗