Life Sciences
August 15, 2023
Lily Freeman-Striegel, John Hamilton, Renuka Kannappan et al.
Acute and chronic Δ9-THC exposure paradigms affect the body differently. More must be known about the impact of chronic Δ9-THC on cannabinoid-1 (CB1R) and mu-opioid (MOR) receptor levels in the brain. The present study examined chronic Δ9-THC's effects on CB1R and MOR levels and locomotor activity. Adolescent Sprague-Dawley rats were given daily intraperitoneal injections of Δ9-THC [0.75mg/kg...
Life Sciences
December 22, 2005
Thomas E Prisinzano
128 citations
At present, the Mexican mint Salvia divinorum is an unregulated hallucinogen. This has resulted in various on-line botanical companies advertising and selling S. divinorum as a legal alternative to other regulated plant hallucinogens. It is predictable that its misuse will increase rapidly. The active ingredient in S. divinorum is the neoclerodane diterpene, salvinorin A (1a), which has been...
Life Sciences
December 22, 2005
Kerry Ann O'Connor, Bryan L. Roth
22 citations
Throughout time, humans have used psychoactive plants and plant-derived products for spiritual, therapeutic and recreational purposes. Furthermore, the investigation of psychoactive plants such as Cannabis sativa (marijuana), Nicotiana tabacum (tobacco) and analogues of psychoactive plant derivatives such as lysergic acid diethylamide (LSD) have provided insight into our understanding of...
Life Sciences
October 15, 2004
Feng Yan, Bryan L. Roth
68 citations
kappa-opioid receptors (KORs) represent the principal site of action of dynorphin and related neuropeptides. Recently, Salvinorin A--a naturally occurring neoclerodane diterpene hallucinogen was identified to be a highly selective KOR agonist. In this brief review we summarize the known chemistry, pharmacology and biology of salvinorin A. Because salvinorin A profoundly alters human...
Life Sciences
September 19, 2003
Stephen I Deutsch, Richard B Rosse, Eddie N Billingslea et al.
The ability of phencyclidine (PCP), a noncompetitive antagonist of NMDA receptor-mediated neurotransmission, to precipitate a schizophreniform psychosis in susceptible individuals is consistent with the hypothesized pathologic occurrence of NMDA receptor hypofunction in this disorder. Because the psychosis caused by PCP resembles schizophrenia in all of the relevant domains of psychopathology,...
Life Sciences
December 8, 2000
Jerrold C Winter, M Doat, R A Rabin
The present investigation examined the interaction between 2,5-dimethoxy-4-methylamphetamine [DOM] and non-competitive NMDA antagonists in rats trained with DOM [0.6 mg/kg; 75 min pretreatment time] as a discriminative stimulus. Pretreatment with phencyclidine [PCP] at a dose of 3 mg/kg shifted the DOM dose-response relationship to the left. When a fixed dose of DOM [0.1 mg/kg] which by itself...
Life Sciences
November 17, 2000
Claudio Acuña-Castillo, C Scorza, M Reyes-Parada et al.
3 citations
To assess the pharmacodynamic profile of ALEPH-2, a phenylisopropylamine derivative with alleged anxiolytic and hallucinogenic properties, Xenopus laevis oocytes were microinjected with either of the rat cRNA for the 5-HT2A or the 5-HT2C receptor. Concentration-response curves were obtained following the exposure of the oocytes to varying concentrations of either ALEPH-2 or 5-hydroxytryptamine...
Life Sciences
June 1, 1998
Sabrina Giacomelli, Maura Palmery, Luca Romanelli et al.
51 citations
The hallucinogenic effects of lysergic acid diethylamide (LSD) have mainly been attributed to the interaction of this drug with the serotoninergic system, but it seems more likely that they are the result of the complex interactions of the drug with both the serotoninergic and dopaminergic systems. The aim of the present study was to investigate the functional actions of LSD at dopaminergic...
Life Sciences
1997
Scott Helsley, R A Rabin, Jerrold C Winter
13 citations
In the present investigation, Fischer-344 rats were trained to discriminate 10.0 mg/kg of ibogaine from water using a pretreatment time of 60 minutes. Analysis of dose response data generated an ED50 of 4.6 mg/kg. The time course of the ibogaine (10.0 mg/kg) cue was also determined. The stimulus reached a maximum level of 94% ibogaine-appropriate responding at the 60-min pretreatment time. This...
Life Sciences
1996
L B Hough, S M Pearl, Stanley D Glick
72 citations
The distribution of the putative anti-addictive substance ibogaine was measured in plasma, brain, kidney, liver and fat after ip and sc administration in rats. One hr after ip dosing (40 mg/kg), drug levels ranged from 106 ng/ml (plasma) to 11,308 ng/g (fat), with significantly higher values after sc administration of the same dose. Drug levels were 10-20 fold lower 12 hr after the same dose....
Life Sciences
1996
Piotr Popik
18 citations
Anecdotal observations in humans indicate that indole alkaloid ibogaine may have anti-addictive properties. It has been suggested that the therapeutic action of ibogaine may depend upon facilitated access to the past experiences, purportedly influencing the initiation of drug addiction. To determine if ibogaine may facilitate memory retrieval, rats were trained in the Morris maze spatial...
Life Sciences
1996
E D French, K Dillon, S F Ali
12 citations
Ibogaine, an indole containing alkaloid, has been shown to reduce the rate of injection of morphine and cocaine in self-administration protocols. Since morphine- and cocaine-induced modulation of dopamine release is impulse dependent and essential for their reinforcing effects, disruption of dopamine neuronal activity by ibogaine could explain its purported 'antiaddictive' properties....
Life Sciences
1995
R H Mach, C R Smith, S R Childers
145 citations
The alkaloid ibogaine is potentially useful to reduce craving for several drugs of abuse, but its mechanism of action is not known. In the current study, in vitro studies were conducted in order to determine the affinity of ibogaine for sigma receptors. Our results indicate that ibogaine has a relatively high affinity for sigma 2 receptors (Ki = 90.4 and 250 nM) and a significantly lower...
Life Sciences
1995
Deborah C. Mash, J K Staley, Michael H. Baumann et al.
108 citations
Ibogaine is a hallucinogenic indole with putative efficacy for the treatment of cocaine, stimulant and opiate abuse. The purported efficacy of ibogaine following single dose administrations has led to the suggestion that a long-acting metabolite of ibogaine may explain in part how the drug reduces craving for psychostimulants and opiates. We report here that 12-hydroxyibogamine, a primary...
Life Sciences
1995
E E Codd
29 citations
The naturally occurring indole alkaloid ibogaine is of interest because of its reported ability to block drug seeking behavior for extended periods. The compound also potentiates morphine-induced analgesia in mice and reduces certain naltrexone-precipitated withdrawal signs in morphine-dependent rats. Although these results might suggest ibogaine interaction with opioid receptors, previous...
Life Sciences
1994
S Okuyama, Y Imagawa, T Sakagawa et al.
Phencyclidine (PCP)-induced psychosis is a useful animal model for studies on schizophrenia. N, N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)-phenyl]- ethylamine monohydrochloride (NE-100) had no effect on conditioned avoidance responses (CAR) in rats, whereas, the PCP-induced impairment of avoidance inhibition was attenuated by NE-100. The PCP-induced ataxia or decreased attention in rhesus...
Life Sciences
1994
S Ogawa, S Okuyama, H Araki et al.
Phencyclidine (PCP)-induced behavior in rats was investigated in water maze and diving behavior tasks. The swimming and diving latencies of PCP-treated groups placed in a water maze apparatus were gradually shortened, and prolonged, respectively, while rats in a control group performed well. In all rats, stereotyped behavior and hyperlocomotion were absent. We propose that this animal model...
Life Sciences
1992
Henry Sershen, Audrey Hashim, L Harsing et al.
65 citations
Ibogaine (40 mg/kg i.p.), when given 2 hours before an acute injection of cocaine (25 mg/kg s.c.) to C57BL/6 mice, reduced the cocaine-induced locomotor stimulation. Such stimulation was also reduced in the ibogaine-treated mice when a second injection of cocaine was given 24 hr later. Thus, the reduction in locomotor activity was not just the short-term depression of locomotor activity seen...
Life Sciences
1992
Henry Sershen, L G Harsing, Audrey Hashim et al.
33 citations
The effect of ibogaine hydrochloride on locomotor stimulation induced by d-amphetamine sulfate was tested in male C57BL/6By mice and in female Sprague-Dawley rats. In mice, locomotor stimulation induced by d-amphetamine at 1 or 5 mg/kg s.c. was reduced by prior administration of one or two injections of ibogaine (40 mg/kg), given 2 or 18 hours earlier. This reduction in locomotor activity...
Life Sciences
1990
Yossef Itzhak, Ira D. Stein
99 citations
An increasing amount of evidence suggests the existence of specific binding sites for psychotomimetic drugs from the opiate-benzomorphan and arylcyclohexylamine series. The sigma binding sites have preferential affinity for the dextrorotatory isomers of certain opiate benzomorphans, such as (+)SKF 10047, (+)cyclazocine and (+)pentazocine and also for some neuroleptics (e.g., haloperidol). The...
Life Sciences
1989
Ramesh Arora, Herbert Y. Meltzer
175 citations
3H-Lysergic acid diethylamide (3H-LSD) binding, a putative measure of 5-HT2 receptor binding, was studied in the blood platelets of 29 depressed patients and 24 normal controls. The Bmax (maximum number of 3H-LSD binding sites) in the blood platelets of depressed patients was significantly greater than that of normal volunteers. This increase in Bmax was due to an increase in female depressed...
Life Sciences
September 1, 1986
Elizabeth A. Sykes
10 citations
Motor impairment, especially ataxia, is often mentioned as a 'side effect' of doses of psychoactive drugs which depress animal behaviour; it is difficult to determine it accurately from visual observation, but relatively few attempts have been made to measure it objectively and quantitatively. Mescaline, in moderate to large doses, can induce biphasic--depressant followed by stimulant--effects...
Life Sciences
July 1, 1985
M A Sills, I Lucki, A Frazer
54 citations
Repeated administration to rats of the 5-HT1A-selective agonist 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) produced tolerance to the ability of a test dose of 5-MeODMT to produce the serotonin behavioral syndrome, but not to the ability of a test dose of the 5-HT1B-selective agonist m-chlorophenylpiperazine (mCPP) to decrease locomotor activity. Conversely, repeated administration of mCPP...
Life Sciences
December 17, 1984
Richard A Glennon, M Titeler, J D Mckenney
636 citations
The affinities (Ki values) of twenty two psycho-active agents, including LSD, 5-OMe DMT and a series of phenalkylamine derivatives, for cortical 5-HT1 and 5-HT2 binding sites were compared with two measures of behavioral activity. It was found that a significant correlation (r = 0.938) exists between the 5-HT2 binding affinities of these agents and their ED50 values as determined in tests of...
Life Sciences
March 19, 1984
A A Larson
3 citations
Both acute and chronic effects of lysergic acid diethylamide (LSD) and 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) on the dorsal root potential (DRP), evoked by stimulation of the nucleus raphe magnus of the cat, were examined. Single injections of LSD potentiated while those of 5-MeODMT inhibited the raphe-evoked DRP. The electrophysiologic response produced by each drug correlates well in...