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At least 145 records · Page 8Linked to original sources
PubMed1984

Structural correlations of choline acetyltransferase inhibitors: trans-N-(carboxymethyl)-4-(beta-1-naphthylvinyl)pyridinium bromide and cis-N-(2-aminoethyl)-4-(beta-1-naphthylvinyl)-3-methylpyridinium bromide hydrobromide.

This paper correlates the X-ray structures of two 4-(beta-1-naphthylvinyl)pyridine analogues (one cis and one trans) with chemical and biological activity data for this class of cholineacetylase inhibitors. Our results suggest that one of the two proposed mechanisms for inhibition by this class of compounds better describes their efficacy. Previous arguments about coplanarity of the aromatic rings and nucleophilicty across the vinyl linkage need to be modified. Quantum calculations are also included and substantiate previous suggestions about the charge distribution across the vinyl linkages. An alternate new mechanism of inhibition is proposed to encompass the published data and more recent results discussed in this paper.

Chemical Phenomena↗
PubMed2006

Br(2Pj) atom formation dynamics in ultraviolet photodissociation of tert-butyl bromide and iso-butyl bromide.

The photodissociation dynamics of tert-C(4)H(9)Br and iso-C(4)H(9)Br has been studied at 234 and 265 nm using two-dimensional velocity map imaging technique. The translational energy and angular distributions have been analyzed for Br, Br(*), and tert-C(4)H(9) radical. The energy distribution of Br atom in the photodissociation of tert-C(4)H(9)Br is found to consist of two Gaussian components. The two components are correlated to two independent reaction paths on the excited potential energy surfaces: (1) the high-energy component from the prompt dissociation along the C-Br stretching mode and (2) the low-energy component from the repulsive mode along the C-Br stretching, coupled with some bending motions. For the energy distribution of Br(*) atom in the photodissociation of tert-C(4)H(9)Br, a third multiphoton dissociative ionization channel is observed at 265 nm in addition to the two energy components corresponding to channels (1) and (2). The energy distributions of Br and Br(*) atoms in the photodissociation of iso-C(4)H(9)Br can be fitted using only one Gaussian function indicating a single formation channel. Relative quantum yields for Br((2)P(32)) at 234 and 265 nm in the photodissociation of tert-C(4)H(9)Br are measured to be 0.76 and 0.65, respectively. For iso-C(4)H(9)Br, the measured value is Phi(234 nm)(Br)=0.81. The contribution of bending modes to Br and Br(*) is much more obvious in the photodissociation of tert-C(4)H(9)Br than in iso-C(4)H(9)Br.

Journal Article↗
PubMed1989

Comparative potency of pipecuronium bromide and pancuronium bromide.

Cumulative dose-response curves were constructed to determine the comparative potency of pipecuronium and pancuronium. From these, the ED50 and ED95 values were calculated. These were 24.96 micrograms kg-1 and 44.96 micrograms kg-1, respectively, for pipecuronium and 30.42 micrograms kg-1 and 61.12 micrograms kg-1, respectively, for pancuronium.

Adult↗
PubMed1980

Effect of N-(4-butoxybenzyl) hyoscyaminium bromide (butropium bromide) on the isolated, blood-perfused canine atrium preparation.

The effects of butropium on chronotropic and inotropic activity were investigated in 10 isolated atrial preparations which were suspended in a bath and perfused with arterial blood led from a carotid artery of heparinized support dog. Butropium injected into the cannulated sinus node artery in a dose range of 3 to 100 microgram produced a dose-dependent positive chronotropic and inotropic effect. At relatively higher doses above 30 microgram, slight and brief initial negative chronotropic and inotropic effect followed by a long-lasting positive effect was observed. The positive effect of butropium was markedly suppressed by propranolol or carteolol, but it was not affected by tetrodotoxin or desmethylimipramine. From these results, a large amount of butropium may induce positive chronotropic and inotropic effect through cholinergic blockade and in part stimulation of adrenergic beta-receptors.

Animals↗
PubMed1976

[Ipratropium bromide in controlled clinical trials. Short communication (II): Time-response measurements of pulmonary function after ipratropium bromide and isoprenaline].

(8R)-3alpha-Hydroxy-8-isopropyl-1alphaH, 5alphaH, 5alphaH-tropaniumbromide (+/-)-tropate (ipratropiumbromide, Sch 1000, Atrovent) was compared with isoprenaline in a cross-over study with randomized selection in 12 stable asthmatics, using total airways resistance (Rt) measured by whole-body plethysmography, peak expiratory flow (PEF) and pulse rate as parameters. 2 puffs ipratropiumbromide (0.02 mg per puff) or isoprenaline (0.1 mg per puff) were administered by metered dose inhaler and measurements taken at 5, 20, 35, 50, 90 min, 2, 3, 4, and 6 h later. Drugs were given on alternate days. Rt decreased significantly (p less than 0.001) for 4 h to 53% of the initial value after ipratropiumbromide and to 70% of the initial value after isoprenaline, but only for about 2 h after the latter. The maximum 20-min effect on Rt was almost the same for both drugs. The difference in the time course of the bronchodilation was also significant. The rise in PEF after 4 h following ipratropiumbromide was similarly highly significant (p less than 0.001); as for Rt the time course for both drugs ran nearly parallel. Neither substance caused a significant rise in pulse rate at the dosages used.

Airway Resistance↗