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European Journal of Pharmacology

ISSN 1879-0712, 0014-2999

180 papers in the library · 3,125 citations · publishing 1977-2026

Papers

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Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2 binding affinity

European Journal of Pharmacology December 1, 1986 Kurt Rasmussen, Richard A Glennon, George K. Aghajanian 50 citations

The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2 binding affinity [-) DOB greater than DOM greater than ( + )DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into...

DOI: 10.1016/0014-2999(86)90014-2 (opens in new tab) Serotonin Phenethylamine Hallucinogen Locus coeruleus +8

The effects of 3,4-methylenedioxymethamphetamine (MDMA) and 3,4-methylenedioxyamphetamine (MDA) on monoaminergic systems in the rat brain.

European Journal of Pharmacology August 22, 1986 D M Stone, D C Stahl, Glen R. Hanson et al.

The effects of two amphetamine-like designer drugs, 3,4-methylenedioxyamphetamine (MDA) and 3,4-methylenedioxymethamphetamine (MDMA), on dopaminergic and serotonergic systems in the rat brain were investigated and compared to those of methamphetamine (METH). Like METH, single or multiple 10 mg/kg doses of either drug caused marked reductions in both tryptophan hydroxylase (TPH) activity and...

Cannabidiol attenuates delta 9-tetrahydrocannabinol-like discriminative stimulus effects of cannabinol.

European Journal of Pharmacology June 17, 1986 A J Hiltunen, Torbjörn U C Järbe

Interaction effects of cannabidiol (CBD) and cannabinol (CBN) were examined using a drug discrimination procedure in which rats had been trained to discriminate between 3 mg/kg of delta 9-tetrahydrocannabinol (delta 9-THC) and vehicle (2 ml/kg). The generalization effects of CBN to delta 9-THC were attenuated when CBN was administered together with CBD. The results were time- and dose-dependent.

Direct comparison of hallucinogenic phenethylamines and D-amphetamine on dorsal raphe neurons.

European Journal of Pharmacology April 1, 1986

We compared the effects of the hallucinogens 2,5-dimethoxy-4-methylamphetamine (DOM), mescaline and the simulant D-amphetamine, applied by microiontophoresis to rat dorsal raphe (DR) units. DR neuron firing rate was relatively insensitive to DOM and unaffected by mescaline, but was clearly inhibited by D-amphetamine. Intravenous DOM usually inhibited, but this effect was correlated with blood...

Subtypes of the 5-HT receptor mediating the behavioural responses to 5-methoxy-N,N-dimethyltryptamine in the rat

European Journal of Pharmacology October 1, 1985 Mark D. Tricklebank, Christian Forler, Derek N. Middlemiss et al. 141 citations

The 5-HT receptor subtypes involved in the mediation of reciprocal forepaw treading and the flat body posture induced by the central 5-HT receptor agonist, 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), were examined in intact rats and in rats depleted of monoamines with reserpine. Forepaw treading in non-reserpinised rats was antagonised by the 5-HT2 receptor antagonist, ketanserin, only at...

Development of tolerance to repeated administration of 5-methoxy-N,N-dimethyltryptamine in rats.

European Journal of Pharmacology January 15, 1985 Michael E. Trulson, G F Keltch 18 citations

Chronic administration of 5-methoxy-N,N-dimethyltryptamine (5-MeODMT, 2 mg/kg i.p., every 30 min for 4 h) produced a dramatic tolerance to the behavioral effects of the drug in rats. The ED50 for the syndrome-inducing effects of the drug was increased from 1.3 to 2.4 mg/kg, and the mean duration of the syndrome was decreased from 14.9 to 1.2 min after this treatment. This tolerance effect...

Nitrous oxide generalizes to a discriminative stimulus produced by ethylketocyclazocine but not morphine.

European Journal of Pharmacology October 1, 1984 M D Hynes, D L Hymson

The discriminative stimulus properties of nitrous oxide, an analgesic and anesthetic gas, were evaluated in rats trained to discriminate the effects of morphine or ethylketocyclazocine. Administration of nitrous oxide in concentrations as high as 80 percent did not produce generalization to the discriminative cue produced by morphine. Nitrous oxide did, however, generalize in a...

Increased behavioural response to 5-methoxy-N,N-dimethyltryptamine but not to RU-24969 after intraventricular 5,7-dihydroxytryptamine administration.

European Journal of Pharmacology September 3, 1984 A P Nisbet, C A Marsden 29 citations

Chemical lesioning of the 5-hydroxytryptamine neurones in the brain with 5,7-dihydroxytryptamine (200 micrograms i.c.v., 14 or 21 days previously) resulted in an enhanced behavioral response following administration of the 5-hydroxytryptamine receptor agonist 5-methoxy-N,N-dimethyltryptamine (2.5 mg/kg). The increase in the behavioural response showed a positive correlation with the decrease in...

Long-lasting behavioral effects of bromocriptine in cats.

European Journal of Pharmacology July 1, 1984 F Gonzalez-Lima, W L Stiehl, R Medina

The objective was to determine the behavioral effects and duration of action of bromocriptine (BC) doses from 6 to 60 mg/kg i.p. Cats were housed in large outdoors cages designed for prolonged observation using an ethological approach. Baseline behavior was measured after a 3 month period of habituation. The frequency of 12 behaviors was then scored continuously over 12 h following BC...

5-HT1 and 5-HT2 binding properties of derivatives of the hallucinogen 1-(2,5-dimethoxyphenyl)-2-aminopropane (2,5-DMA).

European Journal of Pharmacology June 15, 1984 M Shannon, G Battaglia, Richard A Glennon et al.

The affinities of a series of 1-(2,5-dimethoxyphenyl)-2-aminopropane (2,5-DMA) derivatives, most of which are hallucinogenic in man, and several related agents were determined for rat cortical serotonin (5-HT) binding sites. Competition assays were performed in which these agents were competed for the 5-HT2 binding of [3H]ketanserin, or the 5-HT1 binding of [3H]LSD (in the presence of...

Some behavioral effects of hallucinogens are mediated by a postsynaptic serotonergic action: evidence from single unit studies in freely moving cats.

European Journal of Pharmacology May 18, 1984 J Heym, K Rasmussen, B L Jacobs

Although central serotonergic systems appear to be linked importantly to the mechanism of action of a variety of hallucinogenic drugs, the nature of this interaction has remained unclear. In the present study, the question of whether the critical link is presynaptic or postsynaptic was examined in cats. Behaviorally inactive doses (1.0 mg/kg) of the serotonin receptor antagonists mianserin,...

Characterisation of [3H]lysergic acid diethylamide binding to a 5-hydroxytryptamine receptor on human platelet membranes

European Journal of Pharmacology 1984 David P. Geaney, Michael Schächter, Jonathan Elliot et al. 90 citations

Specific binding of [3H]lysergic acid diethylamide (LSD) to human platelet membranes, as defined by 300 nM spiperone, was saturable over the concentration range of 0.25-2.5 nM [3H]LSD. At 0.5 nM [3H]LSD the half-time for association at 37 degrees C was 56 min, half-time for dissociation was 173 min, and the kinetically derived affinity was 0.24 nM. In 19 control subjects equilibrium binding...

Mescaline elicits behavioral effects in cats by an action at both serotonin and dopamine receptors

European Journal of Pharmacology December 1, 1983 Michael E. Trulson, Terriann Crisp, Leslie J. Henderson 21 citations

The characteristic behavioral effects of mescaline in cats were nearly completely blocked by pretreatment with low doses of either a specific serotonin antagonist (methysergide) or a dopamine specific antagonist (haloperidol). These blocking effects were not due to non-specific actions, since methysergide did not block the behavioral effects of apomorphine, and haloperidol did not block the...

DOI: 10.1016/0014-2999(83)90544-7 (opens in new tab) Mescaline Methysergide Haloperidol Apomorphine +6

Hyponeophagia in the Roman rat strains: effects of 5-methoxy-N,N-dimethyltryptamine, diazepam, methysergide and the stereoisomers of propranolol.

European Journal of Pharmacology November 25, 1983 R A Shephard, P L Broadhurst 20 citations

The effects of 5-MeODMT (2.5 mg/kg), diazepam (1 mg/kg), methysergide and the stereoisomers of propranolol (6 mg/kg) on hyponeophagia were studied in both sexes of the Roman strains of rats, selectively bred for acquisition of a two-way conditioned avoidance response. Diazepam, methysergide and 1-propranolol increased feeding in a novel environment whilst 5-MeODMT decreased it and d-propranolol...

Influence of psychotomimetics and lisuride on synaptosomal dopamine release in the nucleus accumbens of rats.

European Journal of Pharmacology September 1, 1983

In superfusion experiments with a crude synaptosomal fraction from the nucleus accumbens of rats, lysergic acid diethylamide, mescaline and N,N-dimethyltryptamine (representing different chemical classes of psychotomimetics) produced a concentration-related inhibition of K+-evoked [3H]dopamine release whereas spontaneous release remained unchanged. The nonpsychotomimetic ergoline lisuride...

Antagonism of the effects of the hallucinogen DOM and the purported 5-HT agonist quipazine by 5-HT2 antagonists.

European Journal of Pharmacology July 1, 1983

Rats trained to discriminate 1.0 mg/kg of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline in a two-lever operant choice task were administered doses of mescaline, LSD, 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT), quipazine, TFMPP and RU-24969. The DOM-stimulus generalized to the three hallucinogenic agents and to quipazine, but not to the purported serotonin agonists TFMPP or...

Raphe neurons: firing rate correlates with size of drug response.

European Journal of Pharmacology June 3, 1983 Barry L. Jacobs, J Heym, K Rasmussen 25 citations

Significant negative correlations were obtained between the spontaneous discharge rate during waking and the neural response to systemic injections of either 5-MeODMT or LSD for serotonergic neurons in the dorsal raphe nucleus, nucleus centralis superior, and nucleus raphe pallidus of unanesthetized and unrestrained cats. These data are discussed in terms of an hypothesis which accounts for...

Inhibitory effect of 5-methoxy-N,N-dimethyltryptamine on the synaptosomal uptake of 5-hydroxytryptamine.

European Journal of Pharmacology June 3, 1983 O G Berge, D Chacho, K Hole 20 citations

5-Methoxy-N,N-dimethyltryptamine (5-MeODMT) in concentrations of 0.5-500 microM produced a significant inhibition of [14C]5-hydroxytryptamine [14C]5-HT) uptake in striatal, hippocampal and hypothalamic crude synaptosomes from rat brain. Higher concentrations of 5-MeODMT (10 microM) also inhibited the uptake of [3H]dopamine [3H]DA) and induced the release of [14C]5-HT and [3H]DA from preloaded...

DOM-stimulus generalization to LSD and other hallucinogenic indolealkylamines.

European Journal of Pharmacology January 21, 1983 Richard A Glennon, R Young, John M. Jacyno et al.

Stimulus generalization studies were conducted using rats trained to discriminate 1.0 mg/kg of the phenalkylamine hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline in a two-lever operant procedure. The results suggest that certain indolealkylamine hallucinogens, including LSD and several alpha-methyltryptamine, N,N-dialkyltryptamine and beta-carboline derivatives,...

Medullary serotonergic neurons are insensitive to 5-MeoDMT and LSD.

European Journal of Pharmacology July 30, 1982 J Heym, G F Steinfels, Barry L. Jacobs 21 citations

A comparison was made of the effects of 5-MeoDMT or LSD on serotonergic unit activity in the dorsal raphe nucleus (DRN) and nucleus raphe pallidus (NRP) of freely moving cats. NRP neurons were substantially less responsive than DRN neurons to both drugs. NRP neurons were unresponsive to behaviorally effective low doses of these drugs whereas the activity of DRN neurons was strongly depressed....

Intracellular studies on the effects of systemic administration of serotonin agonists on rat facial motoneurons.

European Journal of Pharmacology February 26, 1982 C P Vandermaelen, George K. Aghajanian 37 citations

Intracellular recordings were made from facial motoneurons of anesthetized rats during systemic administration of 5-methoxy-N,-N-dimethyltryptamine (5-MeODMT) and p-chloroamphetamine (PCA), drugs which elicit the behavioral serotonin syndrome. Both drugs caused a slow depolarization, increased input resistance, and increased excitability of facial motoneurons. These changes are identical to...

Behavioral properties of psychoactive phenylisopropylamines in rats.

European Journal of Pharmacology December 17, 1981 Richard A Glennon, John A. Rosecrans, R Young 21 citations

Rats were trained to discriminate injections of 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT, 3.0 mg/kg) a hallucinogenic agent for which a serotonergic mechanism has been implicated, from saline in a two-lever drug discrimination task. After reliable levels of accuracy (greater than or equal to 85%) were attained, the ability of the 5-OMe DMT cue to generalize to 36 substituted...

LSD, mescaline and serotonin injected into medial raphe nucleus potentiate apomorphine hypermotility

European Journal of Pharmacology November 1, 1981 Heidrun Fink, Wolfgang Oelssner 44 citations

Microinjections of LSD (0.05 microgram), mescaline (0.5 microgram) and serotonin (10 microgram) into the medial raphe nucleus of rats resulted in a strong potentiation of apomorphine (1 mg/kg i.p.)-induced hypermotility. The potentiating effect of LSD or serotonin was suppressed by simultaneous injections of methysergide (0.05 microgram) or cyproheptadine (0.05 microgram) into the medial raphe...

Repeated administration of 5-methoxy-N,N-dimethyltryptamine to male rats potentiates stimulation of prolactin secretion by serotonin agonists.

European Journal of Pharmacology October 15, 1979 Miljana Simonovic, Herbert Y. Meltzer 11 citations

Repeated administration of 5-methoxy-N,N-dimethyltryptamine (5MeODMT, 5 mg/kg, a serotonin agonist, every 3 h for a total of 4 injections) potentiated its prolactin (PRL)-releasing effect and that of two other serotonin agonists, quipazine and N,N-dimethyltryptamine. This pretreatment schedule had no effect on PRL response to anti-dopaminergic drugs. The onset of enhanced PRL response to...

In vivo evidence of partial agonist activity exerted by purported 5-hydroxytryptamine antagonists.

European Journal of Pharmacology October 15, 1979 Françis C. Colpaert, C J Niemegeers, P A Janssen

Using a food-reinforced two-lever operant method, rats (n = 9) were trained to discriminate 0.16 mg/kg LSD from saline. Tests for stimulus generalization in rats so trained indicated that the purported 5-HT antagonists cyproheptadine (1.25 and 10 mg/kg), methysergide (0.16 to 10 mg/kg) and mianserin (2.5 to 40 mg/kg) produced partial generalization with LSD. The hallucinogens mescaline (5 to 40...