| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| M S Kleven, M B Assié, W Koe. Pharmacological characterization of in vivo properties of putative mixed 5-HT1A agonist/5-HT(2A/2C) antagonist anxiolytics. II. Drug discrimination and behavioral observation studies in rats. The Journal of pharmacology and experimental therapeutics. vol 282. issue 2. 1997-09-11. PMID:9262338. |
to characterize their in vivo 5-hydroxytryptamine (5-ht)2a antagonist properties, the ability of the putative mixed 5-ht1a agonists/5-ht(2a,2c) antagonists (n-(29(4-(2-pyrimidinyl)-1-piperazinyl)ethyl)tricyclo(3.3.1.1(3,7) ) decane-1-carboxamide (wy-50,324), (2-(4-(4,4-bis(4-fluorophenyl)butyl)-1-piperazinyl)-3-pyridinecarboxy lic acid hydrochloride (fg5974), 9,10-didehydro-n-(2-propynyl)-6-methylergoline-8b-carboxamid e (lek-8804) and trans-1,3,4,a5,10b-hexahydro10-methoxy-4-propyl-2h-(1)benzopyra nol[3,4-b]pyridine (cgs 18102a) to antagonize both head twitches and discriminative stimulus (ds) effects produced by (+/-)-2,5-dimethoxy-4-iodoamphetamine (doi) in rats were compared with those of the 5-ht2 antagonists ketanserin and ritanserin, and the 5-ht1a agonists 8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat) and buspirone. |
1997-09-11 |
2023-08-12 |
rat |
| M S Kleven, M B Assié, W Koe. Pharmacological characterization of in vivo properties of putative mixed 5-HT1A agonist/5-HT(2A/2C) antagonist anxiolytics. II. Drug discrimination and behavioral observation studies in rats. The Journal of pharmacology and experimental therapeutics. vol 282. issue 2. 1997-09-11. PMID:9262338. |
in vivo 5-ht1a agonist effects were demonstrated by the finding that relatively selective- and mixed-5-ht1a agonists produced one or more elements of the "serotonin syndrome," i.e., flat-body posture, forepaw treading, or lower-lip retraction, and produced high levels of drug-lever selection in rats trained to discriminate 8-oh-dpat (0.16 mg/kg) from saline. |
1997-09-11 |
2023-08-12 |
rat |
| E Seifritz, S M Stahl, J C Gilli. Human sleep EEG following the 5-HT1A antagonist pindolol: possible disinhibition of raphe neuron activity. Brain research. vol 759. issue 1. 1997-09-10. PMID:9219866. |
therefore, the present data, tentatively, are consistent with the contention that pindolol inhibits, possibly selectively, somatodendritic 5-ht1a autoreceptors in humans and may antagonize self-inhibition of midbrain raphe nuclei 5-ht neurons. |
1997-09-10 |
2023-08-12 |
human |
| E A Jewell-Motz, E T Donnelly, M G Eason, S B Ligget. Role of the amino terminus of the third intracellular loop in agonist-promoted downregulation of the alpha2A-adrenergic receptor. Biochemistry. vol 36. issue 29. 1997-09-08. PMID:9220972. |
mutated receptors, consisting of chimeric substitutions of analogous beta2-adrenergic receptor (beta2ar) and serotonin 5-hydroxytryptamine1a (5-ht1a) receptor sequence into the second intracellular loop (icl2) (residues 113-149), the amino terminus (residues 218-235) and carboxy terminus (residues 355-371) of icl3, and a deletion of the beta-adrenergic receptor kinase (betaark) phosphorylation sites in the third intracellular loop (icl3) (residues 293-304), were expressed in chinese hamster ovary (cho) cells. |
1997-09-08 |
2023-08-12 |
Not clear |
| K Tokarski, A Czyrak, M Maćkowiak, K Wedzony, M Bija. Prolonged treatment with antidepressants increases the 5-HT1A-mediated inhibition of hippocampal neurons without changing the 5-HT1A receptor binding. Acta physiologica Hungarica. vol 84. issue 3. 1997-09-05. PMID:9219632. |
the effect of repeated treatment with antidepressant drugs imipramine, (+)oxaprotiline and paroxetine on neuronal responsiveness to 5-ht and the 5-ht1a receptor agonist 8-oh-dpat was examined in the hippocampal slice preparation from the rat. |
1997-09-05 |
2023-08-12 |
rat |
| M Sas. [A new approach to innovating selective anxiolytics: pharmacological profile of a novel 5-HT1A agonist (tandospirone)]. Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology. vol 17. issue 2. 1997-09-04. PMID:9201724. |
this agent binds with 5-ht1a receptors located in both 5-ht neurons in the raphe nucleus and other postsynaptic neurons to induce hyperpolarization of the neurons by opening the k+ channels to eventually inhibit the target neuronal activities. |
1997-09-04 |
2023-08-12 |
rat |
| C Moret, M Brile. Ex vivo inhibitory effect of the 5-HT uptake blocker citalopram on 5-HT synthesis. Journal of neural transmission (Vienna, Austria : 1996). vol 104. issue 2-3. 1997-09-03. PMID:9203078. |
the selective 5-ht reuptake inhibitor, citalopram, the 5-ht1a agonists, (+/-) 8-hydroxy-2-(di-n-propylamino)-tetralin (8-oh-dpat), ipsapirone, gepirone and the 5-ht1a/b agonist, 7-trifluoromethyl-4(4-methyl-1-piperazinyl-pyrolo[1,2-a]-quinox ali ne (cgs 12066b), the 5-ht1a/b ligands and beta-adrenoceptor antagonists, (+/-) pindolol and (+/-) alprenolol, and the non-selective 5-ht ligands, m-chlorophenylpiperazine (mcpp) and metergoline, all inhibited the synthesis of 5-ht. |
1997-09-03 |
2023-08-12 |
rat |
| C Moret, M Brile. Ex vivo inhibitory effect of the 5-HT uptake blocker citalopram on 5-HT synthesis. Journal of neural transmission (Vienna, Austria : 1996). vol 104. issue 2-3. 1997-09-03. PMID:9203078. |
the selective 5-ht1a antagonist, way 100635, which did not modify by itself 5-ht synthesis, had no effect on citalopram-induced reduction of 5-ht synthesis. |
1997-09-03 |
2023-08-12 |
rat |
| C Moret, M Brile. Ex vivo inhibitory effect of the 5-HT uptake blocker citalopram on 5-HT synthesis. Journal of neural transmission (Vienna, Austria : 1996). vol 104. issue 2-3. 1997-09-03. PMID:9203078. |
these results suggest that the effect of citalopram on the synthesis of 5-ht is not mediated by 5-ht1a or 5-ht2 receptors and that other receptors may be involved. |
1997-09-03 |
2023-08-12 |
rat |
| A Mosner, G Kuhlman, C Roehm, W H Voge. Serotonergic receptors modify the voluntary intake of alcohol and morphine but not of cocaine and nicotine by rats. Pharmacology. vol 54. issue 4. 1997-09-03. PMID:9211564. |
effects of fluvoxamine, a relatively selective 5-ht uptake inhibitor, and ipsapirone, a relatively selective 5-ht1a agonist, were studied on the initiation and/or maintenance of the voluntary intake of alcohol, morphine, cocaine, and/or nicotine in rats using the two-bottle free-choice method. |
1997-09-03 |
2023-08-12 |
rat |
| A Mosner, G Kuhlman, C Roehm, W H Voge. Serotonergic receptors modify the voluntary intake of alcohol and morphine but not of cocaine and nicotine by rats. Pharmacology. vol 54. issue 4. 1997-09-03. PMID:9211564. |
these results suggest: (1) selective stimulation of 5-ht1a receptors reduces alcohol preference, (2) stimulation of all 5-ht receptors has no effect on alcohol intake, indicating the presence of inhibitory receptors, (3) stimulation of the serotonergic system in general stimulates morphine preference, (4) the serotonin system does not affect nicotine or cocaine preference and (5) the serotonergic system is not involved in the voluntary consumption of all, but-only of some drugs/chemicals of abuse. |
1997-09-03 |
2023-08-12 |
rat |
| J Eugen-Olsen, P Afzelius, L Andresen, J Iversen, G Kronborg, P Aabech, J O Nielsen, B Hofman. Serotonin modulates immune function in T cells from HIV-seropositive subjects. Clinical immunology and immunopathology. vol 84. issue 2. 1997-09-02. PMID:9245541. |
the effect on lymphocyte proliferation was most likely mediated through the serotonin 5ht1a receptor because similar results could be obtained by using dpat, a specific activator of this receptor. |
1997-09-02 |
2023-08-12 |
human |
| J Eugen-Olsen, P Afzelius, L Andresen, J Iversen, G Kronborg, P Aabech, J O Nielsen, B Hofman. Serotonin modulates immune function in T cells from HIV-seropositive subjects. Clinical immunology and immunopathology. vol 84. issue 2. 1997-09-02. PMID:9245541. |
changes in the expression of 5ht1a receptors as judged by the expression of mrna could not explain why serotonin in vitro had a stronger enhancing effect on cell proliferation in some hiv-seropositive individuals than in others. |
1997-09-02 |
2023-08-12 |
human |
| A Newman-Tancredi, C Conte, C Chaput, L Verrièle, V Audinot-Bouchez, S Lochon, G Lavielle, M J Milla. Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn-Schmiedeberg's archives of pharmacology. vol 355. issue 6. 1997-08-27. PMID:9205951. |
in contrast, serotonin, dihydroergotamine, sumatriptan, naratriptan and alniditan, which are effective in acute interruption of migraine attacks, each displayed high efficacy (emax = 100, 100, 92.6, 79.3, 79.1% respectively) and marked affinity (ki = 18.7, 0.6, 127, 26.4 and 3.0 nm respectively) at 5-ht1a receptors. |
1997-08-27 |
2023-08-12 |
human |
| A Rex, C A Marsden, H Fin. Cortical 5-HT-CCK interactions and anxiety-related behaviour of guinea-pigs: a microdialysis study. Neuroscience letters. vol 228. issue 2. 1997-08-25. PMID:9209103. |
the 'anxiolytic' 5-ht1a agonist 8-hydroxy-2-(di-n-propyl amino) tetralin (8-oh-dpat; 0.3 mg/kg) reduced basal 5-ht and the increase in 5-ht release on the x-maze. |
1997-08-25 |
2023-08-12 |
Not clear |
| A Rex, C A Marsden, H Fin. Cortical 5-HT-CCK interactions and anxiety-related behaviour of guinea-pigs: a microdialysis study. Neuroscience letters. vol 228. issue 2. 1997-08-25. PMID:9209103. |
the results demonstrate an interaction between cck and 5-ht1a mechanisms via the influence on cortical 5-ht release. |
1997-08-25 |
2023-08-12 |
Not clear |
| M J LoCurt. The serotonin syndrome. Emergency medicine clinics of North America. vol 15. issue 3. 1997-08-25. PMID:9255139. |
in most cases, two or more types of medications known to increase the activity of serotonin at the 5-ht1a receptor are required to produce it, and it frequently begins soon after the initiation of a new treatment regimen. |
1997-08-25 |
2023-08-12 |
Not clear |
| R G Johnson, D Fiorella, J C Winter, R A Rabi. [3H]8-OH-DPAT labels a 5-HT site coupled to inhibition of phosphoinositide hydrolysis in the dorsal raphe. European journal of pharmacology. vol 329. issue 1. 1997-08-22. PMID:9218690. |
similarly, although 5-ht and selective 5-ht1a receptor ligands displayed high affinity for the [3h]8-oh-dpat binding site in the dorsal raphe nucleus, the affinity at the dorsal raphe site was less than that observed at the hippocampal 5-ht1a receptor. |
1997-08-22 |
2023-08-12 |
Not clear |
| C G Cardenas, L P Del Mar, R S Scrogg. Two parallel signaling pathways couple 5HT1A receptors to N- and L-type calcium channels in C-like rat dorsal root ganglion cells. Journal of neurophysiology. vol 77. issue 6. 1997-08-19. PMID:9212275. |
the inhibitory effects of 5ht and the 5ht1a agonist 8-oh-dpat were shown to be antagonized by the 5ht1a antagonists spiperone and pindolol, respectively, indicating involvement of a 5ht1a receptor. |
1997-08-19 |
2023-08-12 |
rat |
| C G Cardenas, L P Del Mar, R S Scrogg. Two parallel signaling pathways couple 5HT1A receptors to N- and L-type calcium channels in C-like rat dorsal root ganglion cells. Journal of neurophysiology. vol 77. issue 6. 1997-08-19. PMID:9212275. |
application of 5ht (a membrane impermeant compound) outside the patch pipette produced steady state inhibition only, whereas similar application of membrane permeant 5ht1a agonists, 8-oh-dpat or 5-methoxy-n,n-dimethyl-tryptamine, produced kinetic slowing and steady state inhibition. |
1997-08-19 |
2023-08-12 |
rat |