• These actions were abolished by the 5-HT 1A antagonist, (-)-tertatolol, but unaffected by the hD 2 /hD 3 antagonist, haloperidol. (aspetjournals.org)
  • 4. The effects of MKC-242 and 8-OH-DPAT in the hypothalamus were antagonized by pretreatment with WAY100135 (10 mg kg-1), a silent 5-HT1A receptor antagonist. (biopsychiatry.com)
  • 5. Local administration of 8-OH-DPAT (10-100 microM), citalopram (1 microM), a 5-HT reuptake inhibitor, and MDL72222 (10 microM), a 5-HT3 receptor antagonist, into the hypothalamus, had no effect on NA release. (biopsychiatry.com)
  • The ability of R(+)-8-OH-DPAT (50 μg/kg s.c.) to inhibit d-amphetamine sulfate (1.0 mg/kg s.c.)-induced increase in extracellular dopamine levels was abolished by WAY 100,635 (n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride), a selective 5-HT 1A receptor antagonist (100 μg/kg s.c.), administered 5 min prior to R(+)-8-OH-DPAT in both regions. (elsevierpure.com)
  • The aminotetralins, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and 7-OH-DPAT behave as preferential agonists at serotonin (5-HT) 1A and dopamine D 3 and D 2 receptors, respectively. (aspetjournals.org)
  • Their effects on dialysate dopamine and 3,4-di-hydroxyphenylacetic acid (DOPAC) were measured and compared with the effects of raclopride. (nih.gov)
  • resulted in the animals' making a progressively greater number of responses on the drug-appropriate lever … of 8-OH DPAT plus (+)amphetamine (0.33 mg/kg) elicited 91% (+)amphetamine-appropriate responding. (supp.ai)
  • In our study, we evaluated the influence of their (+)- and (-) isomers on the electrical activity of serotoninergic neurones of the dorsal raphe nucleus (DRN), which bear 5-HT 1A autoreceptors, and of dopaminergic neurones of the ventral tegmental area (VTA), which possess inhibitory D 3 and D 2 receptors. (aspetjournals.org)
  • Neither (+)- nor (-)-7-OH-DPAT show substantial selectivity for hD 3 vs . 5-HT 1A receptors and their inhibition of the firing of VTA as compared to DRN neurones is mediated by hD 3 /hD 2 and 5-HT 1A receptors, respectively. (aspetjournals.org)
  • Finally, VTA neurones are stimulated by (+)-8-OH-DPAT via 5-HT 1A receptors and inhibited by (-)-8-OH-DPAT via hD 3 and/or hD 2 receptors. (aspetjournals.org)
  • 8. These results demonstrate that the majority of thalamocortical neurones are endowed with electrophysiological properties allowing them to oscillate at 0.5-4 Hz, if they have a membrane potential more negative than -65 mV and a high input resistance. (researchgate.net)
  • The effect of systemic administration of the 5-HT precursor, 5-hydroxy-L-tryptophan (5-HTP) on the release of 5-HT in the lateral hypothalamus of the chloral hydrate-anaesthetized rat in vivo was examined using brain microdialysis. (ox.ac.uk)
  • The present study describes the effect of a highly potent and selective 5-HT1A receptor agonist, 5-(3-[[(2S)-1,4-benzodioxan-2-ylmethyl)]amino]propoxy)-1,3-b enzodioxole HC1 (MKC-242), on NA release in the hypothalamus using microdialysis in the freely moving rat. (biopsychiatry.com)
  • Effect of 5-hydroxy-L-tryptophan on the release of 5-HT in rat hypothalamus in vivo as measured by microdialysis. (ox.ac.uk)
  • 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-h. (erowid.org)
  • Since these effects are resistant to prior monoamine depletion and/or synthesis inhibition by means of reserpine and alpha-propyldopacetamide (H22/54), respectively, they are most likely to be attributable to direct serotonin receptor agonism by 8-OH-DPAT. (erowid.org)
  • In this process, serotonin may interact antagonistically with noradrenaline (norepinephrine) and its α 2 -noradrenergic receptors that normally function to enhance carbohydrate intake at the onset of the natural feeding cycle. (springer.com)
  • Administration of the 5-HT1A receptor agonist, 8-hydroxy-2-(di-n-propylamino) tetralin (0.25 mg/kg i.p.), which selectively inhibits serotoninergic neuronal activity by activation of the somatodendritic 5-HT autoreceptor, significantly decreased basal levels of 5-HT and markedly attenuated the 5-HTP-induced increase in 5-HT. (ox.ac.uk)
  • More importantly, we used mice deficient in the gene encoding tryptophan hydroxylase 2 ( Tph2 ), which could not synthesize 5-HT in the brain. (aspetjournals.org)
  • These actions were compared to their in vitro interactions with cloned, human (h)5-HT 1A , hD 3 and hD 2 receptors. (aspetjournals.org)
  • In binding studies, racemic 8-OH-DPAT showed 100-fold selectivity for h5-HT 1A vs . hD 2 and hD 3 receptors and there was little difference between its (+)- and (-)-isomers either in terms of their potency at 5-HT 1A receptors or of their selectivity at 5-HT 1A vs hD 2 /hD 3 sites. (aspetjournals.org)
  • In contrast to 8-OH-DPAT, the (+)- and (-)-isomers of 7-OH-DPAT showed marked stereoselectivity inasmuch as the latter bound with 20-fold less potency than the former at hD 3 and, at higher concentrations, hD 2 receptors. (aspetjournals.org)
  • In conclusion, for these substituted aminotetralins, stereospecificity is a more marked feature of interactions at hD 3 (and hD 2 ) than at h5-HT 1A receptors and is more pronounced for 7- as compared to 8-OH-DPAT. (aspetjournals.org)
  • this is flanked by a series of upstream repressor elements for REST, Freud-1/CC2D1A and Freud-2/CC2D1B factors that not only restrict its expression to neurons, but may also regulate the level of expression of 5-HT1A receptors in various subsets of neurons, including serotonergic neurons. (biomedcentral.com)
  • With regard to central 5-HT neurotransmission the effects of 8 OH-DPAT increased 5-HT levels, decreased 5-HIAA levels, 5-HT-synthesis rate and 5-HT utilization and inhibited 5-HT neuronal firing are virtually identical, and comparable in potency, to those reported to result from the administration of lisuride or LSD. (erowid.org)
  • decreased the levels of ERK1, JNK-1, and JNK-2 phosphorylated in the hippocampus of the animals. (supp.ai)
  • 7. The effect of MKC-242 in increasing NA release was not attenuated by repeated treatment with the drug (0.5 mg kg-1, once a day for 2 weeks). (biopsychiatry.com)
  • It was demonstrated that the simplified ergot congener 8-hydroxy-2-(di-n-propylamino)tetralin, 8-OH-DPAT, is able to elicit pronounced biochemical and behavioural alterations indicative of central serotoninomimetic activity. (erowid.org)
  • Cell counting kit-8 assay and Transwell assays were used to explore cell proliferation, migration and invasion. (bvsalud.org)
  • 2. Subcutaneous injection of MKC-242 (0.5 mg kg-1) increased extracellular levels of NA and its metabolite, 3-methoxy-4-hydroxyphenylglycol, in the hypothalamus and hippocampus. (biopsychiatry.com)
  • There was no significant difference in the distribution of genotypic (χ 2 =2.70, p=0.26) and allelic (χ 2 =1.87, p=0.17) frequencies between the patient groups with TD and without TD. (kjsr.org)
  • The enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin (3) have been synthesized and evaluated for activity at central dopamine (DA), 5-hydroxytryptamine, and norepinephrine (NE) receptors, by use of biochemical and behavioral tests in rats. (nih.gov)
  • The pharmacological effects of both enantiomers are complicated, but (2R,3S)-7-hydroxy-3-methyl-2-(dipropylamino)tetralin [(-)-3] produced biochemical effects in vivo similar to those elicited by classical DA D2-receptor antagonists. (nih.gov)
  • Diazinon evoked up-regulation of 5HT 1A and 5HT 2 receptor expression even at doses devoid of effects on cholinesterase activity, a pattern similar to that seen earlier for another organophosphate, chlorpyrifos. (nih.gov)
  • Using [35S]GTPgammaS binding in rat hippocampal tissue, vilazodone was demonstrated to have an intrinsic activity comparable to the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). (nih.gov)
  • 5-HT1A receptor binding was assayed in post-mortem prefrontal cortex using [3H]8-OH-DPAT, and specific binding determined by 1 microM 5-HT. (nih.gov)
  • Concomitant with this elevated receptor expression, the 5-HT1A receptor agonist 8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) led to an increased hypothermic response in rictor KO mice. (vumc.org)
  • In contrast, rictor KO mice displayed significantly reduced head-twitch response (HTR) to the 5-HT2A/C agonist 2,5-dimethoxy-4-iodoamphetamine (DOI), with evidence of impaired 5-HT2A/C receptor signaling. (vumc.org)
  • We synthesized a small-molecule opioid receptor-like 1 (ORL1) receptor agonist, 2-{3-[1-((1R)-acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-y l}-N-methylacetamide (W-212393), and investigated its effect on the circadian body temperature rhythm of rats. (lookformedical.com)
  • We exposed neonatal rats to daily doses of diazinon or parathion on postnatal days (PND)1-4 and evaluated 5HT receptors and the 5HT transporter in brainstem and forebrain on PND5, focusing on doses of each agent below the maximum tolerated dose and spanning the threshold for cholinesterase inhibition: 0.5, 1, or 2 mg/kg for diazinon, and 0.02, 0.05, and 0.1 mg/kg for parathion. (nih.gov)
  • Using in vivo microdialysis, vilazodone (10 mg/kg p.o.) was demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. (nih.gov)
  • 1 , 2 The selective, full 5-HT 1A -R-agonist repinotan 3 , 4 has been shown to counteract morphine-induced ventilatory depression in spontaneously breathing rats. (silverchair.com)
  • Mice received systemic MPTP treatment at two different temperatures, 4 degrees C and 22 degrees C. MPTP-treated mice maintained at 4 degrees C demonstrated (1) a greater hypothermic response, (2) a significant reduction in striatal DA content and tyrosine hydroxylase (TH) activity, and (3) significantly greater striatal 1-methyl-4-phenylpyridinium (MPP+) levels, as compared to mice dosed with MPTP at room temperature. (nih.gov)
  • Here we examined the effects of the 5-HT 1A/7 agonist 8-OH-DPAT and the 5-HT 1/2 agonist quipazine on the circadian system in mice, with some parallel experiments conducted with hamsters for comparative purposes. (nebraska.edu)
  • In mice, quipazine modestly increased c-Fos expression in the SCN (site of the circadian pacemaker) during the subjective day, whereas 8-OH-DPAT did not affect SCN c-Fos. (nebraska.edu)
  • 8-OH-DPAT did not significantly attenuate light-induced phase shifts in mice but did in hamsters (between-species positive control). (nebraska.edu)
  • Here we examined the effects of the 5-HT1A/7 agonist 8-OH-DPAT and the 5-HT1/2 agonist quipazine on the circadian system in mice, with some parallel experiments conducted with hamsters for comparative purposes. (nebraska.edu)
  • Vilazodone (1-10 mg/kg p.o.) dose-dependently displaced in vivo [3H]DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio)benzylamine) binding from rat cortex and hippocampus, indicating that vilazodone occupies 5-HT transporters in vivo. (nih.gov)
  • Concentrations of naphthols, 2-methoxyphenol and dimethylphenol isomers in the urine of occupationally exposed workers were significantly higher than those of non-exposed subjects. (lookformedical.com)
  • Concentrations of the 2-methoxyphenol and dimethylphenol isomers in urine were significantly higher for the tar distillation workers, whereas concentrations of naphthols were higher for the oil naphthalene distillation workers. (lookformedical.com)
  • It remained to be clarified (1) whether a moderate dose of repinotan, sufficient to stimulate spontaneous breathing, impairs antinociception if plasma concentration decreases over time, and if (2) moderate doses prevent ventilatory depression if given before the opioid. (silverchair.com)
  • In hamsters, quipazine intraperitoneally (i.p.) did not induce phase shifts, whereas 8-OH-DPAT induced phase shifts after i.p. but not intra-SCN injections. (nebraska.edu)
  • The magnitude of the W-212393 (0.3-3 mg kg(-1), i.p.)-induced phase advance was dose-dependent and greater than those produced by 8-hydroxy-2-(di-n-propylamino)tetralin (0.3-3 mg kg(-1), i.p.) or melatonin (0.3-3 mg kg(-1), i.p. (lookformedical.com)
  • Concurrent administration of MK-801 or 8-OHDPAT increased the striatal MPP+ levels following MPTP treatment. (nih.gov)