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PubMed1983

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

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 tested at the same concentration range did not modulate spontaneous or K+-evoked [3H]dopamine release. The inhibitory effects of the psychotomimetics tested were antagonized by equal concentrations of haloperidol or methiothepine. It is postulated that the effects of psychotomimetics on DA release were triggered via simultaneous action at presynaptic dopamine and 5-hydroxytryptamine receptors which are located at dopamine nerve endings in the nucleus accumbens.

Animals↗
PubMed1987

Specific antagonists of the acute behavioral response to centrally-administered vasopressin in mice.

Vasopressin and related peptides cause behavioral excitation after intracerebroventricular injection in mice. This behavioral excitation is characterized by excessive scratching and grooming behavior in the unrestrained animal and enhanced escape-directed activity in stressful situations. These effects of vasopressin were found to be blocked by the administration of analogs which act as competitive antagonists of the pressor-activity of vasopressin. The potencies of these analogs in suppressing the behavioral effect paralleled the pressor antagonist potencies. The antagonists did not cause the characteristic behavioral alterations by themselves, nor did they block grooming and/or scratching behavior induced by the structurally-unrelated substances, mescaline, bombesin and substance P. It is suggested that these antagonists provide useful tools for studying the role of endogenous vasopressin in behavior.

Animals↗
PubMed1980

EEG effects of hallucinogens and cannabinoids using sleep-waking behavior as baseline.

Three hallucinogens (d-lysergicacid diethylamide (LSD), mescaline, psilocybin) and two cannabinoid derivatives (tetrahydrocannabinol (THC), synhexyl) were tested for their long-term effects on the EEG of the cat. The drug-induced alterations in the EEG frequency spectrum were "drug-specific" in the sense that they would be statistically unlikely to occur during sleep-waking behavior. The two classes of compounds produced distinctly different EEG effects which were remarkably similar within each class. The duration of activity and relative potencies were consistent with those obtained by other measures, both in cats and in other species including man.

Animals↗
PubMed1981

The role of central serotonergic mechanisms on head-twitch and backward locomotion induced by hallucinogenic drugs.

Head-twitch induced by lysergic acid diethylamide, mescaline and 2,5-dimethoxy-4-methylamphetamine (DOM) was significantly increased by medial raphe (m-R) lesions, but dorsal raphe (d-R) lesions did not produce any changes. Hallucinogen-induced head twitch was inhibited by methysergide and tended to be increased by PCPA. These results suggest that 5-HT receptors innervated with the ascending 5-HT pathway originating in the m-R play a vital role in the manifestation of hallucinogen-induced head-twitch. That is, increase of head-twitch is ascribed to supersensitivity of 5-HT receptors. On the other hand, DOM-induced backward locomotion was inhibited by m-R or both dorsal and medial raphe lesions and methysergide, and was reversed to forward locomotion, differently from the hallucinogen-induced head-twitch. A reversion of backward locomotion was not obtained with d-R lesions or PCPA treatment.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1982

Drug-induced ataxia in opponents elicits "pathological" fighting in undrugged rats exposed to footshock.

One member of a pair of rats was administered either mescaline, lysergic acid diethylamide (LSD), pentobarbital, or ethanol intraperitoneally twenty minutes prior to exposure to footshock in the presence of an undrugged opponent. At high doses, all drugs elicited biting from the undrugged rat of sufficient intensity to produce injury to its drugged opponent. Low doses produced species-typical fighting behavior which consisted of striking each other with their forepaws while upright and failed to elicit biting. Biting attacks by the undrugged rat were highly correlated with ataxic behavior by the drugged rat. Conversely, species-typical aggressive behavior was highly correlated with behaviors such as boxing or upright threat posture. These results suggest that drug-induced ataxic behavior may disinhibit mechanisms that regulate intra-species behavior, thus producing behavior that is more typical of inter-species aggression.

Aggression↗
PubMed1983

Ethanol intake increases during continuous administration of amphetamine and nicotine, but not several other drugs.

Groups of rats, acclimated to drinking both water and 10% v/v ethanol were implanted with a variety of slow-release devices containing d-amphetamine (d-amp), nicotine, caffeine, phencyclidine (PCP), secobarbital, LSD, mescaline or haloperidol. Ethanol intake was elevated only during treatment with d-amp or nicotine; none of the other drugs affected ethanol consumption even though the amounts of all drugs released were pharmacologically sufficient to affect behavior. Nicotine treated rats were not simply seeking calories provided by the EtOH solution, since nicotine treatment did not enhance intake of a distinctively flavored solution isocaloric to 10% ethanol. These results support a self-medication model of ethanol intake.

Alcohol Drinking↗
PubMed1985

The 5HT2 antagonist pirenperone reverses disruption of FR-40 by hallucinogenic drugs.

Indolealkylamine and phenethylamine hallucinogens disrupted responding maintained under a fixed-ratio 40 (FR-40) schedule of reinforcement. LSD, DMT, mescaline and DOM produced dose-dependent decreases in number of reinforcers and increases in 10-sec periods of non-responding (pause-intervals). The 5HT agonist quipazine, as well as the LSD congener lisuride, altered response patterns in a similar manner. The effects of these drugs were examined after pretreatment with pirenperone, an antagonist with specificity toward the 5HT2 receptor with reference to the 5HT1 receptor. The dose-response curves for the phenethylamine hallucinogens were shifted significantly to the right and to a greater degree than were those for the indolealkylamine hallucinogens. Pirenperone also antagonized the effects of quipazine to a degree similar to that observed with the phenethylamine-type hallucinogens. Pirenperone did not significantly shift the dose-response pattern to lisuride. These data suggest that the behavioral disruption induced by these hallucinogens and quipazine relates at least in part to an effect on 5HT2 receptors, while the effects of lisuride do not involve a significant interaction at the 5HT2 receptor.

Animals↗
PubMed1982

Neurophysiological effects of hallucinogens on serotonergic neuronal systems.

Low intravenous doses of the hallucinogen d-lysergic acid diethylamide (LSD) markedly suppress the discharge of serotonin (5-HT)-containing neurons in the dorsal raphe nucleus of the rat. Microiontophoretically applied LSD also inhibits the firing of 5-HT neurons, indicating that the inhibitory effect is mediated directing on 5-HT neurons. Forebrain neurons receiving a major serotonergic input are relatively insensitive to LSD. Other indole hallucinogens (i.e., psilocin, dimethyltryptamine, and 5-methoxydimethyltryptamine) also preferentially inhibit raphe firing as compared to postsynaptic forebrain neurons. These observations led to the hypothesis that hallucinogens produce their psychoactive effects by acting preferentially upon 5-HT autoreceptors in the dorsal raphe allowing postsynaptic neurons to escape from the tonic inhibitory action of 5-HT neurons. However, problems exist with the concept that hallucinogens produce their psychoactive effects by disinhibiting postsynaptic neurons. First, the time course of the behavioral and neuronal effects of LSD do not correlate. Second, 5-HT neurons do not become tolerant to the inhibitory actions of LSD. Third, the hallucinogen mescaline fails to directly inhibit 5-HT neurons. Finally, the nonhallucinogen lisuride markedly suppresses the discharges of 5-HT neurons. These observations suggest that postsynaptic actions of hallucinogens may be of prime importance in producing their psychedelic effects. Evidence is presented to suggest that the hallucinogens may act postsynaptically to sensitize both serotonergic and noradrenergic receptors. It is suggested that a mechanism of receptor sensitization, in distinction to disinhibition, might account for the altered perceptual reactivity produced by these drugs.

Animals↗
PubMed1987

Comparison of stimulants and hallucinogens on shuttle avoidance in rats.

Rats were trained to a high level of performance of a conditioned avoidance response in a shuttlebox to test effects of several classical stimulants in comparison to a variety of hallucinogens. A previously-reported biphasic pattern of effects of mescaline on shuttle avoidance was replicated and extended to 12 other hallucinogens of both phenylethylamine and indolealkylamine classes. Response patterns of hallucinogens could be differentiated from 3 stimulants and from a methoxyamphetamine compound that lacks hallucinogenic activity.

Amphetamines↗
PubMed1998

Second thoughts on psychedelic drugs.

Psychedelic drugs are making a comeback. Proponents of psychedelics point to the widespread medical experimentation with mescaline and lysergic acid diethylamide-125 (LSD) in the 1950s as proof of their safety and efficacy. However, a review of the private and published writings of Sidney Cohen, MD, who conducted the first study of the safety of psychedelics, reveals that serious medical concerns about psychedelics arose before the public backlash against the drugs in the 1960s. The story of psychedelic research is a reminder of the inevitable complications involved in testing drugs on human subjects.

Drug Approval↗
PubMed1991

Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.

A series of 2-(aminoalkyl)naphth[1,8-cd]isothiazole 1,1-dioxides was synthesized and examined in various receptor binding tests. Most compounds demonstrated high affinity for the 5-HT2 receptor with moderate to high selectivity. A member of this series, compound 24 (RP 62203), displays high 5-HT2 receptor affinity (Ki = 0.26 nM), which is respectively more than 100 and 1000 times higher than its affinity for alpha 1 (Ki = 38 nM) and D2 (Ki greater than 1000 nM) receptors. This compound is a potent orally effective and long lasting 5-HT2 antagonist in the mescaline-induced head-twitches test in mice and rats.

Animals↗
PubMed2001

N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.

A series of N(1)-arylsulfonyltryptamines were found to be potent ligands of the human serotonin 5-HT(6) receptor with the 5-methoxy-1-benzenesulfonyl analogue (19) having the highest affinity. Additionally, it was discovered that a group such as 3-(3-methoxybenzyl)-1,2,4-oxadiazol-5-yl in the 2-position of the indole ring (43) can replace the arylsulfonyl substituent in the 1-position with no loss of affinity. This suggested that the binding conformation of the aminoethyl side chain at this receptor was toward the 4-position of the indole ring and was supported by the fact that the 4-(aminoethyl)indoles (45) also displayed high affinity, as did the conformationally rigid 1,3,4,5-tetrahydrobenz[c,d]indole (49). Molecular modeling showed that 19, 43, and 45 all had low-energy conformers that overlaid well onto 49. Both 19 and 49 had good selectivity over other serotonin receptors tested, with 49 also showing excellent selectivity over all dopamine receptors. In a functional adenylate cyclase stimulation assay, 19 and 49 had no agonist activity, whereas 45 behaved as a partial agonist. Finally, it was shown that 19 had good activity in the 5-HT(2A) centrally mediated mescaline-induced head twitch assay, which implies that it is brain-penetrant.

Animals↗
PubMed1998

Chemistry and pharmacology of hallucinogens, entactogens and stimulants.

Amphetamines, tryptamines, phencyclidines, tetrahydrocannabinol and substances of the ecstasy group are characterized as stimulants, hallucinogens and entactogens. The various effects of each group and their mode of action in different transmitter systems are described. 28 new compounds of the amphetamine and tryptamine series has been calculated, which exceed the hallucinogenic effects of mescaline. The different pathways of the metabolism of MDMA (ecstasy) and MDE in humans may probably explain their individual effects.

3,4-Methylenedioxyamphetamine↗
PubMed1970

Steric and electronic relationships among some hallucinogenic compounds.

Stereochemical considerations and total valence electron calculations suggest congruities among the ostensibly dissimilar hallucinogenic compounds, D-lysergic acid diethylamide (LSD), indolcalkylamines, and methoxylated amphetamines. In LSD the aromatic benzene ring A and the N-6 nitrogen are essential for hallucinogenic activity; these sites may react with the receptor. The conformations of amphetamines and indolealkylamines at the receptor are such that the aromatic benzene ring lies like ring A of LSD and the alkylamino nitrogen lies like the N-6 of LSD. Ring A may interact with the receptor by forming a pi-molecular complex, as suggested by the correlation between hallucinogenic activity and energy of the highest occupied molecular orbital (E(H)) of congeneric series. The N-6 nitrogen of LSD and the sterically congruent nitrogen of the other hallucinogenic compounds may react with the receptor by forming a donor acceptor complex of the n-pi(*) or n-sigma(*) type. Other portions of the hallucinogenic molecules confer a favorable E(H): these include the methoxy and hydroxyl groups of the amphetamines (and mescaline), and the indolealkylamines; and the pyrrole ring of LSD and the indolealkylamines.

Amphetamine↗
PubMed1971

Specificity of the antibody receptor site to D-lysergamide: model of a physiological receptor for lysergic acid diethylamide.

Antibodies to D-lysergic acid have been produced in rabbits and guinea pigs and a radioimmunoassay for the hapten was developed. The specificity of this lysergamide-antilysergamide reaction was determined by competitive binding with unlabeled lysergic acid diethylamide (LSD), psychotomimetic drugs, neurotransmitters, and other compounds with diverse structures. LSD and several related ergot alkaloids were potent competitors, three to seven times more potent than lysergic acid itself. The N,N-dimethyl derivatives of several compounds, including tryptamine, 5-hydroxytryptamine, 4-hydroxytryptamine, 5-methoxytryptamine, tyramine, and mescaline, were only about ten times less effective than lysergic acid, even though these compounds lack some of the ring systems of lysergic acid. The pattern of inhibition by related compounds with various substituents suggests that the antibody receptor site recognizes structural features resembling the LSD molecule. In particular, the aromatic nucleus and the dimethylated ethylamine side chain in phenylethylamine and tryptamine derivatives may assume in solution a conformation resembling ring A and the methylated nitrogen in ring C of LSD. Among the tryptamine derivatives, a large percentage of the most potent competitors are also psychotomimetic compounds.

Amines↗
PubMedDate not supplied

Jekyll and Hyde revisited: paradoxes in the appreciation of drug experiences and their effects on creativity.

Historically, states of intoxication--like dreams and madness--are seen in either one of two opposed ways. The intoxicated are either "possessed" or "under the influence" of an external agency, or revealing hidden feelings or truths (in vino veritas). Along the same lines, artists who worked during LSD, mescalin or psilocybin intoxication often refer to feelings of either being "possessed" or "liberated," a difference that can be explained partly by their expectations and partly by their evaluations, which both tend to conform to the cultural dichotomy in interpreting the irrational. Both interpretations, however, tend to obscure not only the other, but also-it is posited-the paradoxical nature of the drug experience itself. Analysis of a protocol shows that intoxication might comprise feelings of "possession" as well as "liberation" almost simultaneously, and mediumistic and some psychedelic art shows stylistic traits that can be seen as the visual expressions of both these feelings. It seems that the "demoniacal" and "psychedelic" mode come together in experiential reality, only to be divided in the cultural sphere.

Art↗
PubMed2004

Transient reinforcing effects of phenylisopropylamine and indolealkylamine hallucinogens in rhesus monkeys.

Relatively few studies have assessed the reinforcing effects of hallucinogenic compounds, and no such studies have attempted to engender contingent responding for these compounds in animals with behavioral histories that include experience with serotonergically mediated reinforcing effects. The objectives of the present study were to investigate the capacity of several hallucinogenic compounds to maintain self-administration behavior in rhesus monkeys with a previous history of 3,4-methylenedioxymethamphetamine (MDMA) self-administration, and to compare these effects across a range of doses of drugs from two structural classes (indolealkylamines and phenylisopropylamines). The results indicate that no compound generated reliable responding and that no subject ever self-administered 4-iodo-2,5-dimethoxyphenylisopropylamine (DOI) at rates above those engendered by contingent saline. However, 3 out of 4 subjects did respond at rates between 0.75 and 3.0 responses/s in one or more sessions where N,N-dimethyltryptamine (DMT), mescaline or psilocybin were available. During some of these sessions in which self-administration was maintained, animals earned a majority of all available infusions and appeared intoxicated by the end of the session. This pattern of transient self-administration may indicate that these compounds have weak reinforcing effects, or mixed reinforcing and aversive effects.

Amines↗
PubMed1957

The preservation of substance P by lysergic acid diethylamide.

Lysergic acid diethylamide (LSD) potentiated the response of guinea-pig ileum to substance P but not to histamine. It also inhibited the disappearance of substance P when incubated with guinea-pig brain extract but not when incubated with chymotrypsin. Eserine, morphine, mescaline, chlorpromazine, ergometrine, strychnine and 2 bromo-LSD did not have this effect. Oxytocin was not destroyed by brain extract. The inhibition of the destruction of substance P by LSD could be antagonized by 2 bromo-LSD. This effect of LSD may have some relation to its pharmacological actions.

Brain↗