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PubMed2006

[The influence of temperature change on determined concentrations of dissolved organic matter in water].

The influence of temperature change on the determined concentrations of dissolved organic matter (DOM) in water was investigated by laser induced fluorescence (LIF) technique in laboratory. The temperature was altered within the range of 20 to 75 degrees C, and the intensity of DOM fluorescence and water Raman scattering were found to decrease with rising temperature. A linear fit of the normalized fluorescence intensity versus temperature yielded a mean value of the temperature coefficient of -5.24 x 10(-4) x degrees C(-1), and a mean value of the temperature coefficient of -3.42 x 10(-3)(mg x L(-1)) x degrees C(-1) was obtained according to the relationship between normalized fluorescence intensity and concentration of DOM. The temperature change will cause relative changes of up to 8.45% in DOM concentration within the range of 20 to 75 degrees C if we assume that the normalized fluorescence intensity remains the same.

English Abstract↗

PubMed1990

Effects of chronic domperidone treatment on rat conditioned avoidance behavior.

The effects of chronic administration of domperidone (DOM), a peripherally acting anti-emetic and hyperprolactinemic D2-dopaminoceptor antagonist, on active and inhibitory conditioned behavior were tested on male and female rats. DOM (4 mg/kg) was injected ip daily either for 5 or 30 days. Although treatment for 5 days failed to affect experimental parameters, treatment for 30 days impaired the performance of active conditioned avoidance of female, but not male, rats. This effect was no longer observed 7 days after ending treatment. No effects of DOM treatment were observed on active conditioned avoidance of male rats or on inhibitory conditioned behavior of all rats. These data suggest that female rats are more susceptible to the hyperprolactinemic effects of DOM than male rats. However, an influence of estrous cycle interruption cannot be rejected.

Animals↗

PubMed1998

[Effect of dietary selenium on the activity of UDP-glucuronosyltransferases and metabolism of mycotoxin deoxynivalenol in rats].

The influence of selenium excess and deficiency on the activity of xenobiotic metabolizing enzymes and the metabolism of mycotoxin deoxynivalenol (DON) in rats was studied. Wistar male rats were fed for 6 weeks semi-synthetic diets containing 0.2, 1.0 or 5.0 ppm selenium. For induction of selenium deficiency the weanling rats were fed for 6 weeks diet containing < or = 0.02 ppm selenium. The activity of selenium-dependent glutathione peroxidase was reduced in the liver of selenium-deficient rats by 93% at 42 days. DON, its de-epoxy metabolite DOM-1, DON and DOM-1 glucuronides were analyzed by reverse-phase HPLC in urine and feces after the single oral dose of DON (8 mg/kg). Selenium-supplemented (5 ppm) diet increased by 2-3 times formation and elimination of DON and DOM-1 glucuronides in urine. Selenium-deficient diet decreased formation of DOM-1, but increased significantly total excretion of DON and DON glucuronides. The activity of GT1 and GT2 forms of UDP-glucuronosyltransferase, an enzyme principally responsible for glucuronidation, was two times higher in the liver of rats fed both selenium-supplemented and selenium-deficient diets.

Administration, Oral↗

PubMed1990

5HT-2 mediation of acute behavioral effects of hallucinogens in rats.

In rats tested during their first exposure to a Behavioral Pattern Monitor chamber, acute injections of the 5HT-2 agonists mescaline, quipazine, 2,5-dimethoxy-4-iodoamphetamine (DOI), 2,5-dimethoxy-4-methylamphetamine (DOM), or 2,5-dimethoxy-4-ethylamphetamine (DOET) produced an inhibition of locomotor and investigatory behavior during the first 30 min of the test session. This suppression of exploratory behavior was attenuated when rats were familiarized with the testing chamber prior to the administration of DOI. Hence, as previously observed with both LSD and DOM, 5HT-2 agonists appear to potentiate the normal neophobic reaction to a novel environment. The mixed 5HT-1 and 5HT-2 agonist 5-methoxy-N,N-dimethyltryptamine (5MeODMT) also produced a decrease in activity when animals were tested in the novel environment. However, as previously found with 5HT-1A agonists, this effect was unchanged when animals were tested in the familiar environment and may therefore reflect a generalized sedation. The receptor specificity of these differential effects of 5HT-1 and 5HT-2 agonists in this paradigm was tested by assessing the ability of selective 5HT-2 antagonists to block the effects of the agonists. A dose of the 5HT-2 antagonist ketanserin which had no effect by itself significantly reduced the behavioral effects of mescaline, DOM, and quipazine. Similarly, the selective 5HT-2 antagonist ritanserin blocked the effect of quipazine. In contrast, ketanserin had no significant effect on the suppression of activity produced by the 5HT-1A agonist 8-hydroxy-2(di-n-propylamino)tetralin (8OHDPAT).(ABSTRACT TRUNCATED AT 250 WORDS)

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1995

5-HT2C receptor-mediated phosphoinositide turnover and the stimulus effects of m-chlorophenylpiperazine.

The present study was designed to investigate the hypothesis that agonist interactions at 5-HT2C receptors mediate the discriminative stimulus properties of m-chlorophenylpiperazine (mCPP). Three structural classes of compounds have been described to stimulate increases in phosphoinositide (PI) hydrolysis at the 5-HT2C receptor site: phenylpiperazines, phenylalkylamines, and indolamines. Four representative phenylpiperazines, mCPP, TFMPP, MK-212 and quipazine, one phenylalkylamine, (-)DOM, and one indolamine, LSD, were employed in the present study. The efficacies of these compounds were defined (1) in vitro, with respect to their abilities to stimulate increases in PI hydrolysis in the choroid plexus, and (2) in vivo with respect to their abilities to substitute for the mCPP discriminative stimulus. In vitro intrinsic activity at the 5-HT2C site was expressed as a fraction of the maximal PI hydrolysis response elicited by serotonin (5-HT). MK-212 (fractional efficacy = 1.1) and (-)DOM (0.77) were full agonists, while mCPP (0.72), LSD (0.27), quipazine (0.24), and TFMPP (0.22) were partial agonists with respect to the stimulation of PI hydrolysis at the 5-HT2C receptor. In vivo, each of the phenylpiperazines fully substituted for the mCPP stimulus, while (-)DOM (75%), and LSD (67%) elicited only partial substitution. While compounds with agonist activity at the 5-HT2C receptor in vitro substitute for the mCPP stimulus in vivo, no clear relationship exists between in vitro intrinsic activity at the 5-HT2C receptor with respect to the stimulation of PI turnover and maximal substitution for the mCPP stimulus in vivo. The present data suggest that mCPP elicits a compound stimulus which is mediated by agonist interactions at the 5-HT2C receptor and possibly additional interactions with 5-HT2A, 5-HT3, and/or 5-HT1B receptors.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1983

Indolealkylamine and phenalkylamine hallucinogens. Effect of alpha-methyl and N-methyl substituents on behavioral activity.

Animals (rats), trained to discriminate the hallucinogenic agent 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline in a two-lever operant procedure, were challenged with various doses of several indolealkylamine and phenalkylamine derivatives. In both series, the alpha-methyl analogs were found to be more active than either their N-methyl or alpha-demethyl counterparts. Furthermore, when the activities of the optical isomers of DOM were compared with the activities of S-(+) and R-(-)-alpha-methyltryptamine (alpha-MeT), it was found that the more potent isomer of alpha-MeT (i.e. S) possessed the opposite absolute configuration of the more potent isomer of DOM (i.e. R). With respect to the mechanism of action of these agents, these findings are not inconsistent with a common site hypothesis.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1987

Stereochemical effects of 3,4-methylenedioxymethamphetamine (MDMA) and related amphetamine derivatives on inhibition of uptake of [3H]monoamines into synaptosomes from different regions of rat brain.

3,4-Methylenedioxymethamphetamine (MDMA) is a recently popularized recreational drug, although some have advocated its psychotherapeutic potential. Since the pharmacology of MDMA is largely uncharacterized, the stereochemical profiles of MDMA and some of its homologs were derived on inhibition of synaptosomal uptake of [3H]monoamines and compared to those of amphetamine and the hallucinogenic phenylisopropylamine 2,5-dimethoxy-4-methylamphetamine (DOM). In contrast to the 5-fold stereoselectivity observed with amphetamine, only the S-(+) enantiomer of MDMA and 3,4-methylenedioxyamphetamine (MDA) inhibited [3H]dopamine uptake into striatal synaptosomes. Neither stereoisomer of the alpha-ethyl homolog of MDMA, N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), inhibited [3H]dopamine uptake. The two stereoisomers of amphetamine and the MDMA-related compounds were equipotent in inhibiting [3H]norepinephrine uptake into hypothalamic synaptosomes. Both stereoisomers of MDMA, MDA and MBDB were potent inhibitors of [3H]serotonin uptake into hippocampal synaptosomes, but only S-(+)-amphetamine produced an appreciable inhibition of [3H]serotonin uptake. Neither stereoisomer of DOM inhibited synaptosomal uptake of any [3H]monoamine. These results suggest that MDMA and its homologs may be more closely related to amphetamine rather than to DOM in their biochemical mode of action. The pronounced effects of the methylenedioxy-substituted compounds on [3H]serotonin and [3H]norepinephrine uptake implicate these neurotransmitters in the pharmacological effects of these drugs.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1986

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

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 pressure changes; i.v. D-amphetamine produced inconsistent responses. These results suggest that most of the effects seen on i.v. administration of phenethylamines are not mediated directly on the serotonergic cell.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1984

MDA: a psychoactive agent with dual stimulus effects.

Rats were trained to discriminate injections of either (+)-amphetamine (1.0 mg/kg) or racemic MDA (1.5 mg/kg) from saline in a two-lever drug discrimination task. After stable discrimination performances (greater than 85%) were attained in each group, stimulus generalization studies were conducted. The amphetamine-stimulus generalized to MDA, but not to the hallucinogenic agent DOM; the MDA-stimulus generalized to both amphetamine and DOM. Taken together with our previous finding that DOM-stimulus generalization occurs to MDA but not to amphetamine, the present study suggests that MDA is capable of producing dual stimulus effects in animals. In addition to these salient features, the results of this study also have an impact on stimulus specificity, and further emphasize the importance of thorough dose-response relationships as related to tests of stimulus generalization.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1990

Rapid desensitization and resensitization of 5-HT2 receptor mediated phosphatidyl inositol hydrolysis by serotonin agonists in quiescent calf aortic smooth muscle cells.

Agonist regulation of 5-hydroxytryptamine2 (5-HT2) receptors was studied in calf aortic smooth muscle cultures incubated in a quiescent, defined synthetic medium that does not stimulate cell proliferation, but that provides cells with supplements that maintain cell viability. In these cells, 5-hydroxytryptamine (5-HT)-induced [3H]inositol phosphates accumulation showed the characteristics of a 5-HT2 receptor coupled transducing system according to the inhibition of the response by 5-HT2 antagonists at nanomolar concentrations. The 5-HT2 receptor coupled response became rapidly desensitized during continued incubation with 5-HT and 1-(2,5-dimethoxy-4-methylphenyl)-2- aminopropane (DOM); nearly full desensitization was obtained in two hours with 10 microM 5-HT and DOM pretreatment. The recovery of the response had a half-live of 5 hours after 2 hours pretreatment and of 9.5 to 12.5 hours after 24 to 96 hours agonist pretreatment. The DOM-induced desensitization of the 5-HT2 receptor coupled response was fully blocked by 0.1 microM cinanserin. Cinanserin alone did not induce desensitization or up-regulation of the 5-HT2 receptor coupled response at 0.1 microM. It may be that the down-regulation of central 5-HT2 receptors by antagonists in vivo is a heterologous process due to mediators which are triggered by 5-HT2 antagonistic action.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1988

Stimulus properties of 1-(3,4-methylenedioxyphenyl)-2-aminopropane (MDA) analogs.

Using a standard two-lever operant procedure, groups of rats were trained to discriminate intraperitoneal doses of the phenylisopropylamines (+)amphetamine (1.0 mg/kg) or racemic 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM; 1.0 mg/kg) from saline using a VI 15-sec schedule of reinforcement for food reward. Once trained, the animals were administered doses of several methylenedioxy analogs (MDAs) of phenylisopropylamine including the N-monomethyl [S(+)MDMA and R(-)MDMA], N-monoethyl [(+/-)MDE, S(+)MDE, and R(-)MDE], and the N-hydroxyl [(+/-)N-OH MDA] derivatives. The DOM-stimulus did not generalize to any of these agents. The amphetamine-stimulus generalized to S(+)MDMA, S(+)N-ethylamphetamine and (+/-)N-hydroxyamphetamine, but not to R(-)MDMA, (+/-)MDE, S(+)MDE, R(-)MDE, or N-OH MDA. The present results are consistent with other reports in the literature suggesting that the psychoactive effects of certain MDA derivatives may be other than simply amphetamine- or DOM-like.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1988

A preliminary investigation of the psychoactive agent 4-bromo-2,5-dimethoxyphenethylamine: a potential drug of abuse.

4-Bromo-2,5-dimethoxyphenethylamine (alpha-desMe DOB) is a psychoactive agent that may possess significant abuse potential. Because of its structural similarity to the established hallucinogen 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB), and because almost no pharmacological data are available on this agent, we undertook this preliminary investigation. alpha-DesMe DOB (Ki = 1 nM), like DOB itself (Ki = 0.79 nM), displays a high affinity for [3H]DOB-labeled central 5-HT2 serotonin receptors. However, unlike DOB, the alpha-desmethyl derivative also binds with significant affinity to 5-HT1A, 5-HT1B, and 5-HT1C serotonin receptors and, as such, is less selective than DOB. In drug discrimination studies using rats trained to discriminate either DOM (i.e., the 4-methyl analog of DOB) or R(-)DOB from saline, stimulus generalization occurred in both groups of animals. However, stimulus generalization was associated with extensive disruption of behavior, alpha-DesMe DOB may produce stimulus effects similar, but not identical, to those of DOM and R(-)DOB; in addition, this agent may be capable of producing other, as yet undefined, central effects at comparable doses. These other effects may be reflective of the lack of selectivity of alpha-desMe DOB for 5-HT2 serotonin receptors. Because other hallucinogenic agents display high affinity for 5-HT2 serotonin receptors and result in stimulus generalization in DOM- and/or DOB-trained animals, it is tentatively concluded that alpha-desMe DOB is a psychoactive agent with at least some hallucinogenic or DOB-like properties.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1986

Discriminative stimulus properties of phenylisopropylamine derivatives.

The phenylisopropylamine unit is a common structural fragment amongst many centrally-acting agents. However, these agents do not necessarily produce similar behavioral effects in test subjects. For example, the phenylisopropylamine derivative amphetamine is a central nervous system (CNS) stimulant whereas its 2,5-dimethoxy-4-methyl analog, i.e. DOM, is considered to be a hallucinogen. Employing animals trained to discriminate either (+)-amphetamine or (+/-)-DOM from saline in a two-lever operant procedure, stimulus generalization studies were conducted to evaluate members of a series of methoxy-substituted, and related, phenylisopropylamines. In this manner, it was possible to classify these agents as to which produced amphetamine-like effects, and which produced DOM-like effects.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed2004

Stimulus effects of three sulfur-containing psychoactive agents.

Two agents gaining popularity on the illicit drug market are the phenylalkylamines 4-MTA and 2C-T-7 [or 1-(4-methylthiophenyl)-2-aminopropane and 2-(2,5-dimethoxy-4-n-propylthiophenyl)-1-aminoethane, respectively]. At this time, there exists a paucity of information on the behavioral actions of these sulfur-containing agents. The present investigation examined these agents, and the N-monomethyl analog of 4-MTA (i.e., 4-MTMA), in tests of stimulus generalization (substitution) using a two-lever drug discrimination task with groups of rats trained to discriminate either the hallucinogen DOM [1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane], the stimulant cocaine, or the empathogen MDMA from vehicle. 4-MTA and its N-monomethyl analog 4-MTMA (ED50 = 0.8 mg/kg in both cases) substituted only for the MDMA stimulus, whereas 2C-T-7 (ED50 = 0.8 mg/kg) substituted only for the DOM stimulus. Thus, at the doses examined, 4-MTA and 4-MTMA appear to be MDMA-like agents, and 2C-T-7 seems best classified as a DOM-like hallucinogen. These results provide additional data that extend the structure-activity relationships of phenylalkylamines and that are consistent with what little is currently known about the action of 4-MTA and 2C-T-7 in humans.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed2000

Antagonism of a PCP drug discrimination by hallucinogens and related drugs.

Drugs such as PCP and MK-801 can cause psychotic reactions in humans by antagonizing NMDA receptors. This action is ultimately toxic to certain cortical neurons and may be one mechanism underlying neurodegenerative diseases, including schizophrenia. It has been reported that hallucinogens such as LSD, DOM, and DOI can block the neurotoxic effects of NMDA antagonists, possibly by activating inhibitory 5-HT2A receptors on GABAergic interneurons that normally inhibit glutamatergic projections to the retrosplenial and cingulate cortexes. The purpose of this experiment was to determine the extent to which similar drugs might also alter the behavioral effects of one NMDA antagonist, PCP. Rats were trained to discriminate this compound (2.5 mg/kg) from saline and were then given a series of antagonist tests. It was found that LSD (0.32 mg/kg) and DOM (4.0 mg/kg) blocked the PCP cue completely; DMT (8.0 mg/kg) and a structural congener of LSD, lisuride (LHM; 0.4 mg/kg), blocked the effects of PCP partially. The 5-HT/DA antagonists spiperone and ritanserin had no effect on the PCP cue. These data suggest that LSD, DOM, and, less effectively, DMT and LHM can block the behavioral as well as the neurotoxic effects of NMDA antagonists most likely through agonist actions at 5-HT2 receptors.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1986

5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.

Arylpiperazines, such as 1-(3-trifluoromethylphenyl)piperazine (TFMPP) and its chloro analogue mCPP, are 5-HT1 agonists, whereas quipazine, i.e., 2-(1-piperazino)quinoline, appears to be a 5-HT2 agonist. Radioligand binding studies using rat cortical membrane homogenates and drug discrimination studies using rats trained to discriminate a 5-HT1 agonist (i.e., TFMPP) or a 5-HT2 agonist (i.e., 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM)) from saline reveal that quipazine and its 1-deaza analogue 2-naphthylpiperazine (2-NP) bind at 5-HT1 and 5-HT2 sites but produce stimulus effects similar to those of DOM. A structurally related compound, 1-naphthylpiperazine (1-NP), possesses a high affinity for 5-HT1 (Ki = 5 nM) and 5-HT2 (Ki = 18 nM) sites. 1-NP produces stimulus effects similar to those of TFMPP and is able to antagonize the stimulus effects produced by DOM. The present results suggest that the unsubstituted benzene ring of quipazine, and of its 1-deaza analogue 2-naphthylpiperazine, makes a significant contribution to the binding of these agents to 5-HT2 sites and, more importantly, may account for their 5-HT2 agonist properties.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1980

Conformational energy differences between side chain alkylated analogues of the hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane.

Theoretical conformational energy calculations were carried out for the (+) and (-) isomers of the hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM, STP). Energies were also calculated for two analogues of DOM, 1-amino-1-(2,5-dimethoxy-4-methylbenzyl)cyclopropane and 1-(2,5-dimethoxy-4-methylphenyl)-2-methyl-2-aminopropane. This method utilized classical, empirical potential-energy functions. A previously proposed active conformational region was studied. Compounds could be ranked in order of potency based on relative conformational energies in this region. Measurement of 13C spin--lattice relaxation times (T1) for the two alpha, alpha-disubstituted DOM analogues confirmed theoretical predictions of very restricted conformational freedom for the dimethyl compound but more flexibility for the cyclopropane analogue.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1982

Behavioral and serotonin receptor properties of 4-substituted derivatives of the hallucinogen 1-(2,5-dimethoxyphenyl)-2-aminopropane.

The serotonin (5-HT) receptor affinities and behavioral (discriminative stimulus) properties of a series of 4-substituted derivatives of 1-(2,5-dimethoxyphenyl)-2-aminopropanes (2,5-DMA) were investigated. The substituents at the 4-position included H, OMe, OEt, Me, Et, F, Br, I, and NO2. Substituent lipophilicities (pi values) of these functionalities appear to have a minimal effect on either 5-HT receptor affinity or behavioral activity. Those derivatives previously found to be most potent in human studies possess significant affinity for 5-HT receptors. Furthermore, when rats trained to discriminate (+/-)-1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline were used, generalization was found to occur upon administration of the 4-substituted 2,5-DMA derivatives. Because a direct relationship exists between the ED50 values obtained from these discrimination studies and human hallucinogenic potencies, the discriminative stimulus paradigm, with DOM as a training drug, appears to be a useful tool for comparing the quantitative and qualitative (DOM-like) effects produced by certain hallucinogenic agents.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗