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PubMed1984

The hallucinogens and the inhalants.

The hallucinogenic drugs represent a recurrent outbreak pattern with each generation or two seeming to rediscover their ego-dissolving effects. The inhalants produce a short-lived intoxication with certain volatile solvents affecting specific organ systems.

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

Discriminative stimulus properties of MDA analogs.

Rats trained to discriminate (+/-) 2,5-dimethoxy-4-methylphenylisopropylamine (DOM) (1.0 mg/kg) from saline, using a standard two-lever operant task, were challenged with various doses of 3,4-methylenedioxyphenylisopropylamine (MDA) and several related agents. The (+/-)-DOM stimulus generalized to (+/-)-MDA, suggesting that both agents apparently produce similar stimulus cues. Related agents, known to produce effects in man similar to those produced by (+/-)-MDA, also resulted in generalization when administered to the DOM-trained animals, e.g., R(-)-MDA and a methoxylated derivative of (+/-)-MDA, (+/-)-2-OMe-4,5-MDA. DOM stimulus generalization was not observed for S(+)-MDA, the N-monomethyl and alpha-demethyl derivatives of MDA, nor for a metabolite of MDA (i.e., 3-methoxy-4-hydroxyphenylisopropylamine). The results suggest that R(-)- and (+/-)-MDA, as well as (+/-)-2-OMe-4,5-MDA, but not the other derivatives of MDA, are capable of producing behavioral (stimulus) effects common to those produced by the training dose of (+/-)-DOM.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1983

QSAR studies on psychotomimetic phenylalkylamines.

Attempts have been made to correlate hyperthermic potencies in rabbits and LSD-like effect in rat of a series of phenylisopropylamines (amphetamines) with physico-chemical parameters. In case of 2,4,5-trisubstituted analogs, hyperthermic potencies are found to be well correlated parabolically with the hydrophobic parameter pi. However, for the same series, the LSD-like effect is found to be related with pi in combination of steric parameter of 4-substituent. It is therefore inferred that hyperthermia in rabbit may be the function only of the hydrophobic character of molecule, but the LSD-like effect is influenced by the steric hindrance of 4-substituent also.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1994

Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands.

5-HT2C receptor antagonists, such as mianserin and mesulergine, exhibit negative intrinsic activity, defined as a decrease in agonist-independent, receptor-mediated, phosphoinositide hydrolysis in cells transfected with the 5-HT2C receptor cDNA. These drugs are classified as inverse agonists. Guanine nucleotides reciprocally modulate the binding of an agonist and inverse agonist, suggesting that an inverse agonist binds preferentially to the G protein-uncoupled form of the 5-HT2C receptor. Another 5-HT2C receptor antagonist, 2-bromolysergic acid diethylamide, functions as a neutral antagonist with no intrinsic activity, but is able to block both agonist and inverse agonist. Chronic treatment of choroid plexus cells with an inverse agonist, but not with the neutral antagonist, causes 5-HT2C receptor down-regulation, suggesting that the biological effects of 5-HT2C receptor antagonists are not solely due to antagonism of endogenous agonist. These results provide evidence that constitutively active 5-HT2C receptors are biologically significant. The functionally distinct properties of inverse agonists and neutral antagonists may elucidate the mechanisms controlling basal receptor activity states and lead to novel approaches in the development of therapeutic agents.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1994

Role of various 5-HT receptor subtypes in mediating neuroendocrine effects of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) in rats.

The phenylisopropylamine hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) produced dose-related increases in plasma concentrations of prolactin, adrenocorticotropic hormone (ACTH) and corticosterone but not growth hormone in rats. Pretreatment with metergoline (serotonin, 5-HT1/5-HT2 antagonist), ritanserin and mianserin (5-HT2A/5-HT2C antagonists) significantly attenuated DOM-induced increases in prolactin, ACTH and corticosterone, whereas mesulergine (5-HT2A/5-HT2C antagonist) pretreatment significantly attenuated DOM-induced increases in plasma prolactin and ACTH but not corticosterone. Pretreatment with propranolol (beta adrenoceptor antagonist that also has high binding affinity for 5-HT1A, 5-HT1B and 5-HT2C sites), MDL-72222 and ondansetron (5-HT3 antagonists) attenuated DOM's effect on plasma prolactin, but did not attenuate DOM-induced increases in either ACTH or corticosterone. On the other hand, spiperone (5-HT1A/5-HT2A/D2 antagonist) pretreatment significantly attenuated DOM-induced increases in ACTH but not corticosterone. These findings demonstrate involvement of 5-HT2A/5-HT2C and 5-HT3 receptors in mediating DOM-induced increases in plasma prolactin, whereas DOM-induced increases in ACTH appear to be mediated by stimulation of 5-HT2A receptors. DOM-induced corticosterone secretion appears to be mediated by stimulation of 5-HT2A and/or 5-HT2C receptors. DOM does not affect growth hormone secretion in rats.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1994

Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists.

Expression of the 5-hydroxytryptamine type 2C (5-HT 2C) receptor in NIH/3T3 fibroblasts results in agonist-independent 5-HT2C receptor activation. Some 5-HT2c receptor antagonists decrease this activation and are termed inverse agonists. The present study uses this system to evaluate functional and receptor binding properties of other 5-HT2C receptor antagonists. A number of inverse agonists, including clozapine, and a neutral antagonist (methysergide) were identified in a functional assay. Guanine nucleotides increased the affinity of a radiolabeled inverse agonist ([3H]mesulergine), suggesting that inverse agonists bind the G protein-uncoupled form of the 5-HT2C receptor with high affinity. Competition binding was performed using conditions that separately labeled the G protein-coupled and -uncoupled forms of the receptor. These studies demonstrated that inverse agonists bound the uncoupled form of the 5-HT2C receptor with higher affinity, compared with the G protein-coupled form. Agonists, on the other hand, had higher affinity for the coupled form whereas neutral antagonists had equal affinity for both forms of the receptor. Thus, 5-HT2C receptor neutral antagonists exhibited functional and receptor binding properties consistent with those of classical receptor antagonists. However, 5-HT2C receptor inverse agonists displayed functional and receptor binding properties that were opposite those of agonists.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1994

Evidence that 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane-induced hypophagia and hyperthermia in rats is mediated by serotonin-2A receptors.

The administration of various doses of the phenylisopropylamine hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) to rats produced dose-related decreases in 1-hr food intake in a food-restricted paradigm and in locomotor activity. DOM also produced dose-related increases in temperature. Pretreatment with propranolol [a beta adrenoceptor antagonist that also has high binding affinity for serotonin (5-HT) 5-HT1A, 5-HT1B and 5-HT2C sites], bemesetron or ondansetron (5-HT3 antagonists) did not attenuate either DOM-induced hypophagia or hyperthermia. In contrast, pretreatment with metergoline (a 5-HT1/5-HT2 antagonist) and ritanserin (a 5-HT2A/5-HT2C antagonist) significantly attenuated both DOM-induced hypophagia and hyperthermia. However, pretreatment with mesulergine (a 5-HT2C/5-HT2A antagonist) significantly attenuated DOM-induced hyperthermia but not hypophagia. On the other hand, spiperone (5-HT1A/5-HT2A/D2 antagonist) pretreatment significantly attenuated DOM-induced hyperthermia but accentuated DOM-induced hypophagia. Daily administration of DOM (1.0 mg kg-1 day-1) produced complete tolerance to its hypophagic effect by day 4 but did not produce cross-tolerance to m-chlorophenylpiperazine-induced hypophagia. In contrast, daily administration of DOM for 7 days did not produce either tolerance to its hyperthermic effect or modify m-chlorophenylpiperazine-induced hyperthermia in rats. These findings suggest that DOM-induced hypophagia and hyperthermia in rats are mediated by stimulation of 5-HT2a receptors.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1993

5-hydroxytryptamine1C receptor density and mRNA levels in choroid plexus epithelial cells after treatment with mianserin and (-)-1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.

5-Hydroxytryptamine (5HT)1C and 5HT2 receptors display paradoxical down-regulation when exposed to receptor antagonists in vivo, a property that is unique to these two subtypes of serotonin (5HT) receptors. Because of the absence of cell culture model systems, the mechanisms involved in this paradoxical down-regulation have been difficult to explore. The present study focuses on the regulation of 5HT1C receptors in primary cultures of rat choroid plexus epithelial cells. Exposure of the epithelial cell cultures to 100 nM mianserin, a receptor antagonist, or (-)-1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane, an agonist, for 72 hr caused a loss of 5HT1C receptor binding sites, as determined by [3H]mesulergine binding to crude membrane preparations. No significant changes in Kd values were observed. Neither the agonist nor antagonist caused a significant change in binding sites after 24 hr. A solution hybridization assay was used to determine whether the down-regulation by mianserin or (-)-1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane was accompanied by a decrease in the steady state level of 5HT1C receptor mRNA. These studies showed that neither treatment caused an alteration in the levels of 5HT1C receptor mRNA. Thus, it is possible to reproduce the in vivo regulatory effects of drugs on 5HT1C receptors in choroid plexus epithelial cells in culture, including the atypical down-regulation by receptor antagonists. Using this cell culture model system, indirect transynaptic effects and decreases in receptor mRNA levels have been ruled out as mechanisms accounting for the down-regulation.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗