Photodimerization of chlorpromazine radical CPZS.+ under the irradiation of UV light.

CPZS.+ radical excited at S atom in the phenothiazine ring was obtained by illumination of aqueous solution of chlorpromazine (CPZ..) for 15 min with UV light (303 nm). The radicals in oxygenated solution formed green, dimeric photoproduct CPZSOOSCPZ (m. wt. 628 +/- 1) lambda max. 741.9 nm, IR spectrum 760, 1470, 3400 cm1, fluorescence emission at 485 nm (max. excitation 365 nm). The dimer decomposed in alkaline methanol (pH 10.0) with intensive luminescence (max. at 500 nm).

Crystalline free radical of chloropromazine.

The method of preparation and the spectral characteristic of the crystalline free radical of chlorpromazine are described. Two absorption maxima at 770 and 860 nm concomitant with those at 530 and 277 nm were found. The highest rate of dismutation of the radical was 4-4.10(-1) M. sec-1 at pH 7-2. The mechanism of luminescence during the decay of the peroxide form of th radical is discussed.

The isolation and fluorometric determination of 3-methoxytyramine in urine and in tissues.

A fluorometric methods is described for determination of cardiac and urinary 3-methoxytyramine, a metabolite of dopamine. Methoxy metabolites were isolated on Amberlite CG-50 resin and oxidation to emitter form was performed with K3Fe(CN)6. Good specificity and sensitivity of determination, and a high recovery of 3-MT were obtained.

Isolation and fluorometric determination of homovanillic acid in urine and tissues.

The fluorometric method is described for determination of the final product of dopamine metabolism homovanillic acid in urine, amniotic fluid and tissue extracts. The metabolite was isolated using three chromatographic columns (1-Amberlit CG-50, 2-Dowex AG 1 x 2, 8-Aluminium oxide). Oxidation of eluates to emitter was done with potassium ferricyanide in alkalic medium. The use of internal standards made high recovery of compound and a good specificity and sensitivity of detection.

Changes in plasma high density lipoproteins (HDL) levels after salbutamol.

Administration of salbutamol--in a single dose of 0.5 mg i.v. and in a dose of 8 mg twice daily during two weeks--was associated with an increase of HDL-cholesterol concentration in the serum of patients with chronic bronchitis and severe airway obstruction. At the end of the second week of oral treatment with salbutamol, the HDL-cholesterol concentration in serum increased by 6.9% (p less than 0.01).

Pharmacodynamics of salbutamol in humans.

Twenty patients with mild chronic bronchial asthma (females and males between 45-69 years old) treated with single dose of 0.5 mg at 1 ml of salbutamol were investigated. Measurements of heart rate, blood pressure, peak expiratory flow rate (PEFR) and plasma concentration or glucose, potassium and non-esterified fatty acids-NEFA, and salbutamol plasma levels were recorded at the same time before and 2, 5, 15, 30, 60, 75, 90, 120, 180, 240, and 360 min after salbutamol injection. Decrease in heart rate, blood systolic pressure and metabolic changes correlated with the salbutamol plasma level. Increase in PEFR was elevated much longer.

Suppression of catecholamine excretion by low doses of clonidine in healthy subjects and feasibility study on clonidine application in angina pectoris.

The effect of low doses of clonidine (CL) (150 microgram/day p.o.) on catecholamine (CA) excretion, blood pressure (BP) and heart rate (HR) was investigated in a double-blind way on 9 healthy volunteers. CL administration for two consecutive days led to marked diminution of urinary CA, mainly of epinephrine, with only slight decrease in systolic BP and HR. The results show that this dose of CL is effective in suppressing adrenergic tone as reflected by the magnitude of CA excretion, without marked influence upon systemic BP. Subsequently, the same dose of the drug was administered for two weeks to 30 unselected patients with intractable angina known to be often associated with adrenergic overactivity. Clinical improvement manifested by complete disappearance of coronary pains or marked decrease in the incidence of anginal attacks was achieved in the majority (over 60%) of patients. Although best results were seen in patients with borderline hypertension, the drug was also effective in normotensive patients and no untoward hypotensive symptoms were noted throughout the trial. Blood CA and free fatty acids (FFA) measurements performed in 5 patients showed that favourable clinical effect of CL therapy coincides with lowering of CA and FFA levels. This study indicates that CL administered in a dose which does suppress adrenergic activity might be of value in the treatment of coronary patients. Favourable results of this preliminary trial incline to undertake well controlled clinical study.