| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| F Gilbert, C Brazell, M D Tricklebank, S M Stah. Activation of the 5-HT1A receptor subtype increases rat plasma ACTH concentration. European journal of pharmacology. vol 147. issue 3. 1988-07-25. PMID:2897920. |
similar increases of plasma acth were induced by other 5-ht1a receptor ligands (buspirone, ipsapirone and gepirone). |
1988-07-25 |
2023-08-11 |
rat |
| 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 |
| D Hoyer, C Waeber, A Pazos, A Probst, J M Palacio. Identification of a 5-HT1 recognition site in human brain membranes different from 5-HT1A, 5-HT1B and 5-HT1C sites. Neuroscience letters. vol 85. issue 3. 1988-06-02. PMID:2966310. |
in contrast, these sites showed low affinity for drugs with high affinity and/or selectivity for 5-ht1a (8-oh-dpat, buspirone), 5-ht1b (21-009, ru 24969), 5-ht1c (mesulergine, mianserin) and 5-ht2 sites (ketanserin, cinanserin). |
1988-06-02 |
2023-08-11 |
human |
| B A McMillen, J K Chamberlain, J P DaVanz. Effects of housing and muricidal behavior on serotonergic receptors and interactions with novel anxiolytic drugs. Journal of neural transmission. vol 71. issue 2. 1988-04-18. PMID:2894404. |
buspirone and gepirone, non-benzodiazepine anxiolytics that stimulate serotonergic receptors (5ht1a) and inhibit isolation-induced intraspecies aggression, were tested for inhibition of muricidal behavior by isolated rats. |
1988-04-18 |
2023-08-11 |
mouse |
| 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. |
its main differences with the 5-ht1a receptor in hippocampal neurons are as follows: 1) 8-oh-dpat was only a poor partial agonist in cortical neurons, whereas it was the best full agonist in hippocampal neurons; and 2) metergoline and methysergide as well as the anxiolytic drugs, ipsapirone and buspirone, which were potent agonists in hippocampal neurons, were competitive antagonists in cortical neurons. |
1988-03-24 |
2023-08-11 |
mouse |
| M D Mauk, S J Peroutka, J D Kocsi. Buspirone attenuates synaptic activation of hippocampal pyramidal cells. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 8. issue 1. 1988-03-08. PMID:3339401. |
the actions of 5-hydroxytryptamine (5-ht) and buspirone, an anxiolytic agent that displays high and selective affinity for 5-ht1a receptor sites, on synaptic activation of hippocampal ca1 pyramidal cells were studied in vitro. |
1988-03-08 |
2023-08-11 |
Not clear |
| F Gilbert, C T Douris. Effects of the novel anxiolytics gepirone, buspirone and ipsapirone on free feeding and on feeding induced by 8-OH-DPAT. Psychopharmacology. vol 93. issue 3. 1988-03-03. PMID:2893412. |
the effects of the novel anxiolytics gepirone, buspirone and ipsapirone on free feeding and on feeding induced by the 5-ht1a receptor agonist, 8-hydroxy-2-(di-n-propylamino) tetralin (8-oh-dpat), were examined. |
1988-03-03 |
2023-08-11 |
rat |
| F Gilbert, C T Douris. Effects of the novel anxiolytics gepirone, buspirone and ipsapirone on free feeding and on feeding induced by 8-OH-DPAT. Psychopharmacology. vol 93. issue 3. 1988-03-03. PMID:2893412. |
gepirone dose-dependently increased feeding 2 and 4 h after injection, the magnitude of the response being larger than previously observed with any other 5-ht1a receptor ligand. |
1988-03-03 |
2023-08-11 |
rat |
| S Pellow, A L Johnston, S E Fil. Selective agonists and antagonists for 5-hydroxytryptamine receptor subtypes, and interactions with yohimbine and FG 7142 using the elevated plus-maze test in the rat. The Journal of pharmacy and pharmacology. vol 39. issue 11. 1988-02-26. PMID:2892916. |
two 5-ht1a receptor ligands, buspirone (4 and 8 mg kg-1) and ipsapirone (2.5-10 mg kg-1) and the 5-ht1 agonist, ru 24969 (0.1875-1.5 mg kg-1) significantly reduced only the percentage of time spent on the open arms. |
1988-02-26 |
2023-08-11 |
rat |
| S J Offord, G A Ordway, A Fraze. Application of [125I]iodocyanopindolol to measure 5-hydroxytryptamine1B receptors in the brain of the rat. The Journal of pharmacology and experimental therapeutics. vol 244. issue 1. 1988-02-24. PMID:3335996. |
by contrast, drugs thought to be selective for the 5-ht1a receptor (e.g., 8-hydroxy-2-(di-n-propylamino)tetralin, buspirone and spiperone) showed very weak affinity for the binding site labeled with [125i]icyp. |
1988-02-24 |
2023-08-11 |
rat |
| J R Ieni, L R Meyerso. The 5-HT1A receptor probe [3H]8-OH-DPAT labels the 5-HT transporter in human platelets. Life sciences. vol 42. issue 3. 1988-02-23. PMID:2961966. |
for example, 8-oh-dpat 5ht1a had an ic50 of 117 nm; tfmpp 5ht1b (2.3 microm0 and papp 1a + 5ht2 (9 microm); ipsapirone 5ht1a (21.1 microm) and buspirone 5ht1a (greater than 100 microm); ketanserin 5ht2 (greater than 100 microm); 5-ht uptake inhibitors: paroxetine (13 nm); chlorimipramine (73 nm) and fluoxetine (653 nm). |
1988-02-23 |
2023-08-11 |
human |
| S J Cooper, A Des. Benzodiazepines and putative 5-HT1A agonists increase hypertonic saline consumption in rehydrating rats. Pharmacology, biochemistry, and behavior. vol 28. issue 2. 1988-01-13. PMID:2825218. |
three putative 5-ht1a agonists, proposed as nonbenzodiazepine-related anxiolytics, were also tested: the highly selective 8-oh-dpat, gepirone and ipsapirone (tvx q 7821). |
1988-01-13 |
2023-08-11 |
rat |
| S J Coope. Novel benzodiazepine receptor ligands stimulate intake of hypertonic NaCl solution in rehydrating rats. Pharmacology, biochemistry, and behavior. vol 27. issue 3. 1987-10-27. PMID:2889219. |
the putative 5-ht1a agonist, buspirone, produced only a dose-dependent decrease in saline intake. |
1987-10-27 |
2023-08-11 |
rat |
| G A Kennett, M Marcou, C T Dourish, G Curzo. Single administration of 5-HT1A agonists decreases 5-HT1A presynaptic, but not postsynaptic receptor-mediated responses: relationship to antidepressant-like action. European journal of pharmacology. vol 138. issue 1. 1987-10-16. PMID:2442002. |
the 5-ht1a agonists, 8-hydroxy-2-(di-n-propylamino) tetralin (8-oh-dpat), buspirone or tvxq 7821 (ipsapirone) but not the 5-ht1b agonist ru 24969, attenuated the hyperphagic response to 8-oh-dpat administered on the next day. |
1987-10-16 |
2023-08-11 |
Not clear |
| K A Cunningham, P M Callahan, J B Appe. Discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT): implications for understanding the actions of novel anxiolytics. European journal of pharmacology. vol 138. issue 1. 1987-10-16. PMID:2887435. |
the similar stimulus properties of 8-ohdpat and the novel anxiolytics (buspirone, ipsapirone) are mirrored by the common abilities of these agents to selectively inhibit 5-ht1a binding and release punished responding. |
1987-10-16 |
2023-08-11 |
rat |
| K A Cunningham, P M Callahan, J B Appe. Discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT): implications for understanding the actions of novel anxiolytics. European journal of pharmacology. vol 138. issue 1. 1987-10-16. PMID:2887435. |
thus, the subpopulation of 5-ht1a receptors may mediate the behavioral effects of these compounds in animals and, in turn, the anxiolytic effects of buspirone and ipsapirone in humans. |
1987-10-16 |
2023-08-11 |
rat |
| M Joëls, P Shinnick-Gallagher, J P Gallaghe. Effect of serotonin and serotonin analogues on passive membrane properties of lateral septal neurons in vitro. Brain research. vol 417. issue 1. 1987-10-13. PMID:2957026. |
two other 5-ht1a analogues, tvx q 7821 and buspirone, could also mimick the effect of 5-ht. |
1987-10-13 |
2023-08-11 |
rat |
| F D Yocca, D K Hyslop, D W Smith, S Maayan. BMY 7378, a buspirone analog with high affinity, selectivity and low intrinsic activity at the 5-HT1A receptor in rat and guinea pig hippocampal membranes. European journal of pharmacology. vol 137. issue 2-3. 1987-09-24. PMID:2886356. |
bmy 7378, a buspirone analog with high affinity, selectivity and low intrinsic activity at the 5-ht1a receptor in rat and guinea pig hippocampal membranes. |
1987-09-24 |
2023-08-11 |
rat |
| J Bockaert, A Dumuis, R Bouhelal, M Sebben, R N Cor. Piperazine derivatives including the putative anxiolytic drugs, buspirone and ipsapirone, are agonists at 5-HT1A receptors negatively coupled with adenylate cyclase in hippocampal neurons. Naunyn-Schmiedeberg's archives of pharmacology. vol 335. issue 5. 1987-09-11. PMID:2886925. |
piperazine derivatives including the putative anxiolytic drugs, buspirone and ipsapirone, are agonists at 5-ht1a receptors negatively coupled with adenylate cyclase in hippocampal neurons. |
1987-09-11 |
2023-08-11 |
mouse |