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At least 19 recordsLinked to original sources
PubMed1968

The formation and release of metaraminol during exposure to warm or cold environments.

1. Rats were injected intraperitoneally with alpha-methyl-m-tyrosine (400 mg/kg) and placed at either 27 degrees C or 4 degrees C. The levels of alpha-methyl-m-tyramine, metaraminol and noradrenaline were determined in heart tissue after 1, 4 and 12 hr of treatment. The excretion of metaraminol, alpha-methyl-m-tyramine, noradrenaline, adrenaline and 3-methoxy-4-hydroxyphenylglycol (MHPG) was also estimated in both treated and control rats.2. Cold exposure increased both the formation and excretion of metaraminol. Hearts removed from the cold-stressed rats 4 hr after injection contained significantly more metaraminol than hearts taken from animals maintained in the warm environment. Twelve hours after treatment, no metaraminol remained in the hearts of cold-exposed rats, whereas significant quantities of the amine still remained in the hearts of rats kept at 27 degrees C. These results support the false transmitter concept advanced for metaraminol as they demonstrate that in vivo sympathetic stimulation can increase both the formation and release of metaraminol.3. Alpha-methyl-m-tyrosine produced a greater fall in cardiac noradrenaline in the rats kept at 27 degrees C. Whereas an approximate mole-for-mole replacement of metaraminol for noradrenaline existed at 27 degrees C, no such relationships existed at 4 degrees C. Twelve hours after treatment the hearts of cold-stressed rats contained no metaraminol and only 40% of control noradrenaline levels. These results do not support the necessity for a mole-for-mole replacement of noradrenaline with metaraminol to produce a catecholamine loss.4. Alpha-methyl-m-tyrosine depressed the noradrenaline excretion for at least 24 hr in the cold-stressed rats. Excretion of 3-methoxy-4-hydroxyphenylglycol was also lower in the treated rats between 0 and 12 hr in the cold but rose abruptly between 12 and 24 hr to exceed the quantity excreted by the control animals. This increase suggests an increase in noradrenaline synthesis, which may be related to the depletion of metaraminol from the body.5. The results of this paper support the postulate that metaraminol may function as a false transmitter. They do not agree with the concept that the loss of noradrenaline from tissue sites is dependent upon a mole-for-mole replacement with metaraminol.

Animals↗
PubMed1970

Effects of chronic metaraminol treatment on the sympathetic activity of intact and adrenal demedullated rats kept in warm or cold environments.

1. Rats were placed at 27 degrees C or 4 degrees C and given metaraminol ((10 mg/kg)/day) in their drinking water for 8 weeks. One experiment was run using adrenal demedullated rats. These animals were treated with metaraminol, as mentioned above, and kept at 4 degrees C for 4 weeks.2. Body temperature and metabolic rate were determined at selected intervals. Urine was collected on day 7 of each week and analysed for adrenaline, noradrenaline, metanephrine, normetanephrine and 3-methoxy-4-hydroxyphenylglycol (MHPG). At the end of each study the rats were killed and the tissues removed and analysed for metaraminol, adrenaline and noradrenaline.3. All animals survived the metaraminol treatment and no change in metabolic rate or body temperature was seen. Metaraminol depressed the growth rate of the rats.4. Metaraminol caused a fall in tissue noradrenaline concentrations, with only negligible quantities being found in brain, heart, lung, liver, kidney and spleen. Only the adrenals contained significant quantities of catecholamines. All tissues contained large amounts of metaraminol.5. Despite the almost complete depletion of noradrenaline from sympathetic nerves, metaraminol did not depress the excretion of noradrenaline, normetanephrine and MHPG, in fact excretion of the latter two substances was higher in the treated animals. The failure of the drug to impair the normal cold-induced increase in noradrenaline secretion explains the survival of the rats at 4 degrees C.6. Adrenal demedullation did not prevent the metaraminol-treated rats from excreting large quantities of noradrenaline, normetanephrine and MHPG in the cold. It is apparent, therefore, that in the intact rats the noradrenaline emanated from the practically depleted nerves. The increase in MHPG excretion, seen during metaraminol treatment, suggests an increased rate of noradrenaline turnover.7. In conclusion, although metaraminol uptake is accompanied by a fall in tissue noradrenaline concentrations, the presence of metaraminol does not depress noradrenaline release. These results do not support the concept that metaraminol can replace noradrenaline and function as a false transmitter.

Adrenal Medulla↗
PubMedDate not supplied

Development of analytical methods for the detection of metaraminol in the horse.

Aramine (metaraminol bitartrate) has been found in the possession of horse trainers and veterinarians who have been investigated for possible inappropriate drug administration to racing horses. Metaraminol (3-hydroxyphenylisopropanolamine) is a sympathomimetic amine that directly and indirectly affects adrenergic receptors, with alpha effects being predominant. Because it has the potential to affect the performance of a racing horse, its use is prohibited. In the present study, methods for the detection of metaraminol were developed. Metaraminol was found to be extracted with poor recovery (< 50%) from aqueous solutions by routine basic extraction or cation exchange/reversed-phase solid-phase extraction techniques. However, an extractive acetylation method gave good (> 90%) recovery of metaraminol from aqueous samples. Sequential urine samples collected from horses administered metaraminol intramuscularly at 0.02, 0.10, and 0.23 mg/kg were extracted by the developed extractive acetylation procedure and analyzed by gas chromatography-mass spectrometry (GC-MS) in full-scan and selected ion monitoring modes. Norphenylephrine was used as an internal standard for quantitative analysis. The maximum concentration of metaraminol occurred between 1 and 2 h postadministration. Metaraminol was detected in the 0.23 mg/kg administration urine for 24 h postadministration. Metaraminol was detected for the 0.10 and 0.02 mg/kg doses for approximately 8 h postadministration. No apparent biotransformation products were observed in a reaction mixture of metaraminol and horse liver microsomal reaction mixture. Comparison of gas chromatograms of the extracts of the postadministration urine samples with those of the pre-administration samples failed to reveal any exogenous compound other than metaraminol.

Adrenergic Agents↗
PubMed1996

[11C]metaraminol, a false neurotransmitter: preparation, metabolite studies and positron emission tomography examination in monkey.

No-carrier-added racemic [11C]metaraminol was prepared by a selective condensation of [11C]nitroethane with 3-hydroxy-benzaldehyde using tetrabutylammonium fluoride in tetrahydrofuran (THF) as a catalyst, followed by a reduction with Raney nickel in formic acid. [11C]Metaraminol was produced in 30 to 45% decay-corrected yield from [11C]nitroethane (13 to 20% decay corrected from [11C]CO2) within 45 to 55 min total synthesis time. Reversed phase high-performance liquid chromatography (HPLC) was used for the separation of the racemic erythro- and threo-forms of [11C]metaraminol. The radiochemical purity was higher than 98%, and the specific radioactivity at the end of synthesis was 500 to 800 Ci/mmol (18 to 30 GBq/mumol). Positron emission tomography (PET) examination of racemic erythro-[11C]metaraminol in a Cynomolgus monkey showed a high uptake of radioactivity in the heart. Following pretreatment with the selective norepinephrine reuptake inhibitor desipramine, the radioactivity uptake in the myocardium was markedly reduced (80%), demonstrating the specificity of erythro-[11C]metaraminol for the norepinephrine reuptake system of the heart. Pretreatment with desipramine had no effect on radioactivity in lung. The metabolism was rapid for [11C]metaraminol. The amounts of the total radioactivity representing [11C]metaraminol in plasma, determined by HPLC, were 14% at 6 min and 8% at 34 min. The high specific uptake of racemic erythro-[11C]metaraminol indicates that enantiomerically pure (R,S)-[11C]metaraminol has potential for detailed mapping of the sympathetic innervation of the human myocardium.

Animals↗
PubMed1989

Effects of metaraminol on the secretion of fluid and glycoproteins from the rat submandibular gland.

The actions of metaraminol on the secretion of fluid and glycoproteins from rat submandibular glands were investigated using phentolamine, propranolol and reserpine. Metaraminol at doses from 1 to 8 mg/kg (i.p.) increased the salivation and the amounts of protein in submandibular saliva in a dose-dependent manner. The salivation induced by metaraminol at 2 mg/kg was inhibited strongly by pretreatment with propranolol, whereas the salivation induced by metaraminol at 8 mg/kg was inhibited strongly by phentolamine. Reserpine inhibited the secretion of fluid caused by both doses of metaraminol. The electrophoretic profiles of saliva evoked by metaraminol at 2 mg/kg revealed two main bands of glycoprotein, I and IV, which originated from the acinus, and the intensities of these bands were decreased by treatment with propranolol, whereas the major band in saliva induced by 8 mg/kg of metaraminol was glycoprotein III, which originated from the granular tubules. The intensity of band III was decreased by pretreatment with phentolamine. These results suggest that metaraminol, at small doses, stimulates mainly the beta-adrenoceptor in the acinus, whereas at large doses, it prominently stimulates the alpha-adrenoceptors in the granular tubules, although metaraminol at small and large doses is able to stimulate alpha- and beta-adrenoceptors in rat submandibular gland.

Animals↗
PubMed1975

[Effect of beta-phenylethylamine derivatives on the central nervous system. III. Motor activity changes in mice due to the intracerebral administration of metaraminol].

Influence of metaraminol on behavioural changes in mice was studied with the following results. 1) When metaraminol was injected i.c., spontaneous motor activity as tested by either the photocell counters method or open-field test markedly increased within 90 min after injection, while on the contrary greatly decreased 3 hr later as compared with control group. Thus, these biphasic effects of metaraminol were clearly established. 2) 30 min after injection, metaraminol in doses of 160 mug did not alter brain catecholamines in mice, however, 6 hr after injection, brain dopamine and norepinephrine markedly decreased. 3) When metaraminol was injected into mice pretreated with reserpine of 6-hydroxydopamine, spontaneous motor activity tested by photo-cell counters method markedly increased and anti-6-hydroxydopamine activity of metaraminol was stronger than anti-reserpine. 4) Metaraminol completely antagonized ptosis and catalepsy induced by rerserpine. 5) Six hr after injection, anti-methamphetamine activity was observed.

Animals↗
PubMed1970

Studies on the interrelationship between the syntheses of noradrenaline and metaraminol.

1. Experiments were conducted to determine the influence of the rate of noradrenaline synthesis on the conversion of alpha-methyl-m-tyrosine to metaraminol.2. Male Wistar rats, 175-200 g, were placed into four groups and treated with (1) alpha-methyl-p-tyrosine methyl ester, 250 mg/kg; (2) DL-alpha-methyl-m-tyrosine, 400 mg/kg; (3) alpha-methyl-p-tyrosine methyl ester, 250 mg/kg plus DL-alpha-methyl-m-tyrosine, 400 mg/kg; or (4) an equivalent volume of injection vehicle. All solutions were injected intraperitoneally.3. Immediately after treatment half of the rats were transferred to 4 degrees C with the remaining animals being kept at 27 degrees C.4. The rats were killed 4, 8 and 12 h after injection, the brains, hearts, spleens and adrenals removed and analysed for adrenaline, noradrenaline, metaraminol and alpha-methyl-m-tyramine.5. In virtually all cases, both during rest (27 degrees C) and sympathetic stress (4 degrees C), treatment of the rats with alpha-methyl-p-tyrosine methyl ester increased the amount of metaraminol formed from alpha-methyl-m-tyrosine. The only organ not containing increased quantities of metaraminol in the presence of alpha-methyl-p-tyrosine methyl ester was the adrenals, taken from the rats kept at 27 degrees C. Adrenals removed from the cold-exposed rats contained more metaraminol when alpha-methyl-p-tyrosine methyl ester was combined with alpha-methyl-m-tyrosine than when alpha-methyl-m-tyrosine was used alone.6. These results demonstrate that the inhibition of noradrenaline synthesis, by treatment with the tyrosine hydroxylase inhibitor alpha-methyl-p-tyrosine methyl ester, increased the conversion of alpha-methyl-m-tyrosine to metaraminol. It is concluded that inhibiting the formation of dopa allowed increased amounts of alpha-methyl-m-tyrosine to enter the biosynthetic pathway. These results support the false sympathetic transmitter concept advanced for metaraminol.

Adrenal Glands↗
PubMed1988

[Metaraminol in therapy of various forms of priapism].

A total of 19 patients (aged 17-66 years) with priapism received primarily conservative treatment in the form of aspiration of blood from the cavernous bodies and subsequent intracavernous (i.c.) administration of the alpha-adrenergic drug metaraminol. In 15 patients the priapism was due to i.c. injection of vasoactive agents; 1 patient each it had developed after hemodialysis, during oral prazosin medication, and in conjunction with Fabry's disease; and in 1 patient the etiopathogenesis was unknown. Treatment of priapism with metaraminol was successful in the first 15 patients and in 2 patients with priapism due to hemodialysis and oral prazosin medication. Therapy failed in long-lasting priapism associated with Fabry's disease and in priapism of unknown etiopathogenesis. Penile detumescence took place in the first 15 patients 3 min to 2.5 h after the injection of 2-4 mg metaraminol. Hemodialysis- and prazosin-linked priapism was treated with 5 and 2 mg metaraminol, respectively; in these patients erection subsided within 15 and 4 min after onset of therapy. In a further 2 patients in whom therapy had failed Al-Ghorab shunts were constructed, with the subsequent postoperative complication of erectile impotence. Injection of metaraminol must be carried out under strict supervision of the patient's circulatory system: doses of 4 mg metaraminol or more led to an increase in blood pressure and heart rate. In 15 patients with priapism induced by i.c. application of vasoactive agents, the analysis of blood gas parameters demonstrated a severe hypercapnia (70.3 +/- 10.0 mm Hg) and acidosis (pH 7.08 +/- 0.08) 5-10 h after the onset of erection, but severe hypoxia (37.0 +/- 16.6 mm Hg) was not found until erection had lasted for more than 10 h.(ABSTRACT TRUNCATED AT 250 WORDS)

Acid-Base Equilibrium↗
PubMed1982

Mechanisms of accumulation of tyramine, metaraminol, and isoproterenol in isolated chromaffin granules and ghosts.

The effects of the transmembrane pH gradient (delta pH) and the transmembrane potential gradient (delta psi) on the uptake of several sympathomimetic amines were investigated, using bovine adrenal chromaffin granules isolated in isotonic sucrose. As previously described [R. Johnson and A. Scarpa, J. Biol. Chem. 254 3750 (1979)], freshly isolated chromaffin granules maintain an intragranular pH of 5.5 as measured by [14C] methylamine distribution and, in the presence of ATP, generate a delta psi of 80 mV, positive inside, as measured by [14C] methylamine distribution. When tyramine, metaraminol, and isoproterenol (1-50 mM) were added to well-buffered suspensions of granules at pH 7.0, a dose-related alkalinization of the granule interior was observed. Study of the time-resolved influx of the same amines labeled radiochemically (5-21 microM) revealed that all the amines were accumulated against an apparent concentration gradient. However, while accumulation of [14C] serotonin and [3H] isoproterenol was totally inhibited by reserpine, [14C] tryramine accumulation was inhibited by only 60% and [14C[ metaraminol uptake was unaffected. The ATP-dependent generation of a delta psi produced a stimulation of amine uptake in the order: serotonin greater than isoproterenol greater than tyramine; metaraminol accumulation was not enhanced by ATP addition. The relationship between the electrochemical proton gradient (delta micro H+) and the electrochemical gradient for each of the sympathomimetic amines (delta micro A) was investigated utilizing chromaffin ghosts devoid of endogenous matrix gradients or components. All amines were accumulated in the presence of delta pH alone. In the presence of delta psi alone, [14C] serotonin, (14C] tyramine, and [3H] isoproterenol were accumulated, but no [3H] metaraminol uptake was demonstrable. The results indicate that serotonin and isoproterenol accumulated in isolated chromaffin granules and ghosts via a reserpine-sensitive mechanism, driven by the magnitude of the electrochemical proton gradient. Conversely, metaraminol permeated the membrane of the chromaffin granule through the apolar lipid phase and distributed according to the delta pH alone. Tyramine uptake proceeded by both mechanisms. The implications of the mechanism of accumulation of these potent physiologic and pharmacologic agents for their in vivo action are discussed.

Adenosine Triphosphate↗
PubMed1980

Comparison of 3H-norepinephrine and 3H-metaraminol accumulation as indices of adrenergic nerve density in rabbit blood vessels.

The possibility that accumulation of 3H-metaraminol, which is not metabolized, would provide a better estimate of adrenergic nerve density than 3H-norepinephrine accumulation was examined in a series of rabbit blood vessels. Accumulation of 3H-metaraminol was linear for up to 10 min. Norepinephrine accumulation was correlated with metaraminol acumulation in the vessels studied, but the relationship was not a simple one. The findings suggest that, even with short incubation times, metabolism may significantly alter the amount of norepinephrine retained by the tissue. Nevertheless, accumulation of metaraminol was still not well-correlated with endogenous norepinephrine content. Norepinephrine contents of the basilar artery, mesenteric artery and mesenteric vein were quite similar: 2.7, 2.8 and 2.8 micrograms/g respectively. However, values for metaraminol accumulation in these vessels ranged from 8.7 to 1.78 ml cleared/g. These findings suggest that norepinephrine content of a single adrenergic varicosity may vary from tissue to tissue. The relationship between norepinephrine content, storage capacity, uptake activity and transmitter release needs to be more carefully examined. No single parameter can provide an adequate estimate of adrenergic nerve density.

Adrenergic Fibers↗
PubMedDate not supplied

Comparative anorectic effects of metaraminol and phenylephrine in rats.

Structure-anorectic activity relationship of two substituted amphetamines has been investigated in this study. Literature reports showed conflicting results in their anorectic activities in spite of the similarity in chemical structures of metaraminol and phenylephrine. Hence, the effects of alpha-carbon atom substitution and primary (metaraminol) and secondary amine (phenylephrine) moieties of these substituted amphetamines on the anorexia of rats were investigated in this study in nonfood- and food-deprived rats. Food intake at 1, 3, 14, and 24 h intervals, water intake at a 24-h interval, and body weight alteration for 10 days were monitored after daily drug administration for 3 consecutive days. Both metaraminol and phenylephrine were found to be potent anorectic. The relative anorectic potencies of phenylephrine were 0.54 and 0.81 of that of metaraminol at 1- and 3-h intervals, respectively. Body weight of rats treated with metaraminol (5.0 mg/kg) and phenylephrine (10 mg/kg) decreased significantly from Days 1 to 9.

Animals↗
PubMed1987

Effect of metaraminol during acute inferior wall myocardial infarction accompanied by hypotension: preliminary study.

This study was designed to evaluate the effects of metaraminol (Aramine) in six patients with evolving acute inferior wall myocardial infarction accompanied by hypotension and warm limbs. There were 16 episodes of acute inferior wall ischemia, and the response to therapy was judged by evaluating blood pressure and ST segment and T wave abnormalities. Three patients received intravenous isosorbide dinitrate and two received streptokinase as the initial therapy. The mean ST segment elevation was significantly reduced (from 4.94 +/- 1 to 0.5 +/- 0.7 [p less than 0.0001]) after metaraminol infusion was initiated. The average T wave height also decreased (from 6.8 +/- 2 to -1.3 +/- 2.5 mm [p less than 0.0005]). The average heart rate decreased from 82 +/- 11 to 69 +/- 9 beats/min (p less than 0.05) and the mean arterial blood pressure increased from 81 +/- 12 mm Hg before metaraminol treatment to 126 +/- 8 mm Hg after treatment. All these changes occurred within a few minutes after metaraminol therapy was instituted. In 12 episodes, accelerated idioventricular rhythm appeared concomitantly with the resolution of ST segment elevation. Coronary angiography performed between 4 and 10 days after admission demonstrated significant obstruction in all infarct-related arteries, but none was totally occluded. Left ventricular function was normal in three patients and slightly hypokinetic in the inferior wall in two. These results indicate that in a selected group of patients with acute inferior myocardial infarction, metaraminol administration (in certain hemodynamic circumstances) can alleviate acute ischemia within a few minutes and thereby reduce ischemic injury.

Adult↗
PubMed1996

Hypotension during subarachnoid anaesthesia: haemodynamic effects of colloid and metaraminol.

We have studied 45 patients, aged 60-95 yr, receiving subarachnoid block for neck of femur fractures. Patient received either colloid (polygeline, Haemaccel) 8 ml kg-1 (n = 15), metaraminol 5 micrograms kg-1 and 1.7 micrograms kg-1 min-1 (n = 15) or a combination of both treatments to maintain systolic arterial pressure (SAP) between 75 and 100% of baseline. If necessary, additional colloid 2 x 4 ml kg-1 or metaraminol 3 x 2.5 micrograms kg-1 was given. Arterial pressure was measured by automated oscillotonometry, central venous pressure (CVP) by a manometer and cardiac index (CI), stoke index (SI) and heart rate (HR) by transthoracic electrical bioimpedance. Systemic vascular resistance index (SVRI) was derived. Colloid was less effective than metaraminol (P < 0.05). In the colloid group, SAP and SVRI decreased and CVP, CI and SI increased (P < 0.001). In the metaraminol group, initial decreases in SAP, SVRI and CVP were restored after 10-15 min and HR decreased after 12 min (P < 0.001). In the combined group, initial decreases in SAP and SVRI were restored after 4 and 16 min, and CVP, CI, SI and HR increased (P < 0.001). Metaraminol was more effective than colloid because it increased SVRI, whereas colloid increased CVP without significantly increasing CI.

Aged↗
PubMed2001

Comparison of metaraminol and ephedrine infusions for maintaining arterial pressure during spinal anesthesia for elective cesarean section.

BACKGROUND: Although ephedrine is usually recommended as the first-line vasopressor in obstetrics, its superiority over other vasopressors has not been proven in humans. METHODS: In a double-blind study, the authors randomized women having elective cesarean section with spinal anesthesia to receive an intravenous infusion of ephedrine, starting at 5 mg/min (n = 25), or metaraminol, starting at 0.25 mg/min (n = 25), titrated to maintain systolic arterial pressure in the target range 90-100% of baseline. Umbilical cord gases, maternal hemodynamics, uterine artery puLsatility index, and Apgar scores were compared. RESULTS: Systolic arterial pressure was maintained more closely in the target range in the metaraminol group compared with the ephedrine group. In the metaraminol group, umbilical arterial pH was greater (median and interquartile range, 7.31 and 7.31-7.33 vs. 7.24 and 7.14-7.29; P < 0.0001), and umbilical venous pH was greater (7.36 and 7.35-7.38 vs. 7.33 and 7.26-7.34; P < 0.0001) compared with the ephedrine group. No patient in the metaraminol group had umbilical arterial pH less than 7.2, compared with nine patients (39%) in the ephedrine group (P = 0.0005). Apgar scores were similar between groups. Changes in uterine artery pulsatility index were similar between groups. CONCLUSIONS: When used by infusion to maintain arterial pressure during spinal anesthesia for cesarean section, metaraminol was associated with less neonatal acidosis and more closely controlled titration of arterial pressure compared with ephedrine.

Adult↗
PubMed1971

Effects of Na+ and K+ on the uptake of metaraminol by rabbit ventricular slices.

1. The ionic dependence of [(3)H]-metaraminol transport by rabbit ventricular slices was studied.2. Transport was Na(+) dependent. Choline, Li(+), K(+), Rb(+) or Cs(+) could not be substituted for Na(+).3. Transport was K(+) dependent. Rb(+) and Cs(+), but not Li, could be substituted for K(+), their relative potencies being K(+) = or >Rb(+)>Cs(+)>>Li(+). Higher concentrations of K(+), Rb(+), Cs(+) and Li inhibited [(3)H]-metaraminol transport.4. The inhibitory effects on transport of either a marked reduction in the concentration of Na(+) or of omission of K(+) were rapidly reversible on exposure of slices to Krebs solution.5. The inhibitory effect of ouabain on [(3)H]-metaraminol transport was markedly time dependent, being significantly increased by preincubation with ouabain. The inhibitory action of ouabain was not affected, however, by the Na(+) concentration present during preincubation.6. An inwardly directed Na(+) gradient did not increase [(3)H]-metaraminol transport in slices in which Na(+) pumping had been prevented by 10(-5)M ouabain, 4 degrees C, omission of K(+) or by metabolic inhibition.7. These findings provide additional evidence that the Na(+) and K(+) activated adenosine triphosphatase may participate in the transport of metaraminol and related amines. In the absence of Na(+) pumping, induced Na(+) gradients were unable to produce transport of amine as would be predicted by the co-transport model proposed by Bogdanski & Brodie (1969).

Adenosine Triphosphatases↗
PubMed2001

A comparative study of three different methods of administering metaraminol during spinal anaesthesia in the elderly.

We compared three methods of administering metaraminol during spinal (subarachnoid) anaesthesia. Fifty-two elderly patients with fractured hips were studied. Blood pressure was maintained by either intramuscular (i.m.) metaraminol (0.1 mg x kg(-1)), intravenous (i.v.) boluses (0.01 mg x kg(-1)) or an infusion (0.05 mg x kg(-1) x h(-1)). Non-invasive blood pressure was recorded every one-minute. Spinal anaesthesia initially decreased the systolic arterial pressure by 15 (14) % compared to 35 (15) % for diastolic pressure (P<0.001). I.m. metaraminol restored the systolic arterial pressure back to baseline values (-3%), but there was significant between-subject variability resulting in a very unpredictable effect. I.v. boluses and infusion had a more predictable effect and maintained systolic arterial pressure at about 20% below baseline. Range of effect, measured by inter-quartile range and variance, was greatest in the i.m. group and least in the infusion group (P<0.003). I.m. metaraminol during spinal anaesthesia has a very unpredictable effect. Infusions of metaraminol provided the best blood pressure control. Diastolic blood pressure fell significantly after spinal anaesthesia and this merits further investigation.

Aged↗
PubMed1975

Uptake and release of 3-H-metaraminol by rat lung. Basic aspects, ionic and energy requirements.

The accumulation of 3H-metaraminol in incubated lung tissue of the rat was examined in vitro. Lung tissue concentrated tritium after incubation with 3H-metaraminol. This uptake proceeds against a concentration gradient and shows saturation kinetics (Km 12.5 X 10(-7) M and Vmax 2.105 nM/g/15 min.) with great affinity for 3H-metaraminol. The accumulation of 3H-metaraminol is dependent of temperature and energy supply, and requires the presence of sodium ions. The loss of accumulated radioactivity showed the possibility that a small fraction of metaraminol is apparently firmly boune (e.g. neuronal sites), while a greater portion is taken up by extraneuronal structures (e.g. capillary endothelial cells). The first localization could represent uptake-1 and the second uptake-2. The results obtained also confirm the important role of the lungs as an organ which participates in the fate of endogenous substances and drugs.

Animals↗
PubMed1975

[Effect of beta-phenylethylamine derivatives on the central nervous system. II. Pharmacological effect of the intracerebral administration of metaraminol on the central nervous system].

Six hours after intracerebral administration, the central effects of metaraminol were examined with the following results. 1) Metaraminol in doses of 40 approximately 160 mug decreased spontaneous motor activity in mice as measured by the photo-cell counters method, the wheel cage method or the open-field test. Ptosis and catalepsy induced at these doses. 2) Metaraminol in doses of 40 approximately 80 mug which influenced the spontaneous motor activity in mice, blocked the avoidance behaviour but not escape. 3) Metaraminol in doses of 1.25 approximately 10 mug which did not influence the spontaneous motor activity in mice, markedly blocked the attaching response induced by the electroshock. 4) Ten min after intraventricular administration, metaraminol in a dose of 500 mug induced the arousal pattern of EEG in sensory cortex of cats and this pattern lasted for 30 min. Ninety min after administration, EEG tracings reverted to the drowsy pattern.

Aggression↗