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PubMedDate not supplied

Validation of a simple liquid chromatographic method for determination and quantitation of residual ivermectin and doramectin in pig liver.

A rapid and quantitative method for the extraction, derivatization, and liquid chromatography with fluorescence detection of ivermectin (IVM) and doramectin (DOM) residues in porcine liver was developed and validated. IVM and DOM were extracted from the liver samples with acetonitrile, the supernatant was evaporated to dryness at 37 degrees C under nitrogen, and the residue was reconstituted in 1-methylimidazole solution. After 2 min at room temperature, IVM and DOM were converted to a fluorescent derivative and then separated on a Hypersil ODS column. The derivatives of IVM and DOM were detected and quantitated with high specificity by fluorescence (excitation: 365 nm, emission: 475 nm). Abamectin was used as an internal standard. The mean extraction efficiencies from fortified samples (15 ng/g) were 75% for IVM and 70% for DOM. The limit of detection was 0.8 ng/g for both IVM and DOM.

Animals↗

PubMed2003

[Characteristics and environmental significance of soil dissolved organic matter].

Soil is a complex ecosystem with multi-interface. A numerous studies on soil dissolved organic matter (DOM) were carried out, and proved that DOM was one of the most active chemical components in the environment. Increasing attention has been paid on the study of soil DOM, especially in recent years, and the study has become an interdisciplinary focus in the fields of soil science, ecology, and environmental science due to the important roles of DOM in the biogeochemical cycles of carbon, nitrogen, phosphorus, sulfur, etc. In addition, DOM has significant effects on pedogenesis, growth and metabolism of soil microorganisms, decomposition and transformation of soil organic matter, and transport of pollutants in soils. The recent literatures about extraction methods, origin, composition, contents and controlling factors, bioavailability, and environmental significance of DOM were therefore reviewed, and future research aspects on this topic were also proposed.

Environmental Monitoring↗

PubMed2004

[Influence of dissolved organic matter on the eco-toxicity of phenanthrene in a soil].

Biological and physico-chemistry experiments were conducted to study the effects of dissolved organic matter (DOM) on eco-toxicity of phenanthrene in a soil. The results showed that DOM was a kind of surfactant. The sensitive range of phe inhibiting wheat root elongation was from 0 to 200 mg/kg, and median inhibition concentration (IC50) was 200 mg/kg. In the presence of DOM, the eco-toxicity of phe could be alleviated and the inhabited degree was related to the content of hydrophobic components and surface activity. This effect could be strengthened by the high concentration of DOM. As a kind of hydrophobic organic compound, phe could reduce the moisture of topsoil, and DOM would slightly increase the moisture of topsoil polluted by phe. It was concluded that DOM could lighten the eco-toxicity of phe in soil.

Ecosystem↗

PubMed2004

[Three-dimensional excitation emission matrix fluorescence spectroscopic characterization of the complexation between mercury (II) and dissolved organic matter].

With the development of fluorescence technique, three-dimensional excitation emission matrix fluorescence spectroscopy (3DEEM) was widely applied to characterize the nature of dissolved organic matter (DOM) in natural waters since the last decade. 3DEEM and fluorescence quenching titration were used to study the interaction between Hg(II) and DOM. The results show that a general decrease in intensity for individual peak A, B and C was found as concentrations of Hg(II) increased. pH is the main parameter that strongly influences the Hg(II)-DOM complexation. The addition of Cl- ion to the Hg(II)-DOM system caused an increase in fluorescence intensity. The results also show that the addition of Ca(II) solution strongly enhanced the fluorescence intensity for humic-like fluorescence, while the protein-like fluorescence only slightly enhanced. On the contrary, no fluorescence enhancement was found in the Hg(II)-DOM system after the addition of Mg(II) ion. A decrease in fluorescence emission intensity was found after the addition of Cu(II) ion to the Hg(II)-DOM solution.

Drug Interactions↗

PubMedDate not supplied

Effects of massage on delayed-onset muscle soreness, swelling, and recovery of muscle function.

CONTEXT: Delayed-onset muscle soreness (DOMS) describes muscle pain and tenderness that typically develop several hours postexercise and consist of predominantly eccentric muscle actions, especially if the exercise is unfamiliar. Although DOMS is likely a symptom of eccentric-exercise-induced muscle damage, it does not necessarily reflect muscle damage. Some prophylactic or therapeutic modalities may be effective only for alleviating DOMS, whereas others may enhance recovery of muscle function without affecting DOMS. OBJECTIVE: To test the hypothesis that massage applied after eccentric exercise would effectively alleviate DOMS without affecting muscle function. DESIGN: We used an arm-to-arm comparison model with 2 independent variables (control and massage) and 6 dependent variables (maximal isometric and isokinetic voluntary strength, range of motion, upper arm circumference, plasma creatine kinase activity, and muscle soreness). A 2-way repeated-measures analysis of variance and paired t tests were used to examine differences in changes of the dependent variable over time (before, immediately and 30 minutes after exercise, and 1, 2, 3, 4, 7, 10, and 14 days postexercise) between control and massage conditions. SETTING: University laboratory. PATIENTS OR OTHER PARTICIPANTS: Ten healthy subjects (5 men and 5 women) with no history of upper arm injury and no experience in resistance training. INTERVENTION(S): Subjects performed 10 sets of 6 maximal isokinetic (90 degrees x s(-1)) eccentric actions of the elbow flexors with each arm on a dynamometer, separated by 2 weeks. One arm received 10 minutes of massage 3 hours after eccentric exercise; the contralateral arm received no treatment. MAIN OUTCOME MEASURE(S): Maximal voluntary isometric and isokinetic elbow flexor strength, range of motion, upper arm circumference, plasma creatine kinase activity, and muscle soreness. RESULTS: Delayed-onset muscle soreness was significantly less for the massage condition for peak soreness in extending the elbow joint and palpating the brachioradialis muscle (P < .05). Soreness while flexing the elbow joint (P = .07) and palpating the brachialis muscle (P = .06) was also less with massage. Massage treatment had significant effects on plasma creatine kinase activity, with a significantly lower peak value at 4 days postexercise (P < .05), and upper arm circumference, with a significantly smaller increase than the control at 3 and 4 days postexercise (P < .05). However, no significant effects of massage on recovery of muscle strength and ROM were evident. CONCLUSIONS: Massage was effective in alleviating DOMS by approximately 30% and reducing swelling, but it had no effects on muscle function.

Journal Article↗

PubMedDate not supplied

Dehydration and symptoms of delayed-onset muscle soreness in hyperthermic males.

CONTEXT: Exercise in the heat produces cellular conditions that may leave skeletal muscle susceptible to exercise-induced microdamage. Delayed-onset muscle soreness (DOMS) is a clinical model of contraction-induced skeletal muscle injury. OBJECTIVE: To determine whether thermoregulation during exercise heat stress adversely affects muscle injury and the accompanying DOMS. DESIGN: Randomized group test-retest design. SETTING: Laboratory. PATIENTS OR OTHER PARTICIPANTS: Ten healthy male volunteers were randomly assigned to either the euhydration/hyperthermic or dehydration/hyperthermic group. INTERVENTION(S): Participants were randomly assigned to treadmill walking in a hot, humid environmental chamber (40 degrees C and 75% relative humidity) with either oral rehydration (euhydration/hyperthermic) or fluid restriction (dehydration/hyperthermic). Immediately after heat exposure and while hyperthermic, participants performed an eccentrically biased downhill run to induce DOMS. MAIN OUTCOME MEASURE(S): We measured DOMS characteristics pre-exercise and at 0.5, 24, 48, 72, and 96 hours postexercise. RESULTS: Treadmill exercise and exposure to the hot ambient environment elicited a 0.9% body mass loss for the euhydrated/ hyperthermic (mean rectal temperature after 60 minutes of heat-stress trial = 38.2 +/- 0.4 degrees C) and 3.3% body mass loss for the dehydrated/hyperthermic participants (mean rectal temperature after 60 minutes of heat-stress trial = 38.1 +/- 0.4 degrees C). Quadriceps perceived pain was significantly higher (F(5,40) = 18.717, P <or= .001) than baseline at 24 and 48 hours postexercise, following the classic pattern of DOMS. Overall lower extremity perceived pain was significantly higher for the dehydration/hyperthermia group than the euhydration/hyperthermia group (F(1,8) = 6.713, P = .032). Punctate tenderness of the vastus lateralis for the dehydration/hyperthermic group was 6.9% higher (F(5,40) = 4.462, P = .003) than for the euhydration/ hyperthermic group. No clinically important findings were revealed for passive range of motion for knee flexion. For both groups, quadriceps isometric strength (F(5,40) = 12.924, P <or= .001) was 17.5% and 20.0% lower at 0.5 hours postexercise than at 72 and 96 hours postexercise, respectively. Further, quadriceps isometric strength remained 10.5% reduced at 24 hours postexercise compared with 96 hours postexercise. CONCLUSIONS: Skeletal muscle microdamage, indirectly evidenced by DOMS, was exacerbated in hyperthermic participants dehydrated by exercise in a hot ambient environment. Individuals performing novel exercise, particularly with a significant eccentric component, should use caution when training in a hot, humid environment and implement frequent rest and rehydration breaks.

Journal Article↗

PubMed1992

Effect of transcutaneous electrical nerve stimulation, cold, and a combination treatment on pain, decreased range of motion, and strength loss associated with delayed onset muscle soreness.

Athletic trainers have a variety of therapeutic agents at their disposal to treat musculoskeletal pain, but little objective evidence exists of the efficacy of the modalities they use. In this study, delayed onset muscle soreness (DOMS) served as a model for musculoskeletal injury in order to: (1) compare the changes in perceived pain, elbow extension range of motion, and strength loss in subjects experiencing DOMS in the elbow flexor muscle group following a single treatment with either transcutaneous electrical nerve stimulation (TENS), cold, a combination of TENS and cold, sham TENS, or 20 minutes of rest; (2) compare the effects of combining static stretching with these treatments; and (3) determine if decreased pain is accompanied by a restoration of strength. DOMS was induced in the non-dominant elbow flexor muscle group in 40 females (age = 22.0 +/- 4.3 yr) with repeated eccentric contractions. Forty-eight hours following exercise, all subjects presented with pain, decreased elbow extension range of motion, and decreased strength consistent with DOMS. Subjects were randomly assigned to 20-minute treatments followed by static stretching. Cold, TENS, and the combined treatment resulted in significant decreases in perceived pain. Treatments with cold resulted in a significant increase in elbow extension range of motion. Static stretching also significantly reduced perceived pain. Only small, nonsignificant changes in muscle strength were observed following treatment or stretching, regardless of the treatment group. These results suggest that the muscle weakness associated with DOMS is not the result of inhibition caused by pain. The results suggest that these modalities are effective in treating the pain and muscle spasm associated with DOMS, and that decreased pain may not be an accurate indicator of the recovery of muscle strength.

Journal Article↗

PubMedDate not supplied

Dehydration and symptoms of delayed-onset muscle soreness in normothermic men.

CONTEXT: A dehydrated individual who performs eccentric exercise may exacerbate skeletal muscle damage, leading to structural, contractile, and enzymatic protein denaturation, in addition to the myofiber and connective damage resulting from the eccentric muscle tension. OBJECTIVE: To identify the effects of dehydration on 5 physiologic characteristics of delayed-onset muscle soreness (DOMS) in normothermic men after an eccentric exercise perturbation. DESIGN: Randomized group test-retest design. SETTING: Laboratory. PATIENTS OR OTHER PARTICIPANTS: Ten healthy male volunteers randomly assigned to either a euhydration (age = 26.2 +/- 4.9 years, height = 174.1 +/- 6.0 cm, mass = 86.5 +/- 15.3 kg) or dehydration (age = 25.8 +/- 2.2 years, height = 177.2 +/- 3.1 cm, mass = 84.4 +/- 3.8 kg) group. INTERVENTION(S): Subjects performed treadmill walking for 45 minutes in either a thermoneutral (euhydration) or a hot, humid (dehydration) environment. After a rest period to allow for return to the normothermic condition, DOMS was induced with a 45-minute downhill run. MAIN OUTCOME MEASURES: We assessed 5 physiologic characteristics of DOMS before and at intervals after the eccentric exercise. The characteristics were perceived pain of the bilateral quadriceps and overall body, bilateral punctate tenderness of the superficial quadriceps muscles, bilateral knee-flexion passive range of motion, bilateral thigh circumference, and bilateral isometric quadriceps muscle strength. Thermoregulatory and cardiovascular measures were obtained to monitor participants' heat load during exercise. RESULTS: The experimental protocol produced a 0.9% increase in body mass of the euhydration group and a significant 2.7% decrease in body mass of the dehydration group. The downhill-running exercise perturbation induced DOMS in both the euhydrated and dehydrated participants, based on increased bilateral quadriceps and overall body perceived pain and punctate tenderness of the bilateral vastus medialis muscle. The signs and symptoms of DOMS after an eccentric exercise perturbation were not exacerbated by moderate dehydration of 2.7% body mass after rest and return to the normothermic condition. CONCLUSIONS: Significantly dehydrated participants who rested and returned to a normothermic condition did not experience increased characteristics of DOMS.

Journal Article↗

PubMed2006

[Effect of sunlight irradiation on fluorescence properties of dissolved organic matter].

Three-dimensional excitation emission matrix fluorescence spectroscopy (3DEEM) was used to investigate the effect of sunlight irradiation on the fluorescence properties of dissolved organic matter (DOM) from Lake Hongfeng and Nanming River waters and a commercial fluka humic acid (FHA). The results show that the DOM samples and FHA fluorescence properties changed under sunlight irradiation. Interestingly, the photodegradation characteristics were different between aquatic DOM and FHA. The fluorescence intensity of the apparent peaks A, B and C of lake and river water DOM decreased with sunlight irradiation. The initial 3DEEM of Fluka HA had only one fluorescence peak at lamda ex / lamda em = 275/500 nm, while two fluorescence peaks occurred at lamda ex / lamda em = 245/450 nm and 310/450 nm, respectively, after sunlight irradiation. lamda ex and lamda maxima of DOM decreased during 7 days of sunlight irradiation. Changes in r(A, C) of DOM and FHA with sunlight irradiation time suggest that fluorescence peaks A and C had different fluorescence loss rates, while peak C fluorophores were more susceptible to sunlight irradiation. FHA appeared to be less susceptible to photodegradation, and its r(A, C) remained almost the same before and after sunlight irradiation.

English Abstract↗

PubMed1990

Serotonin excitation of facial motoneurons: receptor subtype characterization.

The receptor subtype(s) mediating the enhancement of facial motoneuron excitability by serotonin (5-HT) was evaluated by means of single-cell recording in vivo (in the anesthetized rat) and in vitro in brain slices. In vivo, microiontophoretic application of the broad-spectrum 5-HT1 agonist 5-carboxamidotryptamine (5-CT), the 5-HT2/5-HT1C agonist 1-[2,5-dimethoxy-4-methylphenyl]-2-aminopropane (DOM), but not the selective 5-HT1A agonist 8-OH-2[di-n-propylamino]tetralin (8-OH-DPAT), produced a 5-HT-like enhancement of facial motoneuron excitability. Intravenous administration of the 5-HT2/5-HT1C antagonists ritanserin and LY 53857 in vivo blocked the facilitatory effects of 5-HT and DOM, but not norepinephrine (NE). Similarly, in brain slices, bath application of ritanserin blocked the effects of 5-HT, DOM, and 5-CT, but not NE on facial motoneurons. Intracellular recordings showed that DOM induced a slow depolarization and an increase in evoked spikes, but these effects were of lesser magnitude and longer duration than those produced by 5-HT. Taken together, these results indicate a role for 5-HT2 and/or 5-HT1C but not 5-HT1A receptors in serotonergic enhancement of facial motoneuron excitability since 5-HT's effect was 1) at least partially mimicked by the selective 5-HT2/5-HT1C agonist DOM, 2) mimicked by the broad-spectrum 5-HT1 agonist 5-CT but not the selective 5-HT1A agonist 8-OH-DPAT, and 3) blocked by the 5-HT2/5-HT1C antagonists ritanserin and LY 53857.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1995

The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis.

Investigations conducted over the past 3 decades have demonstrated that serotonergic receptors, specifically the 5-HT2A and 5-HT2C subtypes, play an important role in the behavioral effects of hallucinogenic compounds. The present study was designed to determine the respective significance of these two receptors in the stimulus effects of LSD and (-)DOM in the rat. Specifically, the interactions of a series of serotonergic antagonists (risperidone, pirenpirone, metergoline, ketanserin, loxapine, LY53857, pizotyline, spiperone, cyprohepatadine, mesulergine, promethazine, and thioridazine) with the LSD stimulus and the (-)DOM stimulus in LSD-trained subjects was defined. From these data, IC50 values were determined for the inhibition of the LSD-appropriate responding elicited by either 0.1 mg/kg LSD (15-min pretreatment time) or 0.4 mg/kg (-)DOM (75-min pretreatment). In addition, the affinities of these antagonists for 5-HT2A and 5-HT2C receptors were determined in radioligand competition studies, 5-HT2A affinity correlated significantly with IC50 values for the blockade of the LSD (r = +0.75, P < 0.05) and (-)DOM (r = +0.95, P < 0.001) stimuli in the LSD trained subjects. 5-HT2C affinity did not correlate significantly with either series of IC50 values. These data indicate that (1) the stimulus effects of LSD, and (2) the substitution of (-)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1990

Receptor mechanisms for 5-hydroxytryptamine (5-HT) in isolated ovine umbilical vein.

5-Hydroxytryptamine (5-HT) and 2,5-dimethoxy-4-methyl-amphetamine (DOM) produced a concentration-dependent contraction in isolated umbilical veins obtained from fetal lambs within 2 weeks of term. Contractions to 5-HT were antagonized by ketanserin, mianserin and methiothepin with the dissociation constants (KB) being 2.17 +/- 0.36, 1.37 +/- 0.55 and 1.98 +/- 0.48 nM, respectively. The order of potency of serotonergic agonists in this tissue was: DOM greater than 5-HT greater than alpha-methyl-5-HT greater than 1(3-chlorophenyl) piperazine (mCPP) greater than m-trifluoromethyl-phenylpiperazine (TFMPP) greater than 8-hydroxy-dipropylaminotetralin (8-OH-DPAT) = 2-methyl-5-HT. alpha-Methyl-5-HT was a full agonist compared to 5-HT. DOM possessed greater affinity but less efficacy than that of 5-HT. The affinities and efficacies of the other agonists studied were lower than those of 5-HT. Variation in the sensitivity and potency of agonists is primarily due to variations in their affinity for 5-HT receptors. Assessment of receptor occupancy vs. functional response demonstrated very little, if any, receptor reserve for 5-HT receptors in this tissue. Contractile responses to DOM, 8-OH-DPAT, mCPP and 2-methyl-5-HT were effectively blocked by ketanserin. The dissociation constants (KB) of ketanserin against these agonists were as follows: DOM, 2.78 +/- 0.85 nM; 8-OH-DPAT, 3.47 +/- 1.12 nM; mCPP, 1.45 +/- 0.51 nM; 2-methyl-5-HT, 1.99 +/- 0.74 nM. The dissociation constant of MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) vs. 5-HT was 13833 nM. No antagonism by prazosin (10(-7) M) or yohimbine (10(-7) M) of the responses to 5-HT was observed. These results indicate that 5-HT2 receptors are present in the ovine umbilical vein. 5-HT3 receptors were not present in this tissue. Activation of alpha-adrenoceptors was not involved in the contractions to 5-HT.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMedDate not supplied

PMMA-stimulus generalization to the optical isomers of MBDB and 3,4-DMA.

Psychoactive phenylisopropylamines can produce one or more of several different stimulus effects in animals. These effects are typified by the hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM), the central stimulant amphetamine, and by N-methyl-1-(4-methoxyphenyl)-2-aminopropane (PMMA), an agent whose actions are not yet well understood. The optical isomers of two phenylisopropylamines known to lack DOM and amphetamine-stimulus character, that is N-methyl-1-(3,4-methylenedioxyphenyl)-2-aminobutane (MBDB) and 1-(3,4-dimethoxyphenyl)-2-aminopropane (3,4-DMA), were examined in rats trained to discriminate 1.25 mg/kg of PMMA from vehicle. The PMMA stimulus (ED(50)=0.4 mg/kg) generalized to all four agents: S(+)-MBDB (ED(50)=0.8 mg/kg), R(-)-MBDB (ED(50)=2.0 mg/kg), S(+)-3,4-DMA (ED(50)=2.6 mg/kg) and R(-)-3,4-DMA (ED(50)=3.9 mg/kg). The results show that these agents produce stimulus effects similar to those produced by PMMA. Both isomers of MBDB have been previously demonstrated to substitute for N-methyl-1-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) in rats trained to discriminate MDMA from vehicle, but MBDB-trained animals failed to recognize DOM or amphetamine. Similar results were obtained with the 3,4-DMA optical isomers in the present investigation using rats trained to discriminate MDMA, DOM or (+)-amphetamine from vehicle; both isomers of 3,4-DMA substituted for an MDMA stimulus, but not for a DOM or amphetamine stimulus. Taken together, the evidence suggests that PMMA, S(+)-MBDB, R(-)-MBDB, S(+)-3,4-DMA, R(-)-3,4-DMA, and S(+)-MDMA can produce common stimulus effects in rats. The present findings also better define the PMMA stimulus and the structural requirements necessary to produce this type of stimulus effect.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMedDate not supplied

A sensitive method for determining levels of [-]-2,5,-dimethoxy-4-methylamphetamine in the brain tissue.

INTRODUCTION: Indolamine and phenethylamine hallucinogens are drugs of abuse and, as well, mimic some aspects of idiopathic psychosis. To assist in investigating the mechanisms of action of (-)2,5-dimethoxy4-methylamphetamine ([-]-DOM), a member of the phenethylamine class of serotonergic hallucinogens, a sensitive and precise method for determining its levels in the brain tissue is required. METHODS: We now describe a method for determining nanogram quantities of [-]-DOM in the rat brain tissue using D-amphetamine as an intemal standard. The method employs solvent extraction with toluene and derivatization with trifluoroacetic acid anhydride (TFAA) followed by analysis using gas chromatography-mass spectrometry (GS-MS) in the selective ion monitoring (SIM) mode. RESULTS: With SIM detection, our overall recoveries were greater than 90%. The method was reliable in terms of within-day and between-day precision, accuracy, and linearity. The procedure was applied to animal subjects to determine the in vivo [-]-DOM brain levels following intraperitoneal (ip) administration. Our findings indicate that peak levels of [-]-DOM do not coincide with the 75-min pretreatment time established by drug-induced stimulus control. DISCUSSION: This study demonstrates a sensitive and precise analytical method for the determination of [-]-DOM levels in the rat brain following systemic administration of behaviorally relevant doses.

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

Blockade of the behavioral effects of lysergic acid diethylamide, 2,5-dimethoxy-4-methylamphetamine, quipazine and lisuride by 5-hydroxytryptamine antagonists.

The effects of lysergic acid diethylamide (LSD), 2,5-dimethoxy-4-methylamphetamine (DOM), quipazine or lisuride alone and in combination with the 5-hydroxytryptamine antagonist metergoline, pizotifen and cinanserin were studied in rats responding on a fixed-ratio 40 schedule of food presentation. LSD, DOM, quipazine or lisuride produced a similar dose-dependent decrease in the number of food presentations (ED50 values: 81 micrograms/kg, 0.6 mg/kg, 1.6 mg/kg and 31 micrograms/kg, respectively) and a reciprocal increase in the number of pause intervals (IRTs = 10 sec). All three antagonists attenuated the behavioral effects of LSD and DOM for both food presentations and pause intervals. The LSD-response curve for reinforcers was shifted to the greatest degree by pizotifen (1.0 mg/kg), followed by cinanserin (20 mg/kg) and metergoline (1.0 mg/kg). The ED50 values for this effect were 334, 181 and 141 micrograms/kg, respectively. The DOM dose-response pattern for decrease in reinforcers was shifted to the greatest degree by metergoline, followed by pizotifen and cinanserin (ED50 values: 26.5, 3.2 and 1.8 mg/kg, respectively). The effect of quipazine on reinforcers was antagonized by metergoline and pizotifen (ED50 values: greater than 8.0 for both) but not by cinanserin, although all three antagonists attenuated the increase in pause intervals in the same order as they did for DOM. The decrease in reinforcers by lisuride was equally antagonized by metergoline and pizotifen (ED50 values: 58 and 57 micrograms/kg, respectively), whereas cinanserin potentiated the effect of lisuride (ED50: 16 micrograms/kg).(ABSTRACT TRUNCATED AT 250 WORDS)

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

PubMed1999

UV-B-Induced acute toxicity of pyrene to the waterflea Daphnia magna in natural freshwaters.

The effects of various water characteristics in natural freshwaters on the acute toxicity of one polycyclic aromatic hydrocarbon (PAH), pyrene, to a pelagic invertebrate Daphnia magna was studied under ultraviolet B (UV-B) radiation and in the dark. Pyrene was photoactivated and was more toxic to D. magna in the presence of UV-B radiation. Dissolved organic material (DOM), measured as dissolved organic carbon (DOC), significantly reduced the photoenhanced toxicity of pyrene. Under UV-B radiation the EC(50) values were lower and in relation to the amount of DOM, ranging from 3.0 to 30.0 microg/L pyrene, whereas in the dark they were between 29.2 and 54.8 microg/L and not related to the amount of DOM in the waters. Although the condition and mortality of the daphnids in the control groups were not affected by UV-B irradiation, the increased toxicity was considered to be either an additive or a synergistic effect of both the photomodified pyrene and the stressing light conditions of UV-B. The measured binding of pyrene to DOM was low, although it was related to the amount of DOC. Despite the relatively high intensity of UV-B used, humic substances in the waters remained undegraded. It was thus concluded that with their brownish-yellowish color, waters rich in humic substances decreased the photomodification of the freely dissolved parent compound simply by diminishing the light penetration in these waters and, by implication, contact with the intact compound. These results suggest that DOM in surface waters plays an important role in protecting against the photoinduced toxicity of PAHs.

Animals↗

PubMed1995

The release of glutamate and aspartate from rat brain synaptosomes in response to domoic acid (amnesic shellfish toxin) and kainic acid.

Kainic acid is known to stimulate the release of glutamate (GLU) and aspartate (ASP) from presynaptic neurons. It has been suggested that the enhanced release of these endogenous EAA's plays a significant role in the excitotoxic effects of KA. Domoic acid (DOM), a shellfish toxin, is structurally similar to KA, and has been shown to be 3-8 times more toxic than KA. In this study, effects of KA and DOM on the release of GLU and ASP from rat brain synaptosomes were investigated. Amino acid analysis was performed by the reversed phase HPLC, following derivatization with 9-fluorenylmethyl chloroformate (FMOC). Potassium chloride (40 mM) was used as a positive control, and stimulated GLU release from rat brain synaptosomes in presence or absence of Ca2+. DOM enhanced the release of GLU, whereas KA stimulated the release of both GLU and ASP from synaptosomes in the presence of Ca2+. However, their potency to stimulate GLU and ASP release was enhanced in absence of Ca2+. These results indicate that different mechanisms may be involved in the release of GLU and ASP in response to DOM and KA, and that neurotransmitter release appeared to be highly specific for these agonists. It would appear that DOM and KA may interact with different receptors on the presynaptic nerve terminal, and/or activate different subtypes of voltage-dependent Ca2+ channels to promote influx of Ca2+ which is targeted for different pools neurotransmitters.

Animals↗