A method for the fluorimetric determination of 4-(2-Hydroxy-3-isopropylaminopropoxy)-indole (LB 46), aβ-blocking agent, in plasma and urine

Pacha, W.

doi:10.1007/bf01897885

Cited by 73 publications

(24 citation statements)

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“…For instance in the rat, the biological half-life for the disappearance of pindolol from plasma, following oral or intravenous administration, is reported to be approximately 30 min (Pacha, 1969). Moreover in rats, pindolol is extensively metabolized, the metabolites arising principally from side-chain conjugation with glucuronic acid, hydroxylation or oxidation and conjugation of the indole ring, and oxidative ring scission (Kiechel et al, 1975).…”

Section: Discussionmentioning

confidence: 99%

Studies on the Cardiovascular Effects of Pindolol in Doca/Saline Hypertensive Rats

Buckinghamm

Hamilton

Robson

1977

British J Pharmacology

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1 A hypotensive response to orally administered pindolol in conscious normotensive and deoxycorticosterone acetate (DOCA)/saline hypertensive rats (DS‐rats) is described. In DS‐rats, pindolol (10‐50 μg/kg) produced a dose‐dependent fall in blood pressure and elevation of resting heart rate. 2 The hypotensive response and tachycardia produced by oral pindolol (50 μg/kg) in DS‐rats were prevented by propranolol (5 mg/kg), suggesting that pindolol's effects are mediated by β‐adrenoceptor stimulation. 3 After mecamylamine (10 mg/kg), oral pindolol (50 μg/kg) produced a further fall in blood pressure in DS‐rats, suggesting that its hypotensive effects are probably mediated in the peripheral vasculature. 4 Pretreatment with oral pindolol (10 or 50 μg/kg) resulted in a reduction of neuronally‐induced tachycardia in pithed DS‐rats; neuronally‐evoked pressor effects were also antagonized by pindolol (50 μg/kg, orally). 5 Whereas pindolol, 50 μg/kg orally or intraperitoneally, produced a marked and progressive hypotensive response of rapid onset (20 min) in DS‐rats the same dose intravenously produced a smaller response of delayed onset (80 minutes). 6 In anaesthetized DS‐rats, an equivalent degree of cardiac β‐adrenoceptor blockade was produced by pretreatment with pindolol, 50 μg/kg orally (2 h previously) or intravenously (1 h previously). 7 After administration of pindolol, 2 mg/kg intravenously, to conscious DS‐rats, the tachycardia produced by intravenous isoprenaline, 3 μg/kg, was almost abolished for the first 60 min of the study, whereas a hypotensive response to pindolol was delayed in onset (100 minutes). 8 The hypotensive response and tachycardia produced by oral pindolol, 50 μg/kg, in DS‐rats were prevented by inhibition of metabolic enzyme activity by pretreatment with Proadifen (SKF 525‐A), 80 mg/kg. 9 The results suggest that pindolol's effects on blood pressure and heart rate in the conscious DS‐rat are mediated by a metabolite(s) acting by stimulation of peripheral β‐adrenoceptors.

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Section: Discussionmentioning

confidence: 99%

Studies on the Cardiovascular Effects of Pindolol in Doca/Saline Hypertensive Rats

Buckinghamm

Hamilton

Robson

1977

British J Pharmacology

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“…In all the studies the drug was determined in plasma and urine by a fluorimetric method (Pacha, 1969). This method proved to be sensitive and specific for the unchanged drug, because the polar metabolites (Kiechel, Niklaus, Schreier & Wagner, 1975) were eliminated by the extraction procedure.…”

Section: Pindolol Ap-adrenoceptor Blocking Agent With a Negligible Fmentioning

confidence: 99%

Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Meier¹,

Nüesch²

1977

Brit J Clinical Pharma

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“…Metoprolol was assayed according to Ervik (1975), atenolol according to Scales & Copsey (1975), and pindolol according to Pacha (1969). As seen from Table 1 blood samples for catecholamine determination were obtained at rest and at peak exercise, i.e.…”

Section: Introductionmentioning

confidence: 99%

Comparison of beta‐adrenoceptor blockers under maximal exercise (pindolol v metoprolol v atenolol).

Erikssen¹,

Thaulow²,

Mundal³

et al. 1982

Brit J Clinical Pharma

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1 The time-related, comparative 3-adrenoceptor blocking effect of metoprolol 150 mg twice daily, atenolol 100mg once daily and pindolol 7.5 mg twice daily on heart rate, blood pressure, work performance, blood lactate, free fatty acids and plasma catecholamines was studied in ten males aged 19-25 years by means of repeated maximal bicycle exercise tests. 2 At steady state several differences in effects were noted among the drugs. These could be explained by differences in P3-selectivity, potency of the chosen drug-doses and intrinsic sympathomimetic activity (ISA). 3 This study emphasizes the importance of including strong sympathetic stimuli in any model used for comparing 3-adrenoceptor blockers with and without ISA in order not to underrate the effects of 1-adrenoceptor blockers with ISA.4 In the chosen doses pindolol was more effective, and atenolol less effective than metoprolol in suppressing heart rate and blood pressure responses to maximal exercise.

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A method for the fluorimetric determination of 4-(2-Hydroxy-3-isopropylaminopropoxy)-indole (LB 46), aβ-blocking agent, in plasma and urine

Cited by 73 publications

References 0 publications

Studies on the Cardiovascular Effects of Pindolol in Doca/Saline Hypertensive Rats

Studies on the Cardiovascular Effects of Pindolol in Doca/Saline Hypertensive Rats

Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Comparison of beta‐adrenoceptor blockers under maximal exercise (pindolol v metoprolol v atenolol).

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