| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| M R Briejer, L M Akkermans, R A Lefebvre, J A Schuurke. Novel 5-HT2-like receptor mediates neurogenic relaxation of the guinea-pig proximal colon. European journal of pharmacology. vol 279. issue 2-3. 1995-11-06. PMID:7556392. |
the curve to 5-ht was not affected by pargyline, citalopram, phentolamine, or by the 5-ht4 receptor antagonists 2-methoxy-4-amino-5-chloro-benzoic acid 2-(diethylamino)ethyl ester (sdz 205-557) and (1-butyl-4-piperidinylmethyl)-8-amino-7-chloro-1,4-benzodioxan+ ++-5-carboxylate (sb 204070). |
1995-11-06 |
2023-08-12 |
Not clear |
| E Leung, D Blissard, M F Jett, R M Egle. Investigation of the 5-hydroxytryptamine receptor mediating the "transient" short-circuit current response in guinea-pig ileal mucosa. Naunyn-Schmiedeberg's archives of pharmacology. vol 351. issue 6. 1995-10-19. PMID:7675117. |
in the presence of methysergide, the high potency phase 5-ht response was mimicked by 5-methoxytryptamine (5-meot) and the selective 5-ht4 agonist sc-53116 but not by bimu 8. |
1995-10-19 |
2023-08-12 |
Not clear |
| J J Lucas, R He. New players in the 5-HT receptor field: genes and knockouts. Trends in pharmacological sciences. vol 16. issue 7. 1995-10-11. PMID:7667899. |
in recent years, cloning has revealed the existence of no less than 14 mammalian 5-ht receptors, as well as evidence that isoforms of the 5-ht4 and 5-ht7 receptors are generated by alternative splicing. |
1995-10-11 |
2023-08-12 |
Not clear |
| P R Saxen. Serotonin receptors: subtypes, functional responses and therapeutic relevance. Pharmacology & therapeutics. vol 66. issue 2. 1995-10-10. PMID:7667401. |
thus, based on operational criteria (agonist and antagonist rank order), as well as transduction mechanisms involved and the structure of the receptor protein, the nomenclature committee of the serotonin club has proposed the following classification and nomenclature: the main receptor types 5-ht1 to 5-ht4, recombinant receptors (e.g. |
1995-10-10 |
2023-08-12 |
Not clear |
| F S Tam, K Hillier, K T Bunce, C Grossma. Differences in response to 5-HT4 receptor agonists and antagonists of the 5-HT4-like receptor in human colon circular smooth muscle. British journal of pharmacology. vol 115. issue 1. 1995-09-26. PMID:7647972. |
the azabicycloalkyl benzimidazolones, bimu 8 and bimu 1, which have 5-ht4 receptor stimulant properties, inhibited motility with ec50 values of 0.76 microm and 3.19 microm respectively and their emax values were not significantly different from 5-ht (ec50, 0.13 microm). |
1995-09-26 |
2023-08-12 |
human |
| F S Tam, K Hillier, K T Bunce, C Grossma. Differences in response to 5-HT4 receptor agonists and antagonists of the 5-HT4-like receptor in human colon circular smooth muscle. British journal of pharmacology. vol 115. issue 1. 1995-09-26. PMID:7647972. |
the 5-ht4 receptor antagonist, dau 6285 (1-10 microm), displaced the 5-ht concentration-response curve to the right in a parallel concentration-dependent manner without depressing the maximum. |
1995-09-26 |
2023-08-12 |
human |
| F S Tam, K Hillier, K T Bunce, C Grossma. Differences in response to 5-HT4 receptor agonists and antagonists of the 5-HT4-like receptor in human colon circular smooth muscle. British journal of pharmacology. vol 115. issue 1. 1995-09-26. PMID:7647972. |
the high affinity selective 5-ht4 receptor antagonist, gr 113808, at a concentration of 3 nm displaced the 5-ht concentration-response curve in a parallel manner giving an apparent pkb estimate of 8.9 +/- 0.24. |
1995-09-26 |
2023-08-12 |
human |
| P G McLean, I M Coupar, P Molenaa. A comparative study of functional 5-HT4 receptors in human colon, rat oesophagus and rat ileum. British journal of pharmacology. vol 115. issue 1. 1995-09-26. PMID:7647983. |
the pharmacological properties of 5-hydroxytryptamine (5-ht), the 5-ht4 receptor agonists, dau 6236 and sc 53116 and the 5-ht4 receptor antagonist, gr 1130808, were studied in the rat oesophagus, rat ileum and human colon. |
1995-09-26 |
2023-08-12 |
human |
| P G McLean, I M Coupar, P Molenaa. A comparative study of functional 5-HT4 receptors in human colon, rat oesophagus and rat ileum. British journal of pharmacology. vol 115. issue 1. 1995-09-26. PMID:7647983. |
gr 113808 competitively antagonized the 5-ht4 receptor-mediated relaxation of the rat oesophagus with a pa2 value of 8.59 (8.18-9.00) against 5-ht and 9.05 (8.79-9.31) against sc 53116. |
1995-09-26 |
2023-08-12 |
human |
| M R Briejer, L M Akkermans, J A Schuurke. Interactions of serotonin with multiple receptors and neurotransmitters in the guinea-pig isolated colon. Archives internationales de pharmacodynamie et de therapie. vol 329. issue 1. 1995-09-14. PMID:7639614. |
by means of the neurotoxin, tetrodotoxin, the muscarinic cholinoceptor antagonist, atropine, and selective 5-ht receptor antagonists, it was shown that the contractions to 5-ht are mediated by 5-ht2a receptors, localized on the smooth muscle, and by 5-ht3 and 5-ht4 receptors, localized on cholinergic nerves. |
1995-09-14 |
2023-08-12 |
Not clear |
| M R Briejer, G J Veen, L M Akkermans, R A Lefebvre, J A Schuurke. Cisapride and structural analogs selectively enhance 5-hydroxytryptamine (5-HT)-induced purinergic neurotransmission in the guinea pig proximal colon. The Journal of pharmacology and experimental therapeutics. vol 274. issue 2. 1995-09-08. PMID:7636723. |
in the continuous presence of ketanserin (0.3 microm) and tropisetron (3 microm) to block contractions via 5-ht2a, 5-ht3 and 5-ht4 receptors, 5-ht induced relaxations that yielded a biphasic concentration-response curve. |
1995-09-08 |
2023-08-12 |
Not clear |
| N Bonhomme, P De Deurwaèrdere, M Le Moal, U Spampinat. Evidence for 5-HT4 receptor subtype involvement in the enhancement of striatal dopamine release induced by serotonin: a microdialysis study in the halothane-anesthetized rat. Neuropharmacology. vol 34. issue 3. 1995-09-01. PMID:7543190. |
evidence for 5-ht4 receptor subtype involvement in the enhancement of striatal dopamine release induced by serotonin: a microdialysis study in the halothane-anesthetized rat. |
1995-09-01 |
2023-08-12 |
rat |
| N Bonhomme, P De Deurwaèrdere, M Le Moal, U Spampinat. Evidence for 5-HT4 receptor subtype involvement in the enhancement of striatal dopamine release induced by serotonin: a microdialysis study in the halothane-anesthetized rat. Neuropharmacology. vol 34. issue 3. 1995-09-01. PMID:7543190. |
these results demonstrate that in vivo 5-ht exerts a facilitatory influence on striatal da release and that the 5-ht4, but not the 5-ht1, 5-ht2 or 5-ht3, receptor subtype is implicated, at least partially, in this effect. |
1995-09-01 |
2023-08-12 |
rat |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608898. |
the serotonin 5-ht4 receptor. |
1995-08-17 |
2023-08-12 |
Not clear |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608898. |
a conformational study of the 5-ht4 receptor agonists serotonin and zacopride led to the identification of an initial pharmacophore and to the definition of a three-dimensional map of the 5-ht4 agonist recognition site. |
1995-08-17 |
2023-08-12 |
Not clear |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608899. |
the serotonin 5-ht4 receptor. |
1995-08-17 |
2023-08-12 |
Not clear |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608899. |
their selectivity for the 5-ht4 receptor was established by examining their affinity for other 5-ht receptors using radioligand-binding techniques. |
1995-08-17 |
2023-08-12 |
Not clear |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608899. |
for example, 1b,d were found to be the most potent, full 5-ht4 receptor agonist described so far (ec50 = 0.5 and 0.8 nm, respectively), being 6 and 4 times more potent than serotonin itself. |
1995-08-17 |
2023-08-12 |
Not clear |
| K H Buchheit, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Matte. The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. Journal of medicinal chemistry. vol 38. issue 13. 1995-08-17. PMID:7608899. |
on the other hand, 5b and 1h appeared as partial 5-ht4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, ki = 12 nm) to and 300-fold higher (1h, ki = 0.04 nm) than serotonin. |
1995-08-17 |
2023-08-12 |
Not clear |
| T Takahashi, J K Ward, S Tadjkarimi, M H Yacoub, P J Barnes, M G Belvis. 5-Hydroxytryptamine facilitates cholinergic bronchoconstriction in human and guinea pig airways. American journal of respiratory and critical care medicine. vol 152. issue 1. 1995-08-10. PMID:7599849. |
the 5-ht3/4 and 5-ht3 antagonists, ics 205-930 and ondansetron, inhibited the effect of 5-ht competitively (pa2 values of 7.3 and 7.1, respectively); methiothepin (5-ht1/2c antagonist), ketanserin (5-ht2a antagonist), and gr 113808a (5-ht4 antagonist) had no effect. |
1995-08-10 |
2023-08-12 |
human |