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Query: UMLS:C0036572 (seizures)
 80,221 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of ergot alkaloids, together with the DA agonists apomorphine and piribedil, were tested for protective effects against audiogenic seizures in an inbred strain of mice (DBA/2) and for induction of circling behaviour in mice with unilateral destruction of one nigrostriatal DA pathway. The order of potency against audiogenic seizures was apomorphine greater than ergocornine greater than bromocryptine greater than ergometrine greater than LSD greater than methysergide greater than piribedil while that observed in the rotating mouse model was apomorphine greater than ergometrine greater than ergocornine greater than bromocryptine greater than piribedil. LSD caused only weak circling behaviour even when administered in high doses (greater than 1 mg/kg). Methysergide was ineffective. Prior administration of the neuroleptic agent haloperidol blocked the effect of DA agonists and of ergot alkaloids in both animal models. The possible action of ergot alkaloids as DA agonists is discussed.
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PMID:Ergot alkaloids as dopamine agonists: comparison in two rodent models. 98 4

Most street hallucinogens contain either LSD or phenycyclidine HCl (PCP). Because the acute phase of LSD and PCP mimic several other drugs and conditions, it is important to exclude these other possibilities. When faced with LSD or PCP, "talking down" usually suffices for the mild case; management becomes more complex should hyperpyrexia, coma, seizures or a hypertensive crisis ensue. Diazepam, not a phenothiazine, is preferred for sedation.
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PMID:Management of hallucinogen abuse. 106 15

During the period of survey, the number of narcotic drug seizures by the law, especially cannabis resin, has increased considerably. The details on this development are presented. The following main analytical results were obtained: the median concentration of THC in cannabis resin has increased up to 8.6%, in cannabis plants the THC content has fluctuated between 1% and 3%. In the heroin samples since 1982, diamorphin has predominated in the base form; the diamorphin content had dropped to 32%, which is connected with a rise simultaneous in the concentration of noscapine (up to 9%). The concentration of cocaine hydrochloride had diminished at the end of the period to 62%; on the other hand, the amphetamine sulfate content increased to 69%. LSD trips used from 10 to 120 micrograms per trip. Methadone occurred mostly in the form of tablets containing 5 mg methadone hydrochloride.
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PMID:[Analysis of regional trends in narcotic studies between 1980 and 1986]. 280 Jul 29

Social isolation results in dynamic changes of neurobiological functions. The altered internal state of the CNS is reflected in changes in spontaneous behavior, changed responses to transmission-related substances and changed responsiveness to an additional impairment of normal relations between the organism and its environment. We analysed the influence of an acute 2-hour immobilization on such isolation-dependent changes. Whereas the susceptibility to pentetrazole-induced seizures increased continuously with lengthening of isolation and was not affected by the additional impairment, the responsiveness to transmission-related substances changed dynamically depending upon isolation-induced alterations. An immobilization-induced increase in responsiveness to LSD and propranolol was demonstrable in grouped controls and after short-term isolation. The apomorphine stimulation during prolonged isolation experienced a down- and an upregulation which were repeated in a stronger manner by immobilization responses especially after long-term isolation. It is suggested that the dynamics of isolation-induced changes coincided with changed acute adaptive functions.
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PMID:Altered neurobiological responses to acute immobilization in social-isolated mice. 287 73

If the frequency of seizures by police of hallucinogens reflects the frequency with which various hallucinogens are ingested in Australasia, most toxic states resulting from hallucinogen abuse are due to Bromo-DMA and not to LSD as is commonly reported by the subjects. Two cases of intoxication with the new hallucinogen, Bromo-DMA, are reported. Both recovered within 24 hours following treatment with haloperidol.
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PMID:Bromo-DMA: the Australasian hallucinogen? 658 Aug 96

In vitro binding studies to serotoninergic receptors were performed using 3H-LSD, 3H-5-HT and 3H-spiperone. An overview is given on findings using these three ligands with respect to the following: (1) Localization of specific binding sites, i.e., in various animal species, the regional distribution in the brain and periphery, the subcellular and cellular distribution. (2) Properties of the binding sites, i.e., influence of the composition of the assay medium, binding kinetic properties, receptor regulation in vivo. (3) Identity of the binding sites, i.e., differences between sites for various 3H-ligands, pharmacological specificity of the membranous binding sites, chemical composition of the macromolecular complex constituting the binding site. (4) Function of the receptor. Binding affinities of 44 compounds were measured in binding assays using 3H-spiperone and 3H-LSD with rat frontal cortex membrane preparations and using 3H-5-HT and 3H-LSD with rat hippocampal membrane preparations. A significant correlation between binding affinities for 3H-LSD and 3H-spiperone binding sites in the frontal cortex was found. Binding to these sites correlates with potencies of compounds to antagonize 5-HT-induced contraction in isolated rat caudal arteries and also with potencies of compounds to antagonize tryptamine-induced clonic seizures in rats. There was a very significant correlation between binding affinities for 3H-LSD and 3H-5-HT labelled sites in the hippocampus. These hippocampal binding sites are different from those for 3H-LSD and 3H-spiperone in the frontal cortex. Binding to 3H-5-HT or 3H-LSD sites in the hippocampus could not be related to a pharmacological effect.
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PMID:Serotoninergic receptors in brain tissue: properties and identification of various 3H-ligand binding sites in vitro. 728 50

LSD is making a comeback nationwide among Caucasian middle-class high school and college students. Compared to the mean values during the years 1985 to 1990, an approximately 25% increase occurred in lifetime-, annual-, and monthly-use rates of LSD, in 1993, according to the annual NIDA high school senior survey. In 1992, an increase in LSD-related arrests occurred, as did seizures of larger quantities of consumer-ready LSD. The number of LSD-related emergency room visits by adolescents increased, and intermittent LSD-related violent behavior, including suicide, homicide, and accidental death, were higher than in the previous 5-year period. Fewer high school students attribute great danger in trying LSD once or twice. The painfully learned lessons about LSD seem, sadly, destined to be relearned by the youth of the 1990s.
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PMID:LSD. Its rise, fall, and renewed popularity among high school students. 772 66

The application of micellar electrokinetic capillary chromatography (MECC) to the analysis of illicit drug seizures is presented. Areas investigated include general screening and qualitative and, in some instances, quantitative analysis of various drugs, including heroin, opium, cocaine, amphetamines, LSD and anabolic steroids. Due to its high efficiency, high selectivity and general applicability, MECC is well suited for forensic drug analyses.
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PMID:Application of micellar electrokinetic capillary chromatography to the analysis of illicit drug seizures. 933 31

SB-271046, potently displaced [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT(6) receptors recombinantly expressed in HeLa cells in vitro (pK(i) 8.92 and 9.09 respectively). SB-271046 also displaced [(125)I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pK(i) 8.81, 9.02 and 8.55 respectively). SB-271046 was over 200 fold selective for the 5-HT(6) receptor vs. 55 other receptors, binding sites and ion channels. In functional studies on human 5-HT(6) receptors SB-271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA(2) of 8.71. SB-271046 produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of < or =0.1 mg kg(-1) p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC(50) of 0.16 microM) and brain concentrations of 0.01-0.04 microM at C(max). These data, together with the observed anticonvulsant activity of other selective 5-HT(6) receptor antagonists, SB-258510 (10 mg kg(-1), 2-6 h pre-test) and Ro 04-6790 (1-30 mg kg(-1), 1 h pre-test), in the rat MEST test, suggest that the anticonvulsant properties of SB-271046 are likely to be mediated by 5-HT(6) receptors. Overall, these studies demonstrate that SB-271046 is a potent and selective 5-HT(6) receptor antagonist and is orally active in the rat MEST test. SB-271046 represents a valuable tool for evaluating the in vivo central function of 5-HT(6) receptors.
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PMID:Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. 1092 64

N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134) potently inhibited [125I]SB-258585 and [3H]LSD binding in a HeLa cell line expressing human 5-HT(6) receptors (pK(i)=8.6 and 8.54, respectively). Furthermore, SB-357134 inhibited [125I]SB-258585 binding in human caudate--putamen and in rat and pig striatum membranes (pK(i)=8.82, 8.44, and 8.61, respectively). SB-357134 displayed over 200-fold selectivity for the 5-HT(6) receptor versus 72 other receptors and enzymes. 5-HT-stimulated cyclic AMP (cAMP) accumulation in human 5-HT(6) receptors was competitively antagonised by SB-357134 (pA(2)=7.63). SB-357134 inhibited ex vivo [125I]SB-258585 binding in the rat with an ED(50) of 4.9 +/- 1.3 mg/kg po, 4 h postdose. In the rat maximal electroshock seizure threshold (MEST) test, SB-357134 produced a potent and dose-dependent increase in seizure threshold, with a minimum effective dose of 0.1 mg/kg po. At 10 mg/kg po, maximum activity occurred between 4 and 6 h postdose. Good exposure was observed with SB-357134 at 10 mg/kg po, reaching maximal blood and brain concentrations of 4.3 +/- 0.2 and 1.3 +/- 0.06 microM, respectively, 1 h postdose. In addition, SB-357134 (10 mg/kg po) enhanced memory and learning following chronic administration (twice a day for 7 days) in the rat water maze. Overall, these studies demonstrate that SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist.
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PMID:Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist. 1188 56


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