| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| P Blier, C de Montign. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse (New York, N.Y.). vol 1. issue 5. 1989-02-23. PMID:2905533. |
the sustained administration of the 5-ht1a agonist gepirone (15 mg/kg/day, s.c.) in the rat produced an initial decrease of the firing activity of dorsal raphe 5-ht neurons which was followed by a progressive recovery to normal after 14 days of treatment. |
1989-02-23 |
2023-08-11 |
rat |
| P Blier, C de Montign. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse (New York, N.Y.). vol 1. issue 5. 1989-02-23. PMID:2905533. |
at this point in time, the effect of intravenous lysergic acid diethylamide (lsd) on the firing activity of 5-ht neurons was markedly reduced, whereas those of 8-hydroxy-2-n,n-propylamino-tetralin (8-oh-dpat) and of gepirone were unchanged; however, the responsiveness of 5-ht neurons to direct microiontophoretic application of 5-ht, lsd, 8-oh-dpat, and gepirone, but not of gaba, was reduced. |
1989-02-23 |
2023-08-11 |
rat |
| P Blier, C de Montign. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse (New York, N.Y.). vol 1. issue 5. 1989-02-23. PMID:2905533. |
the responsiveness of postsynaptic dorsal hippocampus pyramidal neurons to 5-ht, 8-oh-dpat, and gepirone was not altered by the 14-day gepirone treatment. |
1989-02-23 |
2023-08-11 |
rat |
| P Blier, C de Montign. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse (New York, N.Y.). vol 1. issue 5. 1989-02-23. PMID:2905533. |
it is concluded that the progressive restoration of the firing activity of 5-ht neurons, due to a desensitization of the somatodendritic 5-ht autoreceptor, combined with the direct activation of normosensitive postsynaptic 5-ht1a receptor by gepirone, should result in an augmented tonic activation of postsynaptic 5-ht1a receptors. |
1989-02-23 |
2023-08-11 |
rat |
| S N Mitchell, P J Thoma. Effect of restraint stress and anxiolytics on 5-HT turnover in rat brain. Pharmacology. vol 37. issue 2. 1989-02-21. PMID:2905483. |
the increase in 5-ht synthesis in the frontal cortex following 180 min restraint stress was inhibited by pretreatment with buspirone, when administered at 2.5 mg/kg (s.c.) 30 min prior to the stress period, but not by chlordiazepoxide at 10 mg/kg (s.c.). |
1989-02-21 |
2023-08-11 |
rat |
| P Schoeffter, D Hoye. Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus. British journal of pharmacology. vol 95. issue 3. 1989-02-16. PMID:3207999. |
concentration-dependent inhibition of forskolin-stimulated adenylate cyclase activity was elicited by the reference 5-ht1-receptor agonists (mean ec50 value, nm): 5-ht (22), 5-carboxamidotryptamine (5-ct, 3.2), 8-hydroxy-2-(di-n-propylamino)-tetralin (8-oh-dpat, 8.6), n,n-dipropyl-5-carboxamidotryptamine (dp-5-ct, 2.3), 1-[2-(4-aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)-piperazine (papp or ly 165163, 20), 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h indole (ru 24969, 20), buspirone (65) and ipsapirone (56). |
1989-02-16 |
2023-08-11 |
Not clear |
| B Costall, M E Kelly, R J Naylor, E S Onaiv. Actions of buspirone in a putative model of anxiety in the mouse. The Journal of pharmacy and pharmacology. vol 40. issue 7. 1989-02-08. PMID:2904990. |
in contrast, the injection of 5-hydroxytryptamine and 2-methyl-5-hydroxytryptamine into the dorsal raphe nucleus increased exploratory behaviour in the black section with decreased activity in the white area: the effects of 2-methyl-5-hydroxytryptamine were antagonized by buspirone administered peripherally. |
1989-02-08 |
2023-08-11 |
mouse |
| B Costall, M E Kelly, R J Naylor, E S Onaiv. Actions of buspirone in a putative model of anxiety in the mouse. The Journal of pharmacy and pharmacology. vol 40. issue 7. 1989-02-08. PMID:2904990. |
it is concluded that in the mouse model the ability of buspirone to reduce the aversive response to a brightly illuminated area may reflect an anxiolytic action, that the dorsal raphe nucleus may be an important locus of action, and that the effects of buspirone may reflect an interaction at 5-hydroxytryptamine receptors. |
1989-02-08 |
2023-08-11 |
mouse |
| F G Szele, D L Murphy, N A Garric. Effects of fenfluramine, m-chlorophenylpiperazine, and other serotonin-related agonists and antagonists on penile erections in nonhuman primates. Life sciences. vol 43. issue 16. 1988-11-16. PMID:3172981. |
in contrast, serotonin (5-ht) agonists with 5-ht1a site specificity (8-oh-dpat, buspirone) as well as trazodone, ritanserin, and metergoline were no different from saline in producing penile erections. |
1988-11-16 |
2023-08-11 |
monkey |
| M Lade. Clinical pharmacology of non-benzodiazepine anxiolytics. Pharmacology, biochemistry, and behavior. vol 29. issue 4. 1988-09-29. PMID:2901119. |
the most important of the non-benzodiazepine anxiolytics is buspirone, which seems to act on 5-ht mechanisms. |
1988-09-29 |
2023-08-11 |
Not clear |
| M F Hibert, M W Gittos, D N Middlemiss, A K Mir, J R Fozar. Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. Journal of medicinal chemistry. vol 31. issue 6. 1988-06-30. PMID:3373482. |
a conformational study of four 5-ht1a (serotonin) receptor ligands ((r-(-)-methiothepin, spiperone, (s)-(-)-propranolol, and buspirone) led to the definition of a pharmacophore and a three-dimensional map of the 5-ht1a antagonist recognition site. |
1988-06-30 |
2023-08-11 |
rat |
| M Davis, J V Cassella, J H Kehn. Serotonin does not mediate anxiolytic effects of buspirone in the fear-potentiated startle paradigm: comparison with 8-OH-DPAT and ipsapirone. Psychopharmacology. vol 94. issue 1. 1988-04-18. PMID:2894698. |
serotonin does not mediate anxiolytic effects of buspirone in the fear-potentiated startle paradigm: comparison with 8-oh-dpat and ipsapirone. |
1988-04-18 |
2023-08-11 |
Not clear |
| M Davis, J V Cassella, J H Kehn. Serotonin does not mediate anxiolytic effects of buspirone in the fear-potentiated startle paradigm: comparison with 8-OH-DPAT and ipsapirone. Psychopharmacology. vol 94. issue 1. 1988-04-18. PMID:2894698. |
large lesions of the dorsal and median raphe nuclei or ip injections of the serotonin antagonists cinanserin (10 mg/kg) or cyproheptadine (5 mg/kg) did not alter fear-potentiated startle, nor did these treatments prevent buspirone (5 or 10 mg/kg sc) from blocking fear-potentiated startle. |
1988-04-18 |
2023-08-11 |
Not clear |
| M Davis, J V Cassella, J H Kehn. Serotonin does not mediate anxiolytic effects of buspirone in the fear-potentiated startle paradigm: comparison with 8-OH-DPAT and ipsapirone. Psychopharmacology. vol 94. issue 1. 1988-04-18. PMID:2894698. |
taken together, the data do not support the hypothesis that buspirone's anxiolytic effects are mediated by actions at 5-ht 1a receptors and more generally indicate that serotonergic neurons do not play an important role in fear-potentiated startle. |
1988-04-18 |
2023-08-11 |
Not clear |
| H Gozlan, M Ponchant, G Daval, D Verge, F Menard, A Vanhove, J P Beaucourt, M Hamo. 125I-Bolton-Hunter-8-methoxy-2-[N-propyl-N-propylamino]tetralin as a new selective radioligand of 5-HT1A sites in the rat brain. In vitro binding and autoradiographic studies. The Journal of pharmacology and experimental therapeutics. vol 244. issue 2. 1988-04-12. PMID:2964524. |
in vitro binding assays with 125i-[8-methoxy-2-[n-propyl-n-(3'-iodo-4'-hydroxyphenyl)-propionamido -n'- propylamino] tetralin] (125i-bh-8-meo-n-pat), a 125i-labeled derivative of the potent serotonin (5-ht) agonist 8-hydroxy-2-[di-n-propylamino]tetralin [( 3h]-8-oh-dpat), showed that this compound recognized specific sites with nanomolar affinity for 5-ht and 5-ht1a ligands such as spiroxatrine, ipsapirone, buspirone and gepirone in rat hippocampal membranes. |
1988-04-12 |
2023-08-11 |
rat |
| A Dumuis, M Sebben, J Bockaer. Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture. Molecular pharmacology. vol 33. issue 2. 1988-03-24. PMID:2828913. |
the rank order of potencies of classical 5-ht1 agonists in inhibiting camp formation in hippocampal neurons was 8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat) greater than 5-carboxamidotryptamine (5-ct) greater than d-lysergic acid diethylamide greater than 5-ht greater than 5-methoxy-n,n-dimethyltryptamine (5-meo-n,n-dmt) greater than ru 24969 greater than ipsapirone greater than bufotenine greater than buspirone [half-maximal efficacy (ec50) = 7, 18, 30, 52, 90, 102, 100, 110, and 128 nm, respectively]. |
1988-03-24 |
2023-08-11 |
mouse |
| A Ia Korneev, M I Faktor, T B Cha. [Interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain]. Biulleten' eksperimental'noi biologii i meditsiny. vol 105. issue 1. 1988-03-23. PMID:2892547. |
[interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain]. |
1988-03-23 |
2023-08-11 |
human |
| A Ia Korneev, M I Faktor, T B Cha. [Interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain]. Biulleten' eksperimental'noi biologii i meditsiny. vol 105. issue 1. 1988-03-23. PMID:2892547. |
ic50 of serotonin and buspirone and mj 138-05 for (3h) lsd (2 nm) specific binding sites in the hippocamp was determined as 0.14 microm, 2.3 microm and 6.1 microm, respectively; and for (3h) serotonin specific binding sites in the hippocamp as 0.005 microm, 3.8 microm and 21 microm, respectively. |
1988-03-23 |
2023-08-11 |
human |
| A Ia Korneev, M I Faktor, T B Cha. [Interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain]. Biulleten' eksperimental'noi biologii i meditsiny. vol 105. issue 1. 1988-03-23. PMID:2892547. |
the affinity for human cortex (3h) lsd binding sites was 10-fold lower in case of serotonin and 4-fold lower in case of buspirone and mj 138-05 than in the hippocamp. |
1988-03-23 |
2023-08-11 |
human |
| A Ia Korneev, M I Faktor, T B Cha. [Interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain]. Biulleten' eksperimental'noi biologii i meditsiny. vol 105. issue 1. 1988-03-23. PMID:2892547. |
however, the affinity for (3h) serotonin binding sites in the cortex was the same as in the hippocamp in case of serotonin and 12-15-fold lower than in the hippocamp in case of buspirone and mj 138-05. |
1988-03-23 |
2023-08-11 |
human |