PubMed Health⌕ Search

Biomedical subjects

B N Wu

Publications and source records attributed to B N Wu.

24 records · Page 2Linked to original sources
PubMed1994

Vaninolol: a new selective beta 1-adrenoceptor antagonist derived from vanillin.

The beta-adrenoceptor blocking properties of vaninolol ((+/-)4-[4'-(2-hydroxy-3-tert-butyl-aminopropoxy)-3'-methoxyphenyl]- 3-buten-2-one), derived from vanillin, were first investigated under in vivo and in vitro conditions. Vaninolol (0.1, 0.5, 1.0 mg/kg, i.v.), as well as propranolol, produced a dose-dependent bradycardia response and a sustained pressor action in urethane-anesthetized normotensive rats. Vaninolol inhibited the tachycardia effects induced by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by phenylephrine. These findings suggested that vaninolol possessed beta-adrenergic blocking activity, but was without alpha-adrenergic blocking activity. In isolated guinea-pig tissues, vaninolol antagonized (-)isoproterenol-induced positive inotropic and chronotropic effects of the atria and tracheal relaxation responses in a concentration-dependent manner. The parallel shift to the right of the concentration-response curve of (-)isoproterenol suggested that vaninolol was a beta-adrenoceptor competitive antagonist. The effect of vaninolol was more potent on the atria than on tracheal tissues, indicating it had some beta 1-adrenoceptor selectivity. On the other hand, the order of the hydrophilicity was atenolol >> vaninolol > propranolol. In addition, vaninolol had a mild direct cardiac depression at high concentrations and was without intrinsic sympathomimetic activity (ISA). Furthermore, binding characteristics of vaninolol and other beta-adrenoceptor antagonists were evaluated in [3H]dihydroalprenolol binding to guinea-pig ventricular membranes. The order of potency of beta-adrenoceptor antagonists in competing for the binding sites was (-)propranolol >> vaninolol > or = atenolol. In conclusion, vaninolol was found to be a selective beta 1-adrenoceptor antagonist with relatively low lipophilicity in comparison with propranolol, devoid of ISA, and had a mild myocardial depressant effect.

Adrenergic beta-1 Receptor Antagonists↗
PubMed1994

A new beta-adrenoceptor blocking agent derived from dehydrozingerone.

1. Dehydrozingeronolol (DZPN; 0.1, 0.5, 1.0 mg/kg, i.v.) produced a dose-dependent bradycardia response and a sustained pressor action in urethane-anesthetized normotensive rats. DZPN inhibited the tachycardia effects by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by phenylephrine. 2. In in vitro study, DZPN antagonized (-)isoproterenol-induced positive chronotropic effects in guinea-pig isolated right atria and relaxation responses in rat isolated uterus horns. 3. DZPN causes mild direct cardiac depression at high concentrations without intrinsic sympathomimetic activity (ISA). 4. The order of potency of beta-adrenoceptor antagonists in competing for the [3H]dihydroalprenolol binding sites was (-)propranolol >> DZPN > or = atenolol.

Adrenergic beta-Antagonists↗
PubMed1991

Vanidil: a newly synthesized antiangina nonvolatile organic solid nitrate.

Newly synthesized Vanidil (4-o-(1,2-dinitroglyceryl)-6-nitrovanillic acid) is a nonvolatile organic solid nitrate, mp: 85 degrees C. In in vitro tests, Vanidil can inhibit 3,4-diaminopyridine (2 x 10(-2) M) induced pig coronary rhythmic vasocontraction, a prelude to coronary vasospasm, and nonrhythmic tonic vasocontraction. Vanidil is suggested as a potential antiangina agent.

Angina Pectoris↗
PubMed1990

[Comparative study on the pharmacokinetics and bioequivalence of two brands of norfloxacin preparation].

The pharmacokinetics and bioequivalence of two norfloxacin, Gentle capsule and Baccidal tablet, were compared in eight healthy male volunteers. A 400 mg dose of norfloxacin was given orally after an overnight fasting to volunteers in a balanced two-way cross-over study. Blood samples were obtained at 0, 0.5, 1.0, 2.0, 4.0, 8.0, 12.0 and 24.0 hours after the dosing. Norfloxacin concentration in serum was assayed by a high pressure liquid chromatographic method using an UV detector. All the data was processed by KMCP computer software and the pharmacokinetic parameters were calculated, based on one-compartment model. The results revealed that the maximal concentration (Cmax) of Gentle and Baccidal was 0.96 +/- 0.089 and 0.99 +/- 0.110; the time to reach maximal concentration (Tmax) was 2.0 +/- 0.0 for both; the elimination constant (Kel) was 0.101 +/- 0.006 and 0.098 +/- 0.005 hr-1; the elimination half life (T1/2, beta) was 6.909 +/- 0.483 and 7.094 +/- 0.350 hr; the absorption constant (Ka) was 2.444 +/- 0.188 and 2.490 +/- 0.096 hr-1; the absorption half life (T1/2, alpha) was 0.278 +/- 0.019 and 0.277 +/- 0.010 hr; the area under curve (from 0 to 12 hours) (AUC0-12) was 7.106 +/- 1.065 and 7.380 +/- 1.044 micrograms.hr/ml; and the area under curve (from 0 hour to infinity) (AUC0-infinity) was 9.183 +/- 1.257 and 9.550 +/- 1.300 micrograms.hr/ml respectively. There were no significant difference found between the two groups after statistical analysis with two-way ANOVA (p greater than 0.05). A series of statistical parameters including d%, delta, and 95% C.I. were calculated by a bioequivalence test computer software of Yamaoka Simi. In order to strengthen the statistical evidence, the power of the test (1 - beta) was also calculated. After evaluating all the parameters, there was no significant difference found between the two groups. Therefore, the high similarity of these two formulations is suggested by the authors.

Adult↗
PubMed1983

Postweaning copper restriction and behavior in the Long-Evans rat.

A variety of behaviors was assessed in Long-Evans male rats placed on either a low copper diet, a marginal copper diet, or an adequate copper diet at weaning. Rats in the low copper group had slightly, but significantly, enlarged hearts and gained less weight than rats fed diets containing higher copper levels. Treatment effects were not detected in measurements of muricide, open-field activity, water intake, shock sensitivity, and shock avoidance and memory.

Animals↗