The antihypertensive effect of pindolol (Visken) alone and combined with clopamide (Brinaldix)

Persson, I

doi:10.1007/bf00562931

Cited by 12 publications

(8 citation statements)

References 10 publications

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“…BrLSD was also more potent than D-LSD in increasing levels of dopa (32) and a dopamine metabolite, 3,4-dihydroxyphenylacetic acid (33), in rat striatum. Thus, agonist activity of BrLSD at dopaminergic (26) and serotonergic (27) sites is less than that of D-LSD but the antagonist activity at dopaminergic sites appears to be greater than that of D-LSD (31)(32)(33). Further evidence that D-LSD and BrLSD have affinities for the same receptors is that BrLSD blocks the effect of D-LSD on isolated tissue (34) and its behavioral effect in mice (35).…”

mentioning

confidence: 98%

Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

Green¹,

Johnson²,

Weinstein³

et al. 1977

Proc. Natl. Acad. Sci. U.S.A.

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D-Lysergic acid diethylamide and D-2-bromolysergic acid diethylamide are competitive antagonists of the histamine activation of adenylate cyclase [ATP pyrophosphate-lyase (cyclizing); E.C. 4.6.1.11 in broken cell preparations of the hippocampus and cortex of guinea pig brain. The adenylate cyclase is linked to the histamine H2-receptor. Both Dlysergic acid diethylamide and D-2-bromolysergic acid diethylamide show topological congruency with potent H2-antagonists. D-2-Bromolysergic acid diethylamide is 10 times more potent as an H2-antagonist than cimetidine, which has been the most potent H2-antagonist reported, and D-lysergic acid diethylamide is about equipotent to cimetidine. Blockade of H2-receptors could contribute to the behavioral effects of D-2-bromolysergic acid diethylamide and D-lysergic acid diethylamide.Evidence is growing that histamine may function as a neurotransmitter (see reviews, refs. 1-4). Histamine has a nonuniform regional distribution in brain. Most of the histamine is found in subcellular fractions containing nerve endings. Brain contains specific enzymes for histamine formation and metabolism. Histamine appears to turn over rapidly. Potassium ions release histamine from brain slices by a calcium-dependent process. Brain lesions result in a fall in the activity of histidine decarboxylase in areas distal to the lesion. Neurons respond to histamine. Histamine stimulates the activity of adenylate cyclase JATP pyrophosphate-lyase (cyclizing); EC 4.6.1.1] and this effect is blocked by histamine HI-antagonists (5, 6) and histamine H2-antagonists (6, 7). We show here that D-lysergic acid diethylamide (D-LSD) and D-2-bromo-LSD (D-BrLSD) are competitive antagonists of histamine in the activation of the H2-receptor linked to adenylate cyclase in the hippocampus arid cortex of the brain.MATERIALS AND METHODS Preparation of Tissue. Membrane-bound adenylate cyclase was prepared from brain by homogenization in a Potter-Elvejhem glass-Teflon vessel in 0.32 M sucrose/5 mM Tris-HCl/1 mM ethylene glycol bis(3-aminoethyl ether)-N,N'-tetraacetate (EGTA)/1 mM dithiothreitol pH 7.4. The homogenate was centrifuged at 1000 X g and the supernatant fraction was centrifuged again at 27,000 X g. The pellet from the second centrifugation was washed twice by resuspension in the same medium and collected by centrifugation. The final pellet was suspended in the same medium at a protein concentration of 0.5-0.7 mg/mi. The membranes could be quickly frozen with dry ice/acetone and stored at -70°. Freezing and storage invariably resulted in an increase in basal activity and a decrease in maximal histamine activation, but the agonist potencies (ED50; amount necessary to produce half-maximal response) and antagonist affinities (pA2) were not altered.Adenylate Cyclase Assay. The assay system has been described (8). All assays were performed in triplicate. All additions were made to the assay tubes on ice. They were then transferred to a 30°shaking incubator and preincubated for 5 min to allow the enzymatic activity ...

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mentioning

confidence: 98%

Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

Green¹,

Johnson²,

Weinstein³

et al. 1977

Proc. Natl. Acad. Sci. U.S.A.

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“…The structural resemblance of serotonin (2) to LSD was subsequently noted, and evidence accumulated suggesting that LSD exerts its effects through the serotoninergic neurotransmitter system (3-11). Convincing evidence also indicates dopaminergic involvement in LSD activity (12)(13)(14)(15)(16)(17)(18)(19) clearance); this piston, rotating at 500 rpm, was passed up and down 10 times. The crude homogenate was incubated at 370C for 60 min and then stored in 5-ml aliquots at -20°C for future use.…”

mentioning

confidence: 99%

“…The structural resemblance of serotonin (2) to LSD was subsequently noted, and evidence accumulated suggesting that LSD exerts its effects through the serotoninergic neurotransmitter system (3)(4)(5)(6)(7)(8)(9)(10)(11). Convincing evidence also indicates dopaminergic involvement in LSD activity (12)(13)(14)(15)(16)(17)(18)(19) as well as an a-adrenergic (20)(21)(22) and possibly a histaminergic component (23).…”

mentioning

confidence: 99%

Selective labeling of serotonin receptors by d-[3H]lysergic acid diethylamide in calf caudate.

Whitaker¹,

Seeman²

1978

Proc. Natl. Acad. Sci. U.S.A.

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Since it was known that d-lysergic acid diethylamide (LSD) affected catecholaminergic as well as serotoninergic neurons, the objective in this study was d-Lysergic acid diethylamide (LSD) has been extensively studied since its discovery (1). The structural resemblance of serotonin (2) to LSD was subsequently noted, and evidence accumulated suggesting that LSD exerts its effects through the serotoninergic neurotransmitter system (3-11). Convincing evidence also indicates dopaminergic involvement in LSD activity (12)(13)(14)(15)(16)(17)(18)(19) clearance); this piston, rotating at 500 rpm, was passed up and down 10 times. The crude homogenate was incubated at 370C for 60 min and then stored in 5-ml aliquots at -20°C for future use. Before use, the samples were thawed, resuspended with an additional 5 ml of buffer, and centrifuged at 39,000 X g for 15 min at 4°C. The supernatant was discarded and the pellet was resuspended in 15 ml of buffer by using five up-and-down strokes of a ground-glass homogenizer. This suspension was then homogenized by a Polytron homogenizer (Brinkmann, Westbury, NY) at a setting of 7 (full range = 10) for 10 sec, using a PT-10 homogenizer probe and a 50-ml polycarbonate tube to contain the suspension. This resulted in a final protein concentration of 0.2 mg per tube. Because the membrane homogenate was made up immediately prior to use, it was not necessary to store it on ice.Serotonin-Specific [3HJLSD Binding Assays. The assays were done by using 12 X 75 mm glass test tubes in which the following aliquots were placed (Eppendorf Brinkmann pipettes with polypropylene tips) for control binding: 0.1 ml of nonradioactive LSD (final concentration, 200 nM) or 0.1 ml of buffer; 0.1 ml of buffer containing apomorphine, phentolamine, and spiperone (final concentration, 50 nM for each, referred to as the APS system); 0.2 ml of [3H]LSD (11.5 Ci/mmol; New England Nuclear; final concentration, 2.0 nM); and 0.2 ml of brain homogenate. For tubes with varying concentrations of drugs competing against [3H]LSD, the final contents of the tubes were the same as for control except that the 0.1 ml of buffer or nonradioactive LSD was replaced with 0.1 ml of drug solution.Abbreviations: LSD, d-lysergic acid diethylamide; IC50, concentration that inhibits [3HJLSD binding by 50%; APS system, mixture containing 50 nM each of apomorphine, phentolamine, and spiperone.

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“…The assessment of these combinations by clinic blood pressure alone provides no information on the 24 h control of blood pressure. Pindolol has previously been shown to lead to a reduction in the blood pressure when used alone, which is enhanced when it is used in combination with the thiazide diuretic clopamide (Maetzel, 1978;Persson, 1977). This diuretic in combination with pindolol is marketed as Viskaldix, and has been shown to produce no change in potassium metabolism (Faupel & Gotzen, 1978).…”

Section: Discussionmentioning

confidence: 99%

“…Several studies have demonstrated its anti-hypertensive properties (Torok et al, 1979;Maetzel, 1978) and have demonstrated that a combination with the diuretic clopamide (Viskaldix) is more effective than the f3-adrenoceptor blocker given alone (Maetzel, 1978;Persson, 1977).…”

Section: Introductionmentioning

confidence: 99%

The effect of once daily beta‐adrenoceptor blocker‐thiazide diuretic combination on the ambulatory blood pressure.

Gould¹,

Hornung²,

Kieso³

et al. 1982

Brit J Clinical Pharma

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1 We have assessed the efficacy of Viskaldix, a combination of pindolol 10 mg and clopamide 5 mg using continuous intra-arterial ambulatory blood pressure monitoring. 2 Fourteen of the sixteen patients entered were studied on no therapy and following a minimum of 6 weeks at a constant dosage of Viskaldix. 3 Viskaldix produced a marked and consistent reduction of the blood pressure over the 24 h. The diurnal variation in the heart rate was decreased. 4 The results were compared with those of a similar study with once-daily pindolol where there was control during the day but not in the early morning when the blood pressures rose rapidly.

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The antihypertensive effect of pindolol (Visken) alone and combined with clopamide (Brinaldix)

Cited by 12 publications

References 10 publications

Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

Selective labeling of serotonin receptors by d-[3H]lysergic acid diethylamide in calf caudate.

The effect of once daily beta‐adrenoceptor blocker‐thiazide diuretic combination on the ambulatory blood pressure.

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