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At least 739 records · Page 41Linked to original sources
PubMed1976

[Relationship between biogenic amines and analgesic action of difenamizole in heat induced reflexes].

Effects of drugs that modify catecholaminergic or tryptaminergic mechanisms were determined in experimental animals regarding the analgesic action of difenamizole, morphine, and aminopyrine. Analgesia was assessed by the hot plate method in mice and the hot water induced tail withdrawal reflex in rats. Both 5-hydroxytryptophan (5-HTP) and L-dopa potentiated the analgesic action of morphine, but antagonized the action of difenamizole in the hot plate test. p-Chlorophenylalanine (pCPA), alpha-methyl-p-tyrosine (alpha-MT), and reserpine antagonized the effect of morphine as assessed by this same test. alpha-MT potentiated the analgesic action of difenamizole. The analgesic action of aminopyrine was hardly modified in the hot plate method by pretreatment with 5-HTP, pCPA, L-dopa, and alpha-MT. In rats, 5-HTP antagonized the effect of morphine, while pCPA, L-dopa, and alpha-MT caused no appreciable change in the analgesic action of morphine in the hot water induced tail withdrawal reflex. The effect of difenamizole was not modified by pretreatment with these monoamine-related drugs. On the other hand, brain 5-hydroxytryptamine content was increased by pretreatment with 5-HTP in both tests. These results suggest that the analgesic action of difenamizole and morphine, as measured in the hot plate test in mice, may be mediated by catecholamines and 5-hydroxytryptamine, but that other mechanisms may be involved in the hot water induced tail withdrawal relfex in rats. In addition, the biogenic amines may play a different role depending on the type of analgesic.

5-Hydroxytryptophan↗
PubMed1991

Effects of brain biogenic amines of repeated treatments with calcium antagonists.

Discrete brain sections were obtained from rats once or repeatedly (once a day for 5 days) given i.p. nifedipine, verapamil or diltiazem at doses ranging from 5 to 20 mg/kg. The biogenic amines and metabolites in the hypothalamus, brainstem, hippocampus, striatum, cortex and thalamus-midbrain were determined by high-performance liquid chromatography with electrochemical detection. The drug-induced changes, displaying regional specificity and differences according to the various compounds, suggested that: (a) serotonergic systems were activated, especially in fasted rats or after repeated treatment; (b) the dopaminergic system of the striatum was inhibited by nifedipine which did reduce the HVA levels and the HVA/DA, as well as the DOPAC/DA, ratio. These effects disappeared after repeated treatment. It was also speculated that the data obtained could be of great interest in view of the possible use of calcium antagonists to treat disorders of the central nervous system.

Animals↗
PubMed2006

Central nervous system biogenic amine targets for control of appetite and energy expenditure.

Central biogenic amine systems have long been studied for their effects on feeding behavior, energy balance, and maintenance of body weight. Those monoaminergic systems that use dopamine (DA), norepinephrine (NE), and serotonin (5-hydroxytryptamine, 5-HT) as neurotransmitters have been the main targets of study. A number of antiobesity medications that affect monoaminergic activity have appeared on the market and/or in clinical trials. Early examples of such agents are the so-called CNS stimulants, e.g., the amphetamines, phentermine, ephedrine, etc. These agents release monoamines from neuronal stores, and their antiobesity activity seems to be tied most closely to their ability to release NE. Inhibitors of neuronal reuptake of NE or 5-HT have been shown to reduce feeding and weight gain both preclinically and clinically. However, the magnitude and sustainability of such effects in clinical trials has generally not been great enough to register or label these agents for the treatment of obesity. Sibutramine, however, is an exception. This compound is metabolized in vivo to produce metabolites that have varying degrees of inhibition of NE, 5-HT, and/or DA uptake. Sibutramine is the only drug affecting monoaminergic systems currently approved for the long-term control of obesity. Research continues on serotonergic and histaminergic systems to determine if targets such as the 5-HT2C and H3 receptors may be suitable for developing antiobesity agents. Because the clinical antiobesity effects of monoaminergic drugs have been modest, future directions include looking at combinations of different monoaminergic mechanisms and/or combinations of monoaminergic drugs with non-monoaminergic mechanisms.

Anti-Obesity Agents↗
PubMed1977

[Effect of biogenic amines on rat anterior pituitary cyclic AMP].

The effects of biogenic amines on the formation of adenosine-3',5' monophosphate (cAMP) in the anterior pituitary of rats were investigated. Pituitary halves were preincubated in a Krebs-Ringer bicarbonate buffer (pH 7.4) containing theophylline (10(-2)M) at 37 degrees C for 30 minutes and incubated in a fresh buffer for 15 minutes after the addition of test substances. Noradrenaline at 4 X 10(-4)M and serotonin at 3.3 X 10(-4)M were effective in elevating cAMP, but dopamine at 2 X 20(-4)M was ineffective. The beta adrenergic blocking agent, propranolol, effectively antagonized the cAMP response to noradrenaline, but the alpha adrenergic blocking agent, phentolamine, did not. The serotonin antagonist, methysergide, remarkably antagonized the cAMP response to serotonin, but the alpha and beta adrenergic agents did not.

Animals↗
PubMed2006

Coordination and modulation of locomotion pattern generators in Drosophila larvae: effects of altered biogenic amine levels by the tyramine beta hydroxlyase mutation.

Forward locomotion of Drosophila melanogaster larvae is composed of rhythmic waves of contractions that are thought to be produced by segmentally organized central pattern generators. We present a systematic description of spike activity patterns during locomotive contraction waves in semi-intact wild-type and mutant larval preparations. We have shown previously that Tbetah(nM18) mutants, with altered levels of octopamine and tyramine, have a locomotion deficit. By recording en passant from the segmental nerves, we investigated the coordination of the neuronal activity driving contraction waves of the abdominal body-wall muscles. Rhythmic bursts of activity that occurred concurrently with locomotive waves were frequently observed in wild-type larvae but were rarely seen in Tbetah(nM18) mutants. These centrally generated patterned activities were eliminated in the distal stumps of both wild-type and Tbetah(nM18) larvae after severing the segmental nerve from the CNS. Patterned activities persisted in the proximal stumps deprived of sensory feedback from the periphery. Simultaneous recordings demonstrated a delay in the bursting activity between different segments, with greater delay for segments that were farther apart. In contrast, bilateral recordings within a single segment revealed a well synchronized activity pattern in nerves innervating each hemisegment in both wild-type and Tbetah(nM18) larvae. Significantly, rhythmic patterns of bursts and waves could be evoked in Tbetah(nM18) mutants by head or tail stimulation despite their highly irregular spontaneous activities. These observations suggest a role of the biogenic amines in the initiation and modulation of motor pattern generation. The technique presented here can be readily extended to examine the locomotion motor program of other mutants.

Abdominal Wall↗
PubMed1983

Immediate increase of thyroid hormone release during acute stress in rats: effect of biogenic amines rather than that of TSH?

An increase of thyroxine (T4; 36% in average) and 3,5,3'-triiodothyronine (T3; 9% in average) levels in plasma was found in rats after 2 min of immobilization stress (IMO), while later (from 5 to 240 min of IMO) the level of both hormones decreased sharply. This increase was prevented by ip injection of phenoxybenzamine (4 or 16 mg kg-1), prazosin (2.5 mg kg-1), yohimbin (4 or 16 mg kg-1) and fluoxetine (10 mg kg-1) at 60 min before IMO, but similar injections of phentolamine (4 or 16 mg kg-1), tolazoline (4 or 16 mg kg-1), methysergide (10 mg kg-1), cyproheptadine (10 mg kg-1) as well as of lower doses of prazosin (0.6 or 1.2 mg kg-1) did not show such an effect. The level of TSH was increased after 2 min IMO too, but this was considered to be a separate phenomenon from the increase of T4 and T3, since in several groups injected with some of the above drugs the level of TSH was decreased together with increased levels of T4 and T3. It is suggested that the acute release of thyroid hormone might be due to the effect of biogenic amines which may be blocked by some alpha-adrenergic blocking agents. Since neither adrenalectomy nor adrenal-medullectomy prevented such a release, it may be concluded that circulating catecholamines of adrenal origin did not play any role in this process.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenalectomy↗
PubMed1992

Biogenic amines and thyrotoxicosis.

Circulating levels of T3, T4, gamma-amino-butyric acid, glutamate, 5-hydroxytryptamine, histamine, monoamine oxidase and histaminase were studied in 45 (25M, 20F) hyperthyroid patients and 46 (25M, 21F) normal healthy volunteers. Increased levels of blood 5-hydroxytryptamine, histamine and glutamic acid were observed along with elevated T3 and T4, whereas plasma gamma-aminobutyric acid, monoamine oxidase and histaminase activities were found to be low in both male and female patients. After three months of treatment, circulating levels of 5-hydroxytryptamine, histamine and glutamic acid decreased significantly along with normalization of thyroid hormones and with an increase in the concentrations of gamma-aminobutyric acid, monoamine oxidase and histaminase. There was a positive correlation between these amines and thyroid hormone levels. The findings thus suggest that alterations in the metabolism of biogenic amines may be related to an altered metabolism in thyrotoxicosis, and these parameters may prove to be useful markers for diagnosis and follow-up of these patients.

Adult↗
PubMed1989

Intracellular metabolism of biogenic amines in paraneurons.

Serotonin is one of the representative biogenic amines produced from tryptophan in the gastrointestinal tract as well as in the brain. The pineal gland also synthesizes serotonin, but as an intermediate in the biosynthesis of melatonin. The first enzymic step in the biosynthesis of serotonin is the hydroxylation of L-tryptophan catalyzed by tryptophan 5-monooxygenase. The 5-hydroxy-L-tryptophan (L-5HTP) formed is then decarboxylated to serotonin. Since the second step is catalyzed by non-specific aromatic L-amino acid decarboxylase, whether or not a given cell has the capacity to synthesize serotonin depends on the existence of tryptophan monooxygenase, and regulation of the serotonin biosynthesis is achieved mainly by modulating the activity of the first step enzyme. The activity of tryptophan monooxygenase was detected in extracts of the mouse stomach and intestines, although this activity was as low as approximately 1/20 of that in similar extract of the mouse brainstem. The upper small intestine and colon had a higher level of activity than other parts, and in the upper small intestine the enzyme was found to reside primarily in enterochromaffin cells of the mucosa. The intestinal tryptophan monooxygenase shared a common antigenic character with the enzyme from murine mastocytoma and was immunologically different from the brain enzyme. The enzymic properties were also similar to those of mastocytoma tryptophan monooxygenase which requires loosely-bound functional iron (Fe2+) for the activity. It seemed likely that the activity of tryptophan monooxygenase in paraneurons such as mastocytoma and enterochromaffin cells depends on available ferrous iron, and is therefore regulated, at least in part, by the cytosolic level of chelatable iron.

Animals↗
PubMed1995

Biogenic amines in the hypothalamus of rats after diethyldithiocarbamate or AIMAX treatment, an alternative for norepinephrine depletion.

The objective of this study was to determine whether AIMAX (a dithiocarbamoylhydrazine derivative) is suitable for determining the effects of norepinephrine (NE) depletion on reproduction in domestic animals. Therefore, the effect of AIMAX (n = 6) on concentrations of biogenic amines in the medial basal hypothalamus (MBH) and anterior hypothalamic area (AHA) of ovariectomized (OVX) rats primed with ovarian steroids was compared to that of diethyldithiocarbamate (DDC; n = 5), a potent dopamine-beta-hydroxylase (DBH) inhibitor, which is chemically similar to AIMAX. Rats that received only ovarian steroids and saline injections served as controls (n = 6). Treatment with DDC resulted in sedation and reduced body temperature. In contrast, rats behaved normally after AIMAX treatment. AI-MAX reduced (P < .05) NE but increased (P < .05) dopamine (DA) concentrations in MBH and AHA compared with controls. Similar changes in NE and DA concentrations were observed in DDC-treated rats. However, elevated epinephrine (EPI) levels were measured in MBH and AHA of only DDC-treated rats. Serum LH concentrations were suppressed (P < .005) in both AIMAX- and DDC-treated rats compared with control animals. Because AIMAX, like DDC, suppressed hypothalamic NE content and LH secretion, AIMAX should be useful in studying effects of NE depletion on gonadotropin secretion in domestic animals.

Animals↗
PubMed2000

Inhibition of cytochrome P450c11 by biogenic amines and an aziridine precursor, 2-(4-acetoxyphenyl)-2-chloro-N-methyl-ethylammonium chloride.

The interaction of several biogenic amines and Compound A (2-(4-acetoxyphenyl)-2-chloro- N-methyl-ethylammonium chloride), an analogue of the active substance in a HPLC fraction isolated from the shrub, Salsola tuberculatiformis Botsch., with cytochrome P450c11 was investigated. Noradrenaline, octopamine and Compound A inhibited the type I DOC induced difference spectrum of P450c11 and elicited a type II difference spectrum when added alone. The Ks-values for noradrenaline, octopamine, and Compound A were 0.8 mM, 0.16 mM and 0.36 mM, respectively. Dopamine, adrenaline and synephrine did not interact with, or inhibit, P450c11. Further investigation of Compound A indicated that it is a mixed inhibitor of sheep P450c11 with a stronger competitive (Kic = 106-110 microM) than uncompetitive (Kiu = 667-737 microM) element, and that it inhibits the conversion of deoxycorticosterone to corticosterone by human 11beta-hydroxylase and aldosterone synthase with EC50 values of 97 microM and 190 microM, respectively, in fetal calf serum.

Acetates↗
PubMed1985

Inhibition of dihydropteridine reductase in rat striatal synaptosomes and from human liver by metabolites of biogenic amines.

Catecholamines are potent noncompetitive inhibitors of dihydropteridine reductase in rat striatal synaptosomal preparations or purified from human liver. Their metabolites, except homovanillic acid, also inhibit the enzyme from both sources. The inhibitory potency of these compounds depends on the presence of the catechol or the 4-hydroxyphenyl structure, but may be modified by the 2-carbon side chain and its substituents. Indoleamines which have a hydroxylated aromatic nucleus (5-hydroxytryptamine and 5,6-dihydroxytryptamine) are equally inhibitory to the enzyme. These results suggest that biogenic amines themselves rather than their metabolites may serve as physiological inhibitors of dihydropteridine reductase in rat brain.

Animals↗
PubMed1985

Somatostatin mediates the effect of growth hormone surges on splanchnic biogenic amines.

Experiments were conducted in trained, conscious dogs fitted with an indwelling portal catheter. Radioenzymatic methods were employed for the quantitative measurement of plasma-free serotonin and catecholamines. An injection of ovine growth hormone (GH, 100 micrograms/kg) or an equimolar amount of somatostatin (somatotropin release inhibitory factor, SRIF, 7.5 micrograms/kg) into a saphenous vein led, within the first 15 min, to a transient but significant increase in plasma serotonin and a decrease in the concentrations of dopamine, norepinephrine, and epinephrine. The changes were frequently in excess of 40% of baseline values, and were found only in the portal and not in the peripheral circulation. When the animals were pretreated with an antiserum specifically directed against SRIF, GH surges no longer caused alterations in the portal levels of biogenic amines. Thus, the effects of spike concentrations of GH on plasma serotonin and catecholamines are apparently mediated by SRIF, a novel and unexpected function for a hormone that is known as an inhibitor of GH secretion.

Animals↗
PubMed1991

Hypothalamic biogenic amine levels in broiler chicks showing advanced sexual maturation.

Parasagittal knife cuts through the lateral hypothalamic area of 2-wk-old male broiler chicks induced precocious testes development. Two experiments were performed to determine whether hypothalamic biogenic amine levels in these chicks were changed by lateral hypothalamic deafferentation. In Experiment 1, chicks responding to surgery with advanced sexual maturation had reduced levels of norepinephrine (NE), epinephrine (E), and homovanillic acid (HVA) in the anterior hypothalamus and elevated levels of dopamine (DA) and serotonin in the median eminence, compared with controls. In Experiment 2, NE and HVA were reduced in the anterior hypothalamus of nonresponders. Dopamine was reduced in the anterior hypothalamus of nonresponders and elevated in the median eminence of responders. Serotonin was found to be higher in the median eminence of nonresponders. The increased DA in the median eminence suggests an excitatory role for this neurotransmitter in gonadotropin release at puberty.

Animals↗
PubMed1999

Biogenic amines and sensory changes associated with the microbial flora of Mediterranean gilt-head sea bream (Sparus aurata) stored aerobically at 0, 8, and 15 degrees C.

Changes in the concentrations of tyramine, agmatine, putrescine, cadaverine, spermidine, tryptamine, spermine, histamine, and trimethylamine were studied in parallel with the development of the microbial population during the storage of Mediterranean gilt-head sea bream (Sparus aurata) at three temperatures (0, 8, 15 degrees C). Changes in sensory scores were also recorded. Pseudomonads and H2S-producing bacteria were the dominant microorganisms. Enterobacteriaceae and lactic acid bacteria were also present in the fish microflora. Among the biogenic amines, putrescine and cadaverine were detected when pseudomonads exceeded 10(6) to 10(7) CFU/g. Histamine was produced only in samples stored at 15 degrees C. Tyramine, tryptamine, agmatine, and trimethylamine were absent regardless of the storage temperature.

Aerobiosis↗
PubMed1999

Biogenic amine survey and organoleptic changes in fresh, stored, and temperature-abused bluefish (Pomatomus saltatrix).

Changes in histamine, putrescine, and cadaverine concentrations in bluefish filets (Pomatomus saltatrix) stored at 5, 10, and 15 degrees C were determined using high-performance liquid chromatography. An organoleptic assessment was conducted simultaneously with the biogenic amine analyses. The histamine levels found in fresh bluefish obtained from wholesale seafood distributors ranged between <1 ppm and 99 with an average of 39 ppm. Putrescine and cadaverine were not found in fresh bluefish. Fish fillets stored at each of the three temperatures developed histamine. The greatest accumulation of histamine was observed in fish stored at 15 degrees C, which developed histamine levels as high as 2,200 ppm. Putrescine levels increased at each temperature during storage. Cadaverine was present only in uninoculated bluefish stored at 15 degrees C. Histamine achieved higher levels in bluefish pieces inoculated with Morganella morganii, which demonstrates that bluefish support bacterial histamine formation. Histamine levels at each temperature exceeded the 50-ppm advisory level established by the Food and Drug Administration before 100% sensory rejection. Standard plate counts increased during storage of fish at all temperatures, but the correlation between histamine levels and standard plate count was not significant.

Animals↗
PubMed2000

Formation of biogenic amines in raw milk Hispánico cheese manufactured with proteinases and different levels of starter culture.

Two proteinases, a neutral proteinase from Bacillus subtilis and a cysteine proteinase from Micrococcus sp., were used to accelerate the ripening process of raw cow's milk Hispánico cheese, a semihard variety. Two levels (0.1% and 1%) of a commercial starter culture containing Lactococcus lactis subsp. lactis and L. lactis subsp. cremoris were added for cheese manufacture. The influence of both factors, proteinase addition and level of starter culture, on the growth of amino acid-decarboxylating microorganisms and on the formation of biogenic amines during cheese ripening was investigated in duplicate experiments. The population of tyrosine decarboxylase-positive bacteria, which represented less than 1% of the total bacterial population in most cheese samples, and tyrosine decarboxylase-positive lactobacilli was not influenced by proteinase addition or level of starter culture. Tyramine was detected in all batches of cheese from day 30. Its concentration was significantly (P < 0.05) influenced by proteinase addition but not by the level of starter culture and increased with cheese age. After 90 days of ripening, 103 to 191 mg/kg of tyramine was found in the different cheese batches. Histamine was not detected until day 60 in cheese with neutral proteinase and 1% starter culture and until day 90 in the rest of the cheeses. The concentration of this amine did not exceed 20 mg/kg in any of the batches investigated. Phenylethylamine and tryptamine were not found in any of the samples.

Animals↗