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PubMed1976

Studies on the biochemical aspects of the 'disulfiram-like' reaction induced by oral hypoglycemics.

In vitro experiments, using rat liver homogenates, were designed to examine certain of the proposed enzymatic mechanisms for the interaction of oral hypoglycemic drugs with monoamine and ethanol metabolism. The oxidative degradation of tryptamine was studied by measuring indoleacetic acid (IAA) production and conclusions were drawn with regard to the activity of monoamine oxidase, aldehyde dehydrogenase and ethanol dehydrogenase. Acetohexamide, hydroxyhexamide, tolazamide, tolbutamide and chlorpropamide failed to reveal any specific inhibition of the three enzymes. Ethanol (0.2% w/v) and disulfiram decreased IAA formation, as did a lack of available aldehyde dehydrogenase and NAD, but these reductions were not enhanced by the hypoglycemic agents. The results suggest that the 'disulfiram-like' reaction which occurs in certain patients imbibing ethanol while receiving oral hypoglycemic drugs, depends upon some factor(s) other than, or additional to, a specific interference with monoamine and/or ethanol metabolism.

Administration, Oral↗
PubMed1982

Fluvoxamine, a new antidepressant drug, fails to show antiserotonin activity.

Fluvoxamine, (E)-5-methoxy-4'-(trifluoromethyl)valerophenone O-2(2-aminoethyl)oxime, a new antidepressant drug inhibiting serotonin (5-HT) uptake, was studied in rats and mice in order to check whether it has any central anti-5-HT activity, as do some tricyclic antidepressants, e.g. amitriptyline and doxepin. Fluvoxamine did not influence either the 5-hydroxytryptophan-induced head twitch response in mice or the tryptamine convulsions in rats. In the hind limb flexor reflex of the spinal rat the stimulation induced by fenfluramine was inhibited, that induced by LSD was not changed. Fluvoxamine also antagonized the hyperthermia (at ambient temperature of 28 degrees C), induced in rats by fenfluramine or p-chloroamphetamine. The hyperthermia caused by m-chlorophenylpiperazine was not inhibited. Fluvoxamine did not antagonize the 5-HT pressor effect in pithed rats. It has no effect on the immobility time in the behavioural despair test in rats. The results indicate that fluvoxamine fails to show anti-5-HT activity.

5-Hydroxytryptophan↗
PubMed1989

Inhibition of noradrenaline release in the pig coronary artery via a novel serotonin receptor.

In pig coronary artery preincubated with [3H]noradrenaline, the effects of serotonin (5-HT) receptor agonists and antagonists on the electrically evoked (0.66 Hz) tritium overflow were determined. Tritium overflow was inhibited by 5-HT, 5-aminotryptamine, N,N-dimethyl-5-hydroxytryptamine, 5-hydroxytryptamine, 5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole (RU 24969) and tryptamine. The maximum inhibition obtainable with 5-HT was by about 35%, its pIC20 value was 7.85. 8-Hydroxy-di(n-propylamino)tetralin, urapidil, ipsapirone, 5-carboxamidotryptamine, 4-hydroxytryptamine, 5-methoxytryptamine and alpha-methyl-5-hydroxytryptamine did not decrease 3H overflow. The inhibitory effect of 5-HT was not antagonized by ketanserin, mesulergine, metitepine, propranolol, (3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester (ICS 205-930) and yohimbine. Additionally, it was not altered by indomethacin. We conclude from the present data that the sympathetic nerves of the pig coronary artery are endowed with inhibitory presynaptic 5-HT receptors which do not belong to the 5-HT1, 5-HT2 or 5-HT3 receptor type but seem to represent a so far unknown receptor class.

Animals↗
PubMed1988

Mechanisms of serum protein binding and cell anchorage to immobilized serotonin and indole analogs.

Bovine aortal endothelial cells, bovine smooth muscle cells, chick embryo fibroblasts, and baby hamster kidney cells all attached and grew on immobilized tryptamine or L-tryptophan as successfully as on immobilized serotonin. A detailed investigation employing different serum compositions combined with cell blotting and immunoblotting techniques revealed that adhesion of cells to each of the immobilized indole analogs was mediated by vitronectin and fibronectin. Quantitative analyses revealed major differences in the variety of serum proteins adsorbed to each of the immobilized indole analogs and in particular major differences in the amounts of adsorbed vitronectin. However, similar levels of adsorbed fibronectin and fibronectin fragments were found on each of the immobilized indole analogs. The results indicate that (i) different composites of surface-adsorbed proteins may be directed by chemical differences between the immobilized indole analogs and (ii) mammalian cells may still populate chemically different surfaces with equal success despite differences in the surface profiles of adsorbed serum proteins.

Animals↗
PubMed1995

NMR-titrations with complexes between ds-DNA and indole derivatives including tryptophane containing peptides.

It is shown that NMR titrations can be used on a quantitative basis to derive binding constants and binding modes of ds-DNA ligand complexes from several signals. The results are partially at variance with literature conclusions; they can be interpreted by additive and independent contributions of electrostatic interactions between DNA phosphate and ammonium centers in the side chain of the ligands, and of very weak stacking contributions of the indole rings. While gramine and tryptamine are found to intercalate, tryptophane-containing peptides do so only, if the tryptophane is flanked by at least two lysine units.

Alkaloids↗
PubMed1983

Enhanced serotonin-stimulated adenylate cyclase activity in membranes from adult guinea pig hippocampus.

We have developed an assay for serotonin (5-HT) stimulation of adenylate cyclase activity in membranes from adult guinea pig hippocampus. The response to 5-HT is concentration-dependent, with an EC50 of 0.01 microM, a shallow slope, and mean maximal stimulation of 90% over basal activity. The response to 5-HT is GTP-dependent and additive to the maximal stimulation by histamine. Micromolar concentrations of the known 5-HT receptor agonists, tryptamine and 5-methoxytryptamine, also stimulate cAMP production in this system, and their effect is not additive to that elicited by a maximal concentration of 5-HT. These results are consistent with the hypothesis that the response to 5-HT is elicited through a distinct receptor coupled to adenylate cyclase; the magnitude and the reproducibility of the 5-HT response in this system should make it useful for receptor classification. To examine the effect of prior exposure to endogenous 5-HT on the responsiveness of the system, we assayed 5-HT stimulation of enzyme activity in membranes prepared from animals 25-27 hrs after treatment with a single injection of reserpine (5 mg/kg, i.p.). The mean maximal stimulation of adenylate cyclase by 5-HT was increased to 150% over basal activity with no effect on the EC50 or slope of the 5-HT concentration-response curve. Reserpine pretreatment did not affect basal activity or histamine-stimulated adenylate cyclase activity. These results are discussed in the context of a hypothesis that endogenous 5-HT normally exerts a desensitizing effect on its receptors in situ.

5-Methoxytryptamine↗
PubMed1989

Release of some endogenous trace amines from rat striatal slices in the presence and absence of a monoamine oxidase inhibitor.

The basal and 50 mM K+-stimulated release of m-tyramine (mTA), p-tyramine (pTA), tryptamine (TR) and phenylethylamine (PE) from striatal slices obtained from rats pretreated with a monoamine oxidase inhibitor (MAOI) was investigated. A K+-stimulated release of mTA and pTA was observed, but K+ did not stimulate either TR or PE release. The latter two amines, therefore, are unlikely to be conventional neurotransmitters in the rat striatum. The release of endogenous striatal pTA from control rats was also investigated. Veratridine stimulated endogenous pTA release, but 50 mM K+ did not. It is possible, therefore, that endogenous pTA can be released in a transmitter-like fashion.

Animals↗
PubMed1992

Peripheral 5-carboxamidotryptamine induces hindlimb scratching by stimulating 5-HT1A receptors in rats.

Treatment of rats with 5-carboxamidotryptamine (5-CT) or 5-methoxy-tryptamine (5-MeOT) induces a hindlimb scratch response. These compounds have high affinity for 5-HT1A and 5-HT1D receptors. The selective 5-HT1A receptor agonist N,N-dipropyl-5-CT (DP-5-CT) also induced hindlimb scratching while the selective 5-HT1D receptor agonist, sumatriptan, did not. 5-CT-induced hindlimb scratching was inhibited dose-dependently by several 5-HT1A antagonists (BMY 7378, NAN-190, MDL 73005EF and pindobind-5-HT1A) as well as the non-selective 5-HT antagonist, methiothepin. Pretreatment of rats with the serotonin (5-HT) synthesis inhibitor, p-chlorophenylalanine (PCPA) or the 5-HT depleting agent, reserpine, markedly attenuated 5-CT-induced hindlimb scratching. These data suggest that hindlimb scratching induced by 5-HT agonists may not be centrally mediated but rather may be mediated by a neuronal 5-HT1A receptor localized outside the blood-brain barrier.

5-Methoxytryptamine↗
PubMed1986

Metabolic conversion of IQ and MeIQ to bacterial mutagens.

The metabolic conversion of 2-amino-3-methyl- and 2-amino-3,4-dimethyl-imidazo[4,5-f]quinoline (IQ and MeIQ respectively) to bacterial mutagens was studied using a bacterial mutation assay. Studies were performed using S9 fractions derived from either corn oil (uninduced) or Aroclor-1254-treated Sprague-Dawley rats. Aroclor 1254 treatment lowered the S9 protein concentration required for optimum levels of mutagenesis, enhanced the numbers of mutants observed and altered the effects of metabolic inhibitors and cofactors added to the assay. Studies with uninduced preparations revealed that IQ and MeIQ exhibited similar responses to the effects of metabolic inhibitors and cofactors involved in detoxication reactions. Both IQ and MeIQ activation appeared to be inhibited by the biogenic amines tryptamine and tyramine and inactivated by conjugation with either acetyl coenzyme A or glutathione.

Acetyl Coenzyme A↗
PubMed1982

Further studies on the role of indoleamines in the responses of cortical neurones to stimulation of nucleus raphe medianus: effects of indoleamine precursor loading.

Responses of cortical neurones to stimulation of nucleus raphe medianus (RM) were determined before and after parenteral administration of l-tryptophan or l-5-hydroxytryptophan (5HTP). The short latency inhibitory effects of stimulation and the longer latency excitation were enhanced by l-tryptophan. 5-Hydroxytryptophan, on the other hand, enhanced the excitatory effects but had no effects on the initial inhibition. Both precursors were able to induce a third type of response, a long-latency inhibition which succeeded the excitation. Inhibition of tryptophan hydroxylase abolished the facilitatory effects of tryptophan on the excitatory and long-latency inhibitory effects of stimulation of the raphé medianus but the enhancement of the short-latency inhibition remained intact. Inhibition of tryptophan hydroxylase failed to alter any of the effects of 5HTP on evoked responses to stimulation of the raphé medianus. Finally, inhibition of aromatic amino acid decarboxylase abolished the effects of both indoleamine precursors on all response phases. The results are consistent with a previous suggestion that the short-latency inhibition may be tryptamine-mediated while the other response phases are mediated by 5-hydroxytryptamine.

5-Hydroxytryptophan↗
PubMed1983

5-hydroxytryptamine: its facilitative action on [3H]dopamine release from the retina.

5-Hydroxytryptamine (5-HT) at 5 X 10(-4) M caused a two-fold increase in [3H]dopamine (DA) release from retinal particulate fractions of the carp (Cyprinus carpio). The 5-HT action was dose- and Ca2+-dependent. The three 5-HT agonists examined (5-methoxytryptamine, 5-methoxy-N,N-dimethyltryptamine and tryptamine) were more effective than 5-HT on [3H]DA release. 5,6-Dihydroxytryptamine was the strongest competitor among drugs tested for [3H ]DA uptake, but did not evoke any significant release of [3H]DA. Noradrenaline (or DA) at 5 X 10(-4) M produced a large increase in [3H]DA release from the particulate fractions, but its action was Ca2+-independent. The 5-HT-induced DA release could be seen in the frog retina but not in the rat retina, which does not contain indoleamine-accumulating cells. The results obtained strongly suggest that 5-HT stimulates [3H ]DA release through a receptor mechanism on DAergic terminals and modifies the DA-cell's function in the retina.

Animals↗
PubMedDate not supplied

Thyroxine and propylthiouracil-induced changes in the activity of monoamine oxidase in the fetal rat.

The activity of monoamine oxidase (MAO) towards tryptamine has been determined in heart, brain and liver of the 21.5 day old rat fetus. The activity was compared between normal, thyroxine and propylthiouracil (PTU) treated animals. Hypothyroidism induced by PTU leads to a decrease in the activity of the three organs, while hyperthyroidism causes an increase in the enzymatic activity. These differences seem to be rather independent of the protein content of the organs. It appears thar rat fetal MAO is under a strong thyroid control.

Animals↗
PubMed1984

Ontogeny of N,N-dimethyltryptamine and related indolealkylamine levels in neonatal rats.

The present study deals with the measurement of the brain levels of the two potent hallucinogens N,N-dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (OMB), the biogenic amine tryptamine (TA), and its condensation product 1,2,3,4-tetrahydro-beta-carboline (THBC) in rats of various ages. Using gas chromatography-mass spectrometry with isotope dilution, we detected DMT, OMB, and THBC in neonatal rats from birth. DMT levels remained low until days 12 and 17 at which time they increased significantly and then returned to the initial low levels for all subsequent ages. The levels of OMB were higher than those measured for DMT with the highest levels being observed at days 12 and 17, and also on day 31. However, the levels for OMB showed much more variation. Although elevated levels of DMT and OMB have been correlated with stress, there are no known functions for these compounds. TA levels remained below detection limits until day 19. THBC levels were observed to be highest on days 22 and 31. The role that THBC plays in mammalian tissues is not known.

Aging↗
PubMed1986

Studies of the relationship between molecular structure and hallucinogenic activity.

The nature of the stereochemistry and aromatic ring substituents and their importance to biological activity for phenethylamine-type hallucinogens is presented. The possibility of a hydrophobic site to bind to the 4-substituent and its likely geometry is described. A brief discussion of the structure-activity relationships for tryptamines such as psilocin and DMT is also given, with comments about the stereochemistry of alpha-methyltryptamines. Evaluation of a series of N(6)-alkyl-nor-LSD derivatives indicated that selected members such as N(6)-ethyl, allyl and propyl were as potent as, if not more potent than LSD, both in a two-lever drug discrimination assay in rats, and in man. N(6)-alkyl groups longer than n-propyl, such as n-butyl or 2-phenethyl, gave compounds that were greatly reduced in activity.

Animals↗
PubMed1980

Changes in body temperature after administration of adrenergic and serotonergic agents and related drugs including antidepressants.

This survey, the third in a series, presents extensive tabulations of literature, primarily since 1965, on thermoregulatory effects of adrenergic and serotonergic agonists and their antagonists including ergot alkaloids, amphetamines, tryptamines, monoamine oxidase inhibitors, tricyclic and other antidepressants, a variety of other agents which alter presynaptic aminergic mechanisms including reserpine, 6-hydroxydopamine, p-chlorophenylalanine, alpha-methyltyrosines, cocaine, guanethidine and bretylium. The information listed includes the species used, route of administration and dose of drug, the environmental temperature at which the experiments were performed, the number of tests, the direction and magnitude of body temperature change and remarks on the presence of special conditions, such as age or lesions, or on the influence of other drugs, such as antagonists, on the response to the primary drug.

Amphetamine↗
PubMed1982

Indolealkylamine and phenalkylamine hallucinogens: a brief overview.

Various indolealkylamine and phenalkylamine derivatives are hallucinogenic in man and/or are behaviorally active in animals. This overview is divided into two parts. The first part attempts to bring together information concerning the activity of indolealkylamines (i.e., tryptamines, alpha-methyltryptamines, N,N-dimethyltryptamines, N-alkyltryptamines, lysergic acid derivatives and beta-carbolines) and phenalkylamines (i.e., phenethylamines, phenylisopropylamines) along with major key references, and with emphasis on those agents not recently reviewed. The latter portion of this overview describes some of the work being conducted in our laboratories in an effort to elucidate the role of the neurotransmitter serotonin in the mechanism of action of various indolealkylamine and phenalkylamine hallucinogens.

Amines↗
PubMed1983

Trace acid levels in the plasma and MAO activity in the platelets of violent offenders.

The plasma concentrations of the unconjugated and conjugated so-called "trace acids," phenylacetic acid (PAA), m- and p-hydroxyphenylacetic acid (mHPA, pHPA), and platelet monoamine oxidase (MAO) activity were measured in 103 male prisoners detained in a psychiatric institution. Twenty-three had been convicted of violent crimes, 18 of sexual offenses, 24 of armed robbery, 27 of nonviolent property offenses, and 11 of miscellaneous nonviolent offenses. Unconjugated pHPA and conjugated PAA were found to be significantly reduced in the violent offenders when compared with those of the "nonviolent" groups. The levels of pHPA were also found to be low in sexual offenders. Platelet MAO activities to phenylethylamine, tryptamine, and p-tyramine between any of the categories of prisoners were not significantly different.

Adolescent↗
PubMed1985

Pentametric distribution of platelet monoamine oxidase activity.

The distribution of catalytic activity of platelet monoamine oxidase (MAO) with both tryptamine and phenylethylamine as substrates was examined in 1,129 Swedish men at age 18 years. A mixture of five components was needed to describe the distribution, even when the original scale was transformed to remove skewness. The proportions of admixture were 2% for the extremely low component with a mean of -2.3 sigma, 29% for moderately low MAO (mean -0.8 sigma), 51% for intermediate MAO (mean 0.0 sigma), 15% for moderately high MAO (mean + 1.3 sigma), and 3% for extremely high MAO (mean + 3.0 sigma). Thus, the upper and lower deciles each contain contributions from two extreme components that differ from a much larger intermediate component with activity near the mean of the general population. This is compatible with a minimum of three alleles at a single major locus or with at least two polymorphic loci. The hypothesis that MAO activity is controlled by two alleles at a single locus was tested and rejected. The demonstration of at least five distinct components to the distribution of MAO warrants further research to characterize the biochemical structure and function of MAO enzyme variants as well as study of the behavioral correlates of the components.

Adolescent↗