| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| E W Taylor, S P Duckles, D L Nelso. Dissociation constants of serotonin agonists in the canine basilar artery correlate to Ki values at the 5-HT1A binding site. The Journal of pharmacology and experimental therapeutics. vol 236. issue 1. 1986-02-20. PMID:2934545. |
logs of these ka values did not correlate with log ki values for the inhibition of binding of the 5-ht2 ligand [3h] ketanserin (r = 0.2253, p greater than .05) or log ic50 values for inhibition of [3h]5-ht binding (r = 0.5732, p greater than 0.05), which labels both 5-ht1a and 5-ht1b sites. |
1986-02-20 |
2023-08-11 |
Not clear |
| M L Cohen, L A Wittenaue. Further evidence that the serotonin receptor in the rat stomach fundus is not 5HT1A or 5HT1B. Life sciences. vol 38. issue 1. 1986-02-18. PMID:3941588. |
meta chlorophenylpiperazine (cpp) and meta trifluoromethylphenylpiperazine (tfmpp), selective ligands for the 5ht1b receptor and ly165163, a selective ligand for the 5ht1a receptor, have been evaluated for their agonist and antagonist activity at serotonin receptors in the rat stomach fundus. |
1986-02-18 |
2023-08-11 |
rat |
| M L Cohen, L A Wittenaue. Further evidence that the serotonin receptor in the rat stomach fundus is not 5HT1A or 5HT1B. Life sciences. vol 38. issue 1. 1986-02-18. PMID:3941588. |
the affinity for serotonin receptors in the rat fundus was similar for all three phenylpiperazines in spite of the reported selectivity of mcpp and tfmpp for 5ht1b and of ly165163 for 5ht1a receptors. |
1986-02-18 |
2023-08-11 |
rat |
| M L Cohen, L A Wittenaue. Further evidence that the serotonin receptor in the rat stomach fundus is not 5HT1A or 5HT1B. Life sciences. vol 38. issue 1. 1986-02-18. PMID:3941588. |
furthermore, the affinity of these agents for serotonin receptors in the rat stomach fundus did not agree with their reported affinity for either 5ht1a or 5ht1b binding sites in rat cortical membranes. |
1986-02-18 |
2023-08-11 |
rat |
| M L Cohen, L A Wittenaue. Further evidence that the serotonin receptor in the rat stomach fundus is not 5HT1A or 5HT1B. Life sciences. vol 38. issue 1. 1986-02-18. PMID:3941588. |
thus, the similarity in affinities of these phenylpiperazine derivatives for serotonin receptors mediating contraction in the rat fundus along with their different affinities for 5ht1a and 5ht1b binding sites argues against the possibility that the serotonin receptor in the rat fundus is of the 5ht1a or 5ht1b subtype of serotonin receptor. |
1986-02-18 |
2023-08-11 |
rat |
| R W Ransom, K B Asarch, J C Shi. [3H]1-[2-(4-aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine: a selective radioligand for 5-HT1A receptors in rat brain. Journal of neurochemistry. vol 46. issue 1. 1986-01-21. PMID:2933490. |
1-[2-(4-aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine (papp) inhibits [3h]5-hydroxytryptamine (5-ht, serotonin) binding to 5-ht1a and 5-ht1b sites in rat brain with apparent equilibrium dissociation constants (kd) of 2.9 and 328 nm, respectively. |
1986-01-21 |
2023-08-11 |
rat |
| R W Ransom, K B Asarch, J C Shi. [3H]1-[2-(4-aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine: a selective radioligand for 5-HT1A receptors in rat brain. Journal of neurochemistry. vol 46. issue 1. 1986-01-21. PMID:2933490. |
[3h]papp was synthesized, its binding to central serotonin receptors was examined, and its potential usefulness as a 5-ht1a receptor radioligand was evaluated. |
1986-01-21 |
2023-08-11 |
rat |
| R W Ransom, K B Asarch, J C Shi. [3H]1-[2-(4-aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine: a selective radioligand for 5-HT1A receptors in rat brain. Journal of neurochemistry. vol 46. issue 1. 1986-01-21. PMID:2933490. |
spiperone and 8-hydroxy-2-(di-n-propylamino)tetralin, two compounds that discriminate [3h]5-ht binding to 5-ht1a and 5-ht1b sites, inhibited [3h]papp binding in accordance with their much higher affinities for the 5-ht1a receptor subtype. |
1986-01-21 |
2023-08-11 |
rat |
| P J Monroe, D J Smit. Demonstration of an autoreceptor modulating the release of [3H]5-hydroxytryptamine from a synaptosomal-rich spinal cord tissue preparation. Journal of neurochemistry. vol 45. issue 6. 1985-12-16. PMID:3877146. |
spiperone, in a concentration that approximated the affinity constant of 5-ht1a sites for the drug, was ineffective in altering the ability of exogenous 5-ht to modulate k+-stimulated [3h]5-ht release. |
1985-12-16 |
2023-08-11 |
Not clear |
| G M Goodwin, R J De Souza, A R Gree. Presynaptic serotonin receptor-mediated response in mice attenuated by antidepressant drugs and electroconvulsive shock. Nature. vol 317. issue 6037. 1985-11-14. PMID:2931606. |
recently a new drug, 8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat), has been identified which shows high selectivity for binding to 5-ht1 (possibly 5-ht1a) receptors and which binds to presynaptic serotonin autoreceptors in some regions of rat brain. |
1985-11-14 |
2023-08-11 |
mouse |
| S J Peroutk. Selective labeling of 5-HT1A and 5-HT1B binding sites in bovine brain. Brain research. vol 344. issue 1. 1985-11-12. PMID:4041865. |
drug interactions with serotonin(1a) 5-ht1a and serotonin(1b) (5-ht1b) binding sites were analyzed in bovine brain membranes. |
1985-11-12 |
2023-08-11 |
cattle |
| S J Peroutk. Selective labeling of 5-HT1A and 5-HT1B binding sites in bovine brain. Brain research. vol 344. issue 1. 1985-11-12. PMID:4041865. |
5-ht, bufotenine, n,n-dimethyltryptamine (dmt) and quipazine were only slightly more potent at the 5-ht1a binding site. |
1985-11-12 |
2023-08-11 |
cattle |
| D Verge, G Daval, A Patey, H Gozlan, S el Mestikawy, M Hamo. Presynaptic 5-HT autoreceptors on serotonergic cell bodies and/or dendrites but not terminals are of the 5-HT1A subtype. European journal of pharmacology. vol 113. issue 3. 1985-11-08. PMID:2931289. |
presynaptic 5-ht autoreceptors on serotonergic cell bodies and/or dendrites but not terminals are of the 5-ht1a subtype. |
1985-11-08 |
2023-08-11 |
Not clear |
| K Gradin, A Pettersson, T Hedner, B Persso. Acute administration of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), a selective 5-HT-receptor agonist, causes a biphasic blood pressure response and a bradycardia in the normotensive Sprague-Dawley rat and in the spontaneously hypertensive rat. Journal of neural transmission. vol 62. issue 3-4. 1985-09-27. PMID:3161997. |
8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat) is a new serotonin (5-ht) receptor agonist that binds selectively to the 5-ht1a binding site. |
1985-09-27 |
2023-08-11 |
rat |
| H N Doods, H O Kalkman, A De Jonge, M J Thoolen, B Wilffert, P B Timmermans, P A Van Zwiete. Differential selectivities of RU 24969 and 8-OH-DPAT for the purported 5-HT1A and 5-HT1B binding sites. Correlation between 5-HT1A affinity and hypotensive activity. European journal of pharmacology. vol 112. issue 3. 1985-09-16. PMID:3160596. |
following addition of spiperone (1 microm) as a selective ligand for the putative 5-ht1a recognition site of [3h]5-ht, the displacement curve of ru 24969 underwent a leftward shift, whereas spiperone induced a shift to the right for the displacement curve of 8-oh-dpat. |
1985-09-16 |
2023-08-11 |
rat |
| H N Doods, H O Kalkman, A De Jonge, M J Thoolen, B Wilffert, P B Timmermans, P A Van Zwiete. Differential selectivities of RU 24969 and 8-OH-DPAT for the purported 5-HT1A and 5-HT1B binding sites. Correlation between 5-HT1A affinity and hypotensive activity. European journal of pharmacology. vol 112. issue 3. 1985-09-16. PMID:3160596. |
based on the proposal that the 5-ht1a site corresponds to the high affinity site of 8-oh-dpat and the low affinity site of ru 24969, it is hypothesized that the late depressor phase of 5-ht agonists in rats is mediated by activation of peripheral (vascular) 5-ht receptors which have similarities with the 5-ht1a subtype of central 5-ht1 recognition site. |
1985-09-16 |
2023-08-11 |
rat |
| G M Goodwin, A R Gree. A behavioural and biochemical study in mice and rats of putative selective agonists and antagonists for 5-HT1 and 5-HT2 receptors. British journal of pharmacology. vol 84. issue 3. 1985-06-20. PMID:2580582. |
radioligand binding techniques have demonstrated the existence of 5-hydroxytryptamine (5-ht) binding subtypes: 5-ht2, 5-ht1a and 5-ht1b. |
1985-06-20 |
2023-08-11 |
mouse |
| M D Hall, S el Mestikawy, M B Emerit, L Pichat, M Hamon, H Gozla. [3H]8-hydroxy-2-(di-n-propylamino)tetralin binding to pre- and postsynaptic 5-hydroxytryptamine sites in various regions of the rat brain. Journal of neurochemistry. vol 44. issue 6. 1985-06-18. PMID:3157780. |
the postsynaptic hippocampal [3h]8-oh-dpat binding sites are probably identical to the 5-ht1a subsites, but the relationship between the presynaptic binding sites and the presynaptic autoreceptors controlling 5-ht release deserves further investigation. |
1985-06-18 |
2023-08-11 |
rat |
| M D Tricklebank, C Forler, J R Fozar. The involvement of subtypes of the 5-HT1 receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino)tetralin in the rat. European journal of pharmacology. vol 106. issue 2. 1985-04-26. PMID:6241568. |
the centrally active 5-ht receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat) has a high affinity for the 5-ht1a subtype of the 5-ht1 recognition site in cerebral membranes and, in the rat, induces most aspects of the '5-ht behavioural syndrome' including hyperlocomotion, head weaving, a flat body posture and reciprocal forepaw treading. |
1985-04-26 |
2023-08-12 |
rat |
| M B Emerit, H Gozlan, M D Hall, M Hamon, A Marque. Irreversible blockade of central 5-HT binding sites by 8-methoxy-2'-chloro-PAT. Biochemical pharmacology. vol 34. issue 6. 1985-04-17. PMID:3156602. |
although 8-methoxy-2'-chloro-pat bound irreversibly to different classes of 5-ht binding sites (5-ht1a, 5-ht1b, presynaptic sites), it can be considered a selective alkylating agent, since it exerted no action on 3h-spiperone binding to 5-ht2 sites, 3h-muscimol binding to gaba sites, or 3h-flunitrazepam binding to benzodiazepine sites. |
1985-04-17 |
2023-08-11 |
rat |