| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| M B Emerit, S el Mestikawy, H Gozlan, J M Cossery, R Besselievre, A Marquet, M Hamo. Identification of the 5-HT1A receptor binding subunit in rat brain membranes using the photoaffinity probe [3H]8-methoxy-2-[N-n-propyl, N-3-(2-nitro-4-azidophenyl)aminopropyl]aminotetralin. Journal of neurochemistry. vol 49. issue 2. 1987-08-12. PMID:3598578. |
as expected of a possible correspondence between pi and 5-ht1a receptor binding sites, 3h labeling by the photoaffinity probe could be prevented by selective 5-ht1a ligands such as 8-hydroxy-2-(di-n-propylamino)tetralin, ipsapirone, buspirone, and gepirone and by n-ethylmaleimide, but not by the 5-ht2 antagonist ketanserin, noradrenaline- and dopamine-related drugs, monoamine oxidase inhibitors, and chlorimipramine. |
1987-08-12 |
2023-08-11 |
rat |
| B A McMillen, S M Scott, H L Williams, M K Sangher. Effects of gepirone, an aryl-piperazine anxiolytic drug, on aggressive behavior and brain monoaminergic neurotransmission. Naunyn-Schmiedeberg's archives of pharmacology. vol 335. issue 4. 1987-07-30. PMID:2439924. |
both buspirone and gepirone displaced [3h]-5ht from the 5ht1a binding site in the hippocampus with ic50 values of 10 and 58 nm, respectively. |
1987-07-30 |
2023-08-11 |
mouse |
| G A Kennett, C T Dourish, G Curzo. Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression. European journal of pharmacology. vol 134. issue 3. 1987-05-28. PMID:2883013. |
however, the 5-ht1a agonists buspirone and tvxq 7821 (ipsapirone) and the non-specific 5-ht agonist quipazine all possess similar properties to 8-oh-dpat in this test. |
1987-05-28 |
2023-08-11 |
rat |
| M D Tricklebank, J Neill, E J Kidd, J R Fozar. Mediation of the discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) by the putative 5-HT1A receptor. European journal of pharmacology. vol 133. issue 1. 1987-05-01. PMID:2881789. |
in contrast, both buspirone and tvx q 7821, which like 8-oh-dpat have high affinity and selectivity for the 5-ht1a recognition site, generalized to the 8-oh-dpat cue in a dose-dependent manner. |
1987-05-01 |
2023-08-11 |
rat |
| M D Tricklebank, J Neill, E J Kidd, J R Fozar. Mediation of the discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) by the putative 5-HT1A receptor. European journal of pharmacology. vol 133. issue 1. 1987-05-01. PMID:2881789. |
moreover, agonist activity at central 5-ht1a receptors may be an important mechanism contributing to the anxiolytic properties of buspirone and tvx q 7821. |
1987-05-01 |
2023-08-11 |
rat |
| R E Heuring, S J Peroutk. Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 7. issue 3. 1987-04-29. PMID:2951504. |
5-ht1a selective agents such as 8-oh-dpat, ipsapirone, and buspirone display micromolar affinities for these sites. |
1987-04-29 |
2023-08-11 |
rat |
| D G Spencer, J Trabe. The interoceptive discriminative stimuli induced by the novel putative anxiolytic TVX Q 7821: behavioral evidence for the specific involvement of serotonin 5-HT1A receptors. Psychopharmacology. vol 91. issue 1. 1987-04-06. PMID:2881318. |
following discrimination acquisition, tvx q 7821 administration resulted in drug-appropriate responding with an ed50 of 1.5 mg/kg, as did other substances with high affinity for the 5-ht1a receptor: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-oh-dpat, ed50 = 0.16 mg/kg), 5-methoxy-n,n-dimethyltryptamine (5-ome-dmt, ed50 = 2.5 mg/kg), and buspirone (ed50 = 5.4 mg/kg). |
1987-04-06 |
2023-08-11 |
rat |
| M J Rowan, R Anwy. Neurophysiological effects of buspirone and isapirone in the hippocampus: comparison with 5-hydroxytryptamine. European journal of pharmacology. vol 132. issue 1. 1987-04-01. PMID:2880731. |
these results suggest that buspirone and isapirone are agonists for 5-ht1a receptors in the hippocampus. |
1987-04-01 |
2023-08-11 |
rat |
| C P VanderMaelen, G K Matheson, R C Wilderman, L A Patterso. Inhibition of serotonergic dorsal raphe neurons by systemic and iontophoretic administration of buspirone, a non-benzodiazepine anxiolytic drug. European journal of pharmacology. vol 129. issue 1-2. 1986-12-11. PMID:2876903. |
since buspirone inhibits the firing of serotonergic dorsal raphe neurons and binds to 5-ht1a receptors, the present study supports the notion that central serotonergic systems may be involved in the therapeutic effects of anxiolytic drugs. |
1986-12-11 |
2023-08-11 |
rat |
| R W Ransom, K B Asarch, J C Shi. Photoaffinity labeling of the 5-hydroxytryptamine 1A receptor in rat hippocampus. Journal of neurochemistry. vol 47. issue 4. 1986-10-15. PMID:3746296. |
this incorporation could be blocked when membranes were incubated with 1 microm of several agents that have high affinity for 5-ht1a sites [5-ht, 8-hydroxy-2-(di-n-propylamino)tetraline, tvx q 7821, spiperone, buspirone, d-lysergic acid diethylamide, metergoline]. |
1986-10-15 |
2023-08-11 |
rat |
| L M Smith, S J Peroutk. Differential effects of 5-hydroxytryptamine1a selective drugs on the 5-HT behavioral syndrome. Pharmacology, biochemistry, and behavior. vol 24. issue 6. 1986-09-17. PMID:2942947. |
the effects of 8-hydroxy-2-(di-n-propyl-amino) tetralin (8-oh-dpat), 5-methoxy-n,n-dimethyltryptamine (5-meodmt), buspirone and isapirone were examined at 5-hydroxytryptamine1a (5-ht1a) binding sites and on the 5-ht behavioral syndrome in the rat. |
1986-09-17 |
2023-08-11 |
rat |
| S J Peroutka, S Huang, G S Alle. Canine basilar artery contractions mediated by 5-hydroxytryptamine1A receptors. The Journal of pharmacology and experimental therapeutics. vol 237. issue 3. 1986-07-16. PMID:2940360. |
first, drugs such as 8-hydroxy-2-(n,n-dipropylamino)tetralin n-(3-acetylaminophenyl)piperazine hydrochloride, 2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]-1,2-benziso-thiazol-3 -(2h)one-1,1-dioxidehydrochloride] and buspirone display 1.0 to 15 nm potency for the 5-ht1a subpopulation of 5-ht1 binding sites but are more than two orders of magnitude less potent at total 5-ht1 sites. |
1986-07-16 |
2023-08-11 |
rat |
| S J Peroutk. Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Biological psychiatry. vol 20. issue 9. 1985-10-04. PMID:2862927. |
buspirone (ic50 = 24 nm) and tvx q 7821 (ic50 = 9.5 nm) display the highest affinity for 5-hydroxytryptamine1a (5-ht1a) binding sites labeled by 3h-8-hydroxy-2-(di-n-pro-pylamino) tetralin (dpat). |
1985-10-04 |
2023-08-11 |
Not clear |
| S J Peroutk. Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Biological psychiatry. vol 20. issue 9. 1985-10-04. PMID:2862927. |
these results suggest that the anxiolytic effects of buspirone and tvx q 7821 may be mediated by central 5-ht1a receptors. |
1985-10-04 |
2023-08-11 |
Not clear |