| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| G W John, P J Pauwels, M Perez, S Halazy, B Le Grand, Y Verscheure, J P Valentin, C Palmier, T Wurch, P Chopin, M Marien, M S Kleven, W Koek, M B Assie, E Carilla-Durand, J P Tarayre, F C Colpaer. F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. The Journal of pharmacology and experimental therapeutics. vol 290. issue 1. 1999-07-26. PMID:10381763. |
f 11356 has subnanomolar affinity for cloned human and nonhuman 5-ht1b and 5-ht1d receptors, and its affinity for 5-ht1a and other 5-ht receptors, including the 5-ht1f subtype, is 50-fold lower and micromolar, respectively. |
1999-07-26 |
2023-08-12 |
human |
| G W John, P J Pauwels, M Perez, S Halazy, B Le Grand, Y Verscheure, J P Valentin, C Palmier, T Wurch, P Chopin, M Marien, M S Kleven, W Koek, M B Assie, E Carilla-Durand, J P Tarayre, F C Colpaer. F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. The Journal of pharmacology and experimental therapeutics. vol 290. issue 1. 1999-07-26. PMID:10381763. |
in c6 cells expressing human 5-ht1b or human 5-ht1d receptors, f 11356 was the most potent compound in inhibiting forskolin-induced cyclic amp formation (pd2 = 8.9 and 9.6), and in contrast to tryptamine and derivatives, it produced maximal enhancement of [35s]guanosine-5'-o-(3-thio)triphosphate-specific binding equivalent to 5-ht. |
1999-07-26 |
2023-08-12 |
human |
| D D Mitsikostas, M Sanchez del Rio, M A Moskowitz, C Waebe. Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. European journal of pharmacology. vol 369. issue 3. 1999-06-29. PMID:10225363. |
sumatriptan's effects might be mediated by 5-ht1b, 5-ht1d or 5-ht1f receptors. |
1999-06-29 |
2023-08-12 |
rat |
| W D Hirst, N Y Cheung, M Rattray, G W Price, G P Wilki. Cultured astrocytes express messenger RNA for multiple serotonin receptor subtypes, without functional coupling of 5-HT1 receptor subtypes to adenylyl cyclase. Brain research. Molecular brain research. vol 61. issue 1-2. 1999-06-10. PMID:9795156. |
the functional expression of 5-ht1 receptor subtypes was investigated by measuring the ability of 5-ht1 receptor agonists: 8-oh-dpat (5-ht1a receptors), ru24969 (5-ht1a, 5-ht1b, 5-ht1d, and 5-ht1f receptors) or sumatriptan (5-ht1b, 5-ht1d, and 5-ht1f receptors) to modulate forskolin or isoproterenol stimulated camp production. |
1999-06-10 |
2023-08-12 |
rat |
| C Napier, M Stewart, H Melrose, B Hopkins, A McHarg, R Walli. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. European journal of pharmacology. vol 368. issue 2-3. 1999-06-01. PMID:10193663. |
characterisation of the 5-ht receptor binding profile of eletriptan and kinetics of [3h]eletriptan binding at human 5-ht1b and 5-ht1d receptors. |
1999-06-01 |
2023-08-12 |
human |
| C Napier, M Stewart, H Melrose, B Hopkins, A McHarg, R Walli. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. European journal of pharmacology. vol 368. issue 2-3. 1999-06-01. PMID:10193663. |
eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-ht1b, 5-ht1d and putative 5-ht1f receptor. |
1999-06-01 |
2023-08-12 |
human |
| C Napier, M Stewart, H Melrose, B Hopkins, A McHarg, R Walli. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. European journal of pharmacology. vol 368. issue 2-3. 1999-06-01. PMID:10193663. |
kinetic studies comparing the binding of [3h]eletriptan and [3h]sumatriptan to the human recombinant 5-ht1b and 5-ht1d receptors expressed in hela cells revealed that both radioligands bound with high specificity (>90%) and reached equilibrium within 10-15 min. |
1999-06-01 |
2023-08-12 |
human |
| C Napier, M Stewart, H Melrose, B Hopkins, A McHarg, R Walli. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. European journal of pharmacology. vol 368. issue 2-3. 1999-06-01. PMID:10193663. |
however, [3h]eletriptan had over 6-fold higher affinity than [3h]sumatriptan at the 5-ht1d receptor (k(d)): 0.92 and 6.58 nm, respectively) and over 3-fold higher affinity than [3h]sumatriptan at the 5-ht1b receptor (k(d): 3.14 and 11.07 nm, respectively). |
1999-06-01 |
2023-08-12 |
human |
| C Napier, M Stewart, H Melrose, B Hopkins, A McHarg, R Walli. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. European journal of pharmacology. vol 368. issue 2-3. 1999-06-01. PMID:10193663. |
these data indicate that eletriptan is a potent ligand at the human 5-ht1b, 5-ht1d, and 5-ht1f receptors and are consistent with its potent vasoconstrictor activity and use as a drug for the acute treatment of migraine headache. |
1999-06-01 |
2023-08-12 |
human |
| A J Schee. [Pharmacy-clinic medication of the month. Naratriptan (naramig)]. Revue medicale de Liege. vol 54. issue 3. 1999-05-28. PMID:10321110. |
naratriptan, launched by glaxo wellcome under the trade name naramig, is a potent and selective agonist of 5-ht1b and 5-ht1d vascular receptors. |
1999-05-28 |
2023-08-12 |
Not clear |
| D S Dupuis, M Perez, S Halazy, F C Colpaert, P J Pauwel. Magnitude of 5-HT1B and 5-HT1A receptor activation in guinea-pig and rat brain: evidence from sumatriptan dimer-mediated [35S]GTPgammaS binding responses. Brain research. Molecular brain research. vol 67. issue 1. 1999-05-21. PMID:10101238. |
dimerization of sumatriptan increased the binding affinity for h 5-ht1b (pki: 9.22 vs. 7.79 for sumatriptan), h 5-ht1d (9.07 vs. 8.08) and also h 5-ht1a receptors (7.80 vs. 6.40), while the binding affinity for h 5-ht1e (6.67 vs. 6.19) and h 5-ht1f (7.37 vs. 7.78) receptors was not affected. |
1999-05-21 |
2023-08-12 |
rat |
| B Le Grand, A Panissié, P J Pauwels, G W Joh. Activation of recombinant h 5-HT1B and h 5-HT1D receptors stably expressed in C6 glioma cells produces increases in Ca2+-dependent K+ current. Naunyn-Schmiedeberg's archives of pharmacology. vol 358. issue 6. 1999-04-29. PMID:9879718. |
in c6 glioma cells expressing either recombinant h 5-ht1b or h 5-ht1d receptors, sumatriptan similarly increased ik in a concentration-dependent manner (maximum increase 19.4+/-7.2%, n=8, p<0.05 and 25.1+/-3.9%, n=6, p<0.001, respectively) with ec50 values (geometric mean with 95% confidence intervals in parentheses) of 56.3 nm (7.9-140 nm) and 68.7 nm (16-120 nm), respectively. |
1999-04-29 |
2023-08-12 |
Not clear |
| B Le Grand, A Panissié, P J Pauwels, G W Joh. Activation of recombinant h 5-HT1B and h 5-HT1D receptors stably expressed in C6 glioma cells produces increases in Ca2+-dependent K+ current. Naunyn-Schmiedeberg's archives of pharmacology. vol 358. issue 6. 1999-04-29. PMID:9879718. |
sumatriptan failed to elicit increases in ik in non-transfected cells, confirming a specific involvement of the respective membrane h 5-ht1b and h 5-ht1d receptors in transfected c6 cells. |
1999-04-29 |
2023-08-12 |
Not clear |
| B Le Grand, A Panissié, P J Pauwels, G W Joh. Activation of recombinant h 5-HT1B and h 5-HT1D receptors stably expressed in C6 glioma cells produces increases in Ca2+-dependent K+ current. Naunyn-Schmiedeberg's archives of pharmacology. vol 358. issue 6. 1999-04-29. PMID:9879718. |
in the presence of the mixed 5-ht1b/d receptor antagonist gr 127935 (0.1 microm), sumatriptan (1 microm) failed to significantly increase ik in c6 cells expressing h 5-ht1b receptors (-7.5+/-3.5%, p=ns, n=6), although a higher concentration of gr 127935 (1 microm) was required to significantly inhibit sumatriptan-evoked increases in ik in c6 cells expressing h 5-ht1d receptors (-1.8+/-3.5%, p=ns, n=6), confirming that sumatriptan-evoked responses were indeed mediated by h 5-ht1b and h 5-ht1d receptors, respectively. |
1999-04-29 |
2023-08-12 |
Not clear |
| P De Vries, A Sánchez-López, D Centurión, J P Heiligers, P R Saxena, C M Villaló. The canine external carotid vasoconstrictor 5-HT1 receptor: blockade by 5-HT1B (SB224289), but not by 5-HT1D (BRL15572) receptor antagonists. European journal of pharmacology. vol 362. issue 1. 1999-04-13. PMID:9865532. |
it is concluded that mainly 5-ht1b, but not 5-ht1d receptors mediate the canine external carotid vasoconstriction by 5-ht and sumatriptan. |
1999-04-13 |
2023-08-12 |
Not clear |
| M Perez, C Jorand-Lebrun, P J Pauwels, I Pallard, S Halaz. Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. Bioorganic & medicinal chemistry letters. vol 8. issue 11. 1999-03-11. PMID:9871775. |
new dimers of known 5ht1 ligands (5ht, 1-np or 8-oh-dpat) have been prepared and evaluated at human cloned 5ht1b, 5ht1d and 5ht1a receptors. |
1999-03-11 |
2023-08-12 |
human |
| J Stanton, L Castro, A MacLeod, F Sternfeld, L Street, M Bee. [3H]5-HT binding to cloned human, dog, and rat 5-HT1D and 5-HT1B receptors. Annals of the New York Academy of Sciences. vol 861. 1999-02-25. PMID:9928282. |
[3h]5-ht binding to cloned human, dog, and rat 5-ht1d and 5-ht1b receptors. |
1999-02-25 |
2023-08-12 |
human |
| K W Johnson, L A Phebus, M L Cohe. Serotonin in migraine: theories, animal models and emerging therapies. Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques. vol 51. 1999-02-24. PMID:9949863. |
sumatriptan is an agonist at 5-ht1d and 5-ht1b receptor subtypes, and effective in treating migraine pain and associated symptoms. |
1999-02-24 |
2023-08-12 |
Not clear |
| P Bonaventure, X Langlois, J E Leyse. Co-localization of 5-HT1B- and 5-HT1D receptor mRNA in serotonergic cell bodies in guinea pig dorsal raphé nucleus: a double labeling in situ hybridization histochemistry study. Neuroscience letters. vol 254. issue 2. 1999-01-08. PMID:9779933. |
in order to provide further details on the cellular localization of 5-ht1b- and 5-ht1d receptor mrna in the dorsal raphé nucleus, we performed, in the same sections of guinea-pig dorsal raphé nucleus, double labeling in situ hybridization histochemistry for: (1) 5-ht1b receptor mrna and 5-ht1d receptor mrna, (2) 5-ht1b receptor mrna and 5-ht transporter (5-htt) mrna as marker for serotonergic neurons and (3) 5-ht1d receptor mrna and 5-htt mrna. |
1999-01-08 |
2023-08-12 |
Not clear |
| J C Rousselle, M Plantefol, M P Fillion, O Massot, P J Pauwels, G Fillio. Specific interaction of 5-HT-moduline with human 5-HT1b as well as 5-HT1d receptors expressed in transfected cultured cells. Naunyn-Schmiedeberg's archives of pharmacology. vol 358. issue 3. 1998-12-22. PMID:9774213. |
using transfected cells expressing either 5-ht1b or 5-ht1d receptors, it was shown that 5-ht-moduline prevents the binding of [3h]5-ht to 5-ht1b as well as to 5-ht1d receptors with similar biochemical characteristics: the ic50 of the peptide was 1.2x10(-12) m for 5-ht1b and 9x10(-13) m for 5-ht1d receptors. |
1998-12-22 |
2023-08-12 |
human |