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Neuropharmacology

ISSN 1873-7064

176 papers in the library · 4,449 citations · publishing 1982-2026

Papers

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Ibogaine block of the NMDA receptor: in vitro and in vivo studies.

Neuropharmacology April 1, 1996 K Chen, T G Kokate, S D Donevan et al. 55 citations

Ibogaine is an hallucinogenic indole alkaloid claimed to have anti-addictive properties. Although its mechanism of action is unknown, binding studies have indicated that the drug may interact with N-methyl-D-aspartate (NMDA) receptors. We further investigated the nature of the interaction between ibogaine and NMDA receptors in voltage clamp and binding studies, and sought to confirm that the...

Prior morphine exposure enhances ibogaine antagonism of morphine-induced dopamine release in rats.

Neuropharmacology 1996 S M Pearl, Isabelle M Maisonneuve, Stanley D Glick 16 citations

The present study examines the effect of prior morphine exposure on ibogaine antagonism of morphine-induced dopamine release. Female Sprague-Dawley rats were pretreated once a day for 2 days with morphine (20 mg/kg, i.p.) or saline and given a low dose of ibogaine (10 mg/kg, i.p.) or saline 5 hr after the last morphine or saline injection. Nineteen hours later, rats (awake and freely moving)...

Evaluation of agonist-antagonist properties of nitrogen mustard and cyano derivatives of delta 8-tetrahydrocannabinol.

Neuropharmacology 1996 J L Wiley, D R Compton, P M Gordon et al.

delta 8-Tetrahydrocannabinol (delta 8-THC) is a naturally occurring cannabinoid with a characteristic pharmacological profile of in vivo effects. Previous studies have shown that modification of the structure of delta 8-THC by inclusion of a nitrogen-containing functional group alters this profile and may alkylate the cannabinoid receptor, similar to the manner in which beta-funaltrexamine...

Dizocilpine-like discriminative stimulus effects of low-affinity uncompetitive NMDA antagonists.

Neuropharmacology 1996 K A Grant, G Colombo, J Grant et al.

The dizocilpine-like discriminative stimulus effects of a variety of channel blocking (uncompetitive) N-methyl-D-aspartate (NMDA) receptor antagonists were examined in rats trained to discriminate dizocilpine (0.17 mg/kg, i.p) from saline in a two-lever operant procedure. The dissociative anesthetic-type NMDA antagonists dizocilpine (ED50 0.05 mg/kg), phencyclidine (ED50 3.4 mg/kg) and ketamine...

The interactions of typical and atypical antipsychotics with the (-)2, 5,-dimethoxy-4-methamphetamine (DOM) discriminative stimulus.

Neuropharmacology October 1995 David Fiorella, Scott Helsley, R A Rabin et al.

The present study was designed to test the hypothesis that atypical, but not typical, antipsychotics produce a functional in vivo blockade of 5-HT2A receptors. The magnitude of functional in vivo 5-HT2A receptor blockade elicited by representative compounds from each of the six major structural classes of typical antipsychotics, and the representative atypical antipsychotics clozapine and...

Tissue distribution, metabolism and effects of bufotenine administered to rats.

Neuropharmacology July 1, 1995 R W Fuller, H D Snoddy, K W Perry 37 citations

Bufotenine (N, N-dimethyl-5-hydroxytryptamine) is a serotonin analog reported to be hallucinogenic. Bufotenine concentrations were measured by liquid chromatography with electrochemical detection after the s.c. injection of bufotenine (1, 30 or 100 mg/kg) into rats. At 1 hr, bufotenine was high in lung, heart and blood and lower in brain and liver. No N-monomethyl-5-hydroxytryptamine was...

Discriminative stimulus effects of CP 55,940 and structurally dissimilar cannabinoids in rats.

Neuropharmacology June 1995 J L Wiley, R L Barrett, J Lowe et al.

CP 55,940 is a potent synthetic bicyclic cannabinoid analog that has been used in a number of studies as a radioligand for the cannabinoid receptor. This compound shares behavioral and biochemical properties with naturally occurring cannabinoids such as delta 9-THC. The purpose of the present study was 3-fold: to establish the ability of CP 55,940 to serve as a discriminative stimulus, to...

Chlormethiazole, dizocilpine and haloperidol prevent the degeneration of serotonergic nerve terminals induced by administration of MDMA ('Ecstasy') to rats.

Neuropharmacology December 1994 K E Hewitt, A R Green

An investigation has been made into the effect of 3,4-methylenedioxymethamphetamine (MDMA or 'Ecstasy') administration on the concentration of 5-hydroxytryptamine (5-HT), uptake of [3H]5-HT and [3H]paroxetine binding in rat cerebral cortex tissue. Four days after 2 injections of MDMA (20 mg/kg i.p., 6 hr apart) the concentrations of 5-HT and its metabolite 5-HIAA were reduced by 60%. The...

Discriminative stimulus effects of delta 9-tetrahydrocannabinol and delta 9-11-tetrahydrocannabinol in rats and rhesus monkeys.

Neuropharmacology April 1993 J L Wiley, R L Barrett, D T Britt et al.

Previous reports have suggested that delta 9-11-tetrahydrocannabinol (delta 9-11-THC), an exocyclic analog of delta 9-tetrahydrocannabinol (delta 9-THC), may have weak agonist effects as well as antagonistic properties. The purpose of the present study was to examine the effects of delta 9-11-THC in substitution and antagonism tests in rats and in rhesus monkeys trained to discriminate delta...

Effects of mescaline and some of its analogs on cholinergic neuromuscular transmission

Neuropharmacology February 1, 1993 Emmanuel Ghansah, Prapaporn Kopsombut, M A Maleque et al. 22 citations

Mescaline (3,4,5-trimethoxyphenylethylamine; MES) and its analogs, anhalinine (ANH) and methylenemescaline trimer (MMT) were investigated, using sciatic-sartorius preparations of the frog and cortical tissue from the rat. The effects of MES and its analogs were examined with respect to muscle twitch, resting membrane potential and nicotinic receptor binding. Mescaline and its analogs (10-100...

Repeated administration of MDMA causes transient down-regulation of serotonin 5-HT2 receptors.

Neuropharmacology September 1992 Ursula Scheffel, John R. Lever, M Stathis et al.

The present study examined short- and long-term effects of MDMA (3,4-methylene-dioxymethamphetamine) on serotonin (5-HT2 and 5-HT1c) receptors in the brain of the rat. N1-Methyl-2-[125I]lysergic acid diethylamide ([125I]MIL) was used to label these receptors in vitro and in vivo. The usefulness of [125I]MIL for in vivo detection of changes in 5-HT2 receptors was confirmed in preliminary...

Stimulatory and inhibitory effects of serotonergic hallucinogens on spinal mono- and polysynaptic reflex pathways in the rat.

Neuropharmacology July 1, 1992 J Yamazaki, H Ono, T Nagao 23 citations

The effects of two 5-HT-related hallucinogens on rat spinal mono- and polysynaptic reflex pathways in the rat were investigated. 5-Methoxy-N,N-dimethyltryptamine (5-MeODMT, 1 and 100 micrograms/kg, i.v.), an indolealkylamine agent, produced a dose-dependent decrease in the monosynaptic reflex, whereas 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 1-100 micrograms/kg), a phenylalkylamine...

Effects of ibogaine on acute signs of morphine withdrawal in rats: independence from tremor.

Neuropharmacology May 1, 1992 Stanley D Glick, K Rossman, N C Rao et al. 121 citations

Because of the claim that ibogaine suppresses the symptoms of "narcotic withdrawal" in humans, the effect of ibogaine on naltrexone-precipitated withdrawal signs in morphine-dependent rats was assessed. Morphine was administered subcutaneously through implanted silicone reservoirs for 5 days. Ibogaine (20, 40 or 80 mg/kg, i.p.) or saline was administered 30 min prior to challenge with...

Degenerative and axon outgrowth-altering effects of phencyclidine in human fetal cerebral cortical cells.

Neuropharmacology March 1992 M P Mattson, B Rychlik, B Cheng

Babies born to mothers abusing the psychotomimetic drug phencyclidine (PCP), often show profound deficits in CNS function. It is now reported that PCP can cause progressive degeneration and death in human fetal cerebral cortical neurons in culture and sublethal levels of PCP can inhibit axon outgrowth. In cerebral cortical cell cultures established from 14 week fetuses, exposure to 500 microM...

Specificity of phencyclidine-like drugs and benzomorphan opiates for two high affinity phencyclidine binding sites in guinea pig brain.

Neuropharmacology September 1, 1990 A A Reid, M V Mattson, B R De Costa et al.

Recently, the presence of two high affinity binding sites for phencyclidine were described in guinea pig brain, with one site coupled to the glutamate excitatory amino acid receptor, specifically activated by N-methyl-D-aspartate (NMDA) (site 1) and the other site associated with the dopamine (DA) reuptake carrier (site 2). Phencyclidine and its analogs, as well as the benzomorphan opiates, are...

Reduction of in vivo binding of [3H]paroxetine in mouse brain by 3,4-methylenedioxymethamphetamine.

Neuropharmacology July 1990 Kenji Hashimoto, Tsuyoshi Goromaru

The effects of 3,4-methylenedioxymethamphetamine (MDMA) on the in vivo binding of [3H]paroxetine, a potent and selective 5-hydroxytryptamine (5-HT; serotonin) uptake inhibitor, in the brain of the mouse were studied. The distribution of radioactivity in the brain of the mouse, after intravenous administration of [3H]paroxetine, was significantly altered by pretreatment with MDMA (15 mg/kg,...

Effects of self-administered phencyclidine on regional uptake of 2-deoxy-D-[1-14C]glucose in brain.

Neuropharmacology June 1989 A D Weissman, K L Marquis, J E Moreton et al.

Phencyclidine profoundly alters cerebral metabolism in the rat. This study explored whether cerebral metabolic effects of phencyclidine differed when the drug was self-administered by trained rats, compared with when it was given acutely to naive rats. The regional cerebral uptake of 2-deoxy-D-[1-(D14C] glucose (DG) was examined following two injections of phencyclidine (0.5 mg/kg/injection,...

Immediate and long-term effects of 3,4-methylenedioxymethamphetamine on serotonin pathways in brain of rat.

Neuropharmacology December 1987 Donna M. Stone, Kalpana M. Merchant, Glen R. Hanson et al.

In the rat, administration of the psychoactive analog of amphetamine 3,4-methylenedioxymethamphetamine (MDMA), causes selective, pronounced decreases in markers of central serotonergic function. The time course of these neurochemical changes was examined in several serotonergic nerve terminal regions of the brain. Fifteen min after subcutaneous injection of MDMA (10 mg/kg), the enzymatic...

Phencyclidine-induced head-weaving and head-twitch through interaction with 5-HT1 and 5-HT2 receptors in reserpinized rats.

Neuropharmacology October 1987 K Yamaguchi, Toshitaka Nabeshima, K Ishikawa et al.

Phencyclidine mainly produced head-weaving and head-twitches at doses of 5-7.5 mg/kg and of 7.5-12.5 mg/kg, respectively. Phencyclidine-induced head-twitches and head-weaving were blocked by pretreatment with ritanserin (1 mg/kg), a selective serotonin (5-HT)2 receptor antagonist and with pindolol (20 mg/kg, s.c.), a 5-HT1 receptor antagonist, respectively. In reserpine-pretreated rats, the...

Electrophysiological effects of phencyclidine in the medial prefrontal cortex of the rat.

Neuropharmacology September 1987 A Gratton, B J Hoffer, R Freedman

The effects of local applications of phencyclidine (PCP) and dopamine (DA) on neurons of the medial prefrontal cortex were investigated using single unit recording techniques. The activity of the majority of cells in the deeper layers of the medial prefrontal cortex was depressed by both phencyclidine and DA, whereas increases, as well as decreases, in the firing rates were observed in cells...

Interactions between delta 9-tetrahydrocannabinol and cannabidiol as evaluated by drug discrimination procedures in rats and pigeons.

Neuropharmacology February 1986 A J Hiltunen, T U Järbe

Animals (rats and pigeons) were trained to discriminate between the presence and absence of delta 9-THC; the training doses were, respectively: 0.56 mg/kg (pigeons) and 3.0 mg/kg (rats). Once the drug discrimination was mastered, the pigeons were tested repeatedly after a single intramuscular (i.m.) injection of delta 9-THC (0.56 mg/kg) at the following intervals 0.5, 1.5, 4.5 and 9 hr after...

Indolealkylamines and prolactin secretion. A structure-activity study in the central nervous system of the rat.

Neuropharmacology December 1, 1985 G Seeman, G M Brown 5 citations

The present study was performed to examine the central effects of the indolealkylamine hallucinogens, 5-methoxy-N,N-dimethyltryptamine (MDMT), bufotenin and N, N-dimethyltryptamine (DMT), infused intracerebroventricularly (i.c.v.) into the lateral ventricle. They were found to have a stimulatory effect upon the secretion of prolactin. Their order of potency was compared. From a...

Sigma receptors mediated the psychotomimetic effects of N-allylnormetazocine (SKF-10,047), but not its opioid agonistic-antagonistic properties.

Neuropharmacology August 1, 1984 N Khazan, G A Young, E E El-Fakany et al.

Our present findings suggest that SKF-10,047, the prototype sigma agonist, has its opioid entity residing with its (-) isomer, while both its (+) and (-) isomers possess psychotogenic properties similar to those produced by PCP. We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical...

Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. A comparison with prolyl-leucylglycine amide (MIF), anti-Parkinsonian drugs and clonazepam.

Neuropharmacology June 1, 1983 G Zetler 18 citations

Cholecystokinin octapeptide (CCK-8), ceruletide (caerulein, CER) and 10 analogues of ceruletide, were studied in mice for antagonism of the tremors induced by harmine (5 mg/kg, s.c.), ibogaine (20 mg/kg, s.c.) and oxotremorine (0.2 mg/kg, s.c.). The following reference drugs were tested for comparison: prolyl-leucylglycine amide (MIF), atropine, haloperidol, biperiden, ethopropazine,...

Drug interactions do not support reduction in serotonin turnover as the mechanism of action of benzodiazepines.

Neuropharmacology October 1, 1982 R A Shephard, D A Buxton, P L Broadhurst 59 citations

Interactions between 5-methoxy, N,N-dimethyltryptamine (5-MeODMT), chlordiazepoxide and para-chlorophenylalanine (pCPA) on conflict behaviour were studied. 5-Methoxy, N,N-dimethyltryptamine (1.0 and 3.0 mg/kg), induced observable effects and reduced unpunished response rates but did not affect punished behaviour either alone, on in the presence of 5 or 10 mg/kg chlordiazepoxide. However,...