-
1
-
-
0028344125
-
Sumatriptan: A reappraisal of its pharmacology and therapeutic efficacy in the acute treatment of migraine and cluster headache
-
Plosker, G. L.; McTavish, D. Sumatriptan: A Reappraisal of its Pharmacology and Therapeutic Efficacy in the Acute Treatment of Migraine and Cluster Headache. Drugs 1994, 47, 622-651.
-
(1994)
Drugs
, vol.47
, pp. 622-651
-
-
Plosker, G.L.1
McTavish, D.2
-
2
-
-
0028955742
-
Classification and nomenclature of serotonin receptors
-
Hoyer, D.; Bell, G. I.; Berelowitz, M.; Epelbaum, J.; Feniuk, W.; Humphrey, P. P. A.; O'Carroll, A. M.; Patel, Y. C.; Schonbrunn, A. Classification and Nomenclature of Serotonin Receptors. Trends Pharmacol. Sci. 1995, 16, 86-8.
-
(1995)
Trends Pharmacol. Sci.
, vol.16
, pp. 86-88
-
-
Hoyer, D.1
Bell, G.I.2
Berelowitz, M.3
Epelbaum, J.4
Feniuk, W.5
Humphrey, P.P.A.6
O'Carroll, A.M.7
Patel, Y.C.8
Schonbrunn, A.9
-
4
-
-
0030961840
-
5-HT receptor classification and nomenclature: Towards a harmonisation with the human genome
-
Hoyer, D.; Martin, G. 5-HT Receptor Classification and Nomenclature: Towards a Harmonisation With the Human Genome. Neuropharmacology 1997, 36, 419-428.
-
(1997)
Neuropharmacology
, vol.36
, pp. 419-428
-
-
Hoyer, D.1
Martin, G.2
-
5
-
-
0002329973
-
1D receptors: Pharmacology and therapeutic potential
-
1D Receptors: Pharmacology and Therapeutic Potential. Serotonin 1996, 1, 19-29.
-
(1996)
Serotonin
, vol.1
, pp. 19-29
-
-
Hamel, E.1
-
6
-
-
0028073306
-
Adverse reactions attributed to sumatriptan. A postmarketing study in general practise
-
Ottervanger, J. P.; van Witsen, T. B.; Valkenburg, H. A.; Grobbee, D. E.; Stricker, B. H. Adverse Reactions Attributed to Sumatriptan. A Postmarketing Study in General Practise. Eur. J. Clin. Pharmacol. 1994, 47, 305-309.
-
(1994)
Eur. J. Clin. Pharmacol.
, vol.47
, pp. 305-309
-
-
Ottervanger, J.P.1
Van Witsen, T.B.2
Valkenburg, H.A.3
Grobbee, D.E.4
Stricker, B.H.5
-
7
-
-
0027257522
-
5-HT receptors mediating contractions of isolated human coronary artery
-
(a) Bax, W. A.; Rezenbrink, G. J.; van Heuven-Nolsen, D.; Thijssen, E. J. M.; Bos, E.; Saxena, P. R. 5-HT Receptors Mediating Contractions of Isolated Human Coronary Artery. Eur. J. Pharmacol. 1993, 239, 203-210.
-
(1993)
Eur. J. Pharmacol.
, vol.239
, pp. 203-210
-
-
Bax, W.A.1
Rezenbrink, G.J.2
Van Heuven-Nolsen, D.3
Thijssen, E.J.M.4
Bos, E.5
Saxena, P.R.6
-
9
-
-
0029151705
-
Comparison of the contractile effects of 5-hydroxytryptamine, sumatriptan and MK-462 on human coronary artery in vitro
-
Rizatriptan has been shown to have a lower propensity than Sumatriptan in causing contraction of isolated human artery segments: (a) Ferro, A.; Longmore, J.; Hill, R. G.; Brown, M. J. A. Comparison of the Contractile Effects of 5-Hydroxytryptamine, Sumatriptan and MK-462 on Human Coronary Artery in vitro. Br. J. Clin. Pharmacol. 1995, 40 (3), 245-251.
-
(1995)
Br. J. Clin. Pharmacol.
, vol.40
, Issue.3
, pp. 245-251
-
-
Ferro, A.1
Longmore, J.2
Hill, R.G.3
Brown, M.J.A.4
-
10
-
-
0029658680
-
1D receptor agonists and human coronary artery reactivity in vitro: Crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519
-
1D Receptor Agonists and Human Coronary Artery Reactivity in vitro: Crossover Comparisons of 5-HT and Sumatriptan with Rizatriptan and L-741,519. Br. J. Clin. Pharmacol. 1996, 42, 431-441.
-
(1996)
Br. J. Clin. Pharmacol.
, vol.42
, pp. 431-441
-
-
Longmore, J.1
Boulanger, C.M.2
Desta, B.3
Hill, R.G.4
Schofield, W.N.5
Taylor, A.A.6
-
11
-
-
0028050651
-
The mode of action of sumatriptan is vascular? a debate
-
Humphrey, P. P. A.; Goadsby, P. J. The Mode of Action of Sumatriptan is Vascular? A Debate. Cephalagia 1994, 14, 401-410.
-
(1994)
Cephalagia
, vol.14
, pp. 401-410
-
-
Humphrey, P.P.A.1
Goadsby, P.J.2
-
12
-
-
0029151766
-
Neurogenic model of migraine
-
Buzzi, M. G.; Bonamini, M.; Moskowitz, M. A. Neurogenic Model of Migraine. Cephalagia 1995, 15, 277-280.
-
(1995)
Cephalagia
, vol.15
, pp. 277-280
-
-
Buzzi, M.G.1
Bonamini, M.2
Moskowitz, M.A.3
-
13
-
-
0030067627
-
1D agonist drugs: Selectively targeting additional sites of action
-
1D Agonist Drugs: Selectively Targeting Additional Sites of Action. Eur. Neurol. 1996, 36, 13-18.
-
(1996)
Eur. Neurol.
, vol.36
, pp. 13-18
-
-
Martin, G.R.1
-
14
-
-
0029813854
-
Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels
-
Bouchelet, I.; Cohen, Z.; Case, B.; Seguela, P.; Hamel, E. Differential Expression of Sumatriptan-Sensitive 5-Hydroxytryptamine Receptors in Human Trigeminal Ganglia and Cerebral Blood Vessels. Mol. Pharmacol. 1996, 50, 219-223.
-
(1996)
Mol. Pharmacol.
, vol.50
, pp. 219-223
-
-
Bouchelet, I.1
Cohen, Z.2
Case, B.3
Seguela, P.4
Hamel, E.5
-
15
-
-
0030663835
-
1b subtype
-
1B Subtype. J. Med. Chem. 1997, 40, 3497-3500.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 3497-3500
-
-
Castro, J.L.1
Street, L.J.2
Guiblin, A.R.3
Jelley, R.A.4
Russell, M.G.N.5
Sternfeld, F.6
Beer, M.S.7
Stanton, J.A.8
Matassa, V.G.9
-
16
-
-
0030572495
-
1d receptors
-
1D) Receptors. Bioorg. Med. Chem. Lett. 1996, 6, 1825-1830.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 1825-1830
-
-
Sternfeld, F.1
Baker, R.2
Broughton, H.B.3
Guiblin, A.R.4
Jelley, R.A.5
Matassa, V.G.6
Reeve, A.J.7
Beer, M.S.8
Stanton, J.A.9
Hargreaves, R.J.10
Shepheard, S.L.11
Longmore, J.12
Razzaque, Z.13
Graham, M.I.14
Sohal, B.15
Street, L.J.16
-
17
-
-
84920312872
-
-
note
-
Although small, the difference in selectivity between 3b and 4 (9-fold vs 4.3-fold) is statistically significant. Further support for the inherent selectivity of the pyrrolidine base versus tryptamine is provided by the observation that the N-methyl-N-benzyl analogue of 4 is only marginally selective (4-fold).
-
-
-
-
19
-
-
0025122262
-
Agonists and uptake inhibitors. Synthesis, absolute stereochemistry and enantioselectivity of (R)-(-)-and (S)-(+)-homo-β-proline
-
Nielsen, L.; Brehm, L.; Krogsgaard-Larsen, P. GABA Agonists and Uptake Inhibitors. Synthesis, Absolute Stereochemistry and Enantioselectivity of (R)-(-)-and (S)-(+)-Homo-β-proline. J. Med. Chem. 1990, 33, 71-77.
-
(1990)
J. Med. Chem.
, vol.33
, pp. 71-77
-
-
Nielsen, L.1
Brehm, L.2
Gaba, P.3
-
20
-
-
37049111591
-
Controlling the outcome of a carbocation-initiated cylisation
-
Fleming, I.; Pearce, A. Controlling the Outcome of a Carbocation-Initiated Cylisation. J. Chem. Soc., Perkin Trans. 1 1981, 251-255.
-
(1981)
J. Chem. Soc., Perkin Trans. 1
, pp. 251-255
-
-
Fleming, I.1
Pearce, A.2
-
21
-
-
0028024461
-
1D receptor agonist mK-462 via a Pd-catalysed coupling reaction
-
1D Receptor Agonist MK-462 via a Pd-Catalysed Coupling Reaction. Tetrahedron Lett. 1994, 35, 6981-6984.
-
(1994)
Tetrahedron Lett.
, vol.35
, pp. 6981-6984
-
-
Chen, C.1
Lieberman, D.R.2
Larsen, R.D.3
Reamer, R.A.4
Verhoeven, T.R.5
Reider, P.J.6
Cottrell, I.F.7
Houghton, P.G.8
-
22
-
-
84920312871
-
-
note
-
Note that, in the case of 12a, this operation results in inversion of the pyrrolidine C-3 chiral center.
-
-
-
-
23
-
-
84920312870
-
-
note
-
Synthesis of the methylene-bridged triazol-lyltryptophol required for the preparation of 22a-d is described in ref 19.
-
-
-
-
24
-
-
0027056036
-
Synthesis of a conformationally restricted analogue of the anti-migraine drug sumatriptan
-
(a) Macor, J. E.; Blank, D. H.; Post, R. J.; Ryan, K. Synthesis of a Conformationally Restricted Analogue of the Anti-Migraine Drug Sumatriptan. Tetrahedron Lett. 1992, 33, 8011-14.
-
(1992)
Tetrahedron Lett.
, vol.33
, pp. 8011-8014
-
-
Macor, J.E.1
Blank, D.H.2
Post, R.J.3
Ryan, K.4
-
25
-
-
0029095043
-
1D receptor: Discovery of compounds with potential anti-migraine properties
-
1D Receptor: Discovery of Compounds with Potential Anti-Migraine Properties. J. Med. Chem. 1995, 38, 3566-3580.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 3566-3580
-
-
Glen, R.C.1
Martin, G.R.2
Hill, A.P.3
Hyde, R.M.4
Woollard, P.M.5
Salmon, J.A.6
Buckingham, J.7
Robertson, A.D.8
-
28
-
-
0030772313
-
Synthesis of 3-hydroxyalkylbenzo[b]furans via the palladium-catalysed heteroannulation of silyl-protected alkynols with 2-iodophenol
-
(b) Bishop, B. C.; Cottrell, I. F.; Hands, D. Synthesis of 3-Hydroxyalkylbenzo[b]furans via the Palladium-Catalysed Heteroannulation of Silyl-Protected Alkynols with 2-Iodophenol. Synthesis 1997, 1315-1320.
-
(1997)
Synthesis
, pp. 1315-1320
-
-
Bishop, B.C.1
Cottrell, I.F.2
Hands, D.3
-
30
-
-
84920312869
-
-
note
-
35S]GTPγS is resistant to this GTPase, it accumalates in the membrane and can be measured by virtue of its radiolabel. See, for example, ref 26.
-
-
-
-
31
-
-
0027313323
-
35S]GTPγs binding mediated by human muscarinic m1-m4 receptors: Antagonist studies
-
35S]GTPγS Binding Mediated by Human Muscarinic m1-m4 Receptors: Antagonist Studies. Br. J. Pharmacol. 1993, 109, 1120-1127.
-
(1993)
Br. J. Pharmacol.
, vol.109
, pp. 1120-1127
-
-
Lazareno, S.1
Birdsall, N.J.M.2
-
32
-
-
84920312868
-
-
note
-
Inflammation of the dura in animals, induced by electrical stimulation of the trigeminal ganglion, has been proposed as a possible model of migraine. See ref 10.
-
-
-
-
33
-
-
84920312867
-
-
note
-
50 130 nM; maximal efficacy 101% relative to 5-HT).
-
-
-
-
34
-
-
0030669050
-
1D receptor agonists as potential antimigraine agents
-
1D Receptor Agonists as Potential Antimigraine Agents. J. Med. Chem. 1997, 40, 3501-3503.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 3501-3503
-
-
MacLeod, A.M.1
Street, L.J.2
Reeve, A.J.3
Jelley, R.A.4
Sternfeld, F.5
Beer, M.S.6
Stanton, J.A.7
Watt, A.P.8
Rathbone, D.9
Matassa, V.G.10
-
35
-
-
84920312866
-
-
note
-
1D receptor agonists See ref 13.
-
-
-
-
36
-
-
84920312865
-
-
note
-
The structures are local low-energy conformers found using the SYBYL minimization routine with the TRIPOS force field and Gasteiger-Huckel charges on the protonated species. The overlays were formed by directly overlaying the indole rings.
-
-
-
-
38
-
-
84920312863
-
-
note
-
40 based upon the bacteriorhodopsin template as a starting point. Modifications to this starting conformation were made using the SYBYL modeling software from TRIPOS to produce a sensible, energetically favorable structure which conformed to our in-house results. These modifications included helix rotations and translations as well as the introduction of the loop regions between each helix including dynamics and energy minimizations (TRIPOS force field, Gasteiger-Huckel charges with neutral amino acids) with and without agonists bound.
-
-
-
-
39
-
-
84920312862
-
-
note
-
1B 910 nM.
-
-
-
-
40
-
-
84920312861
-
-
note
-
1F 27 nM.
-
-
-
-
41
-
-
84920312860
-
-
note
-
Further evidence for the contribution of the N-4-linked triazole to poor oral absorption is provided by comparison of the hepatic portal vein concentrations of 3b (135 and 31 ng/mL at 0.5 and 2 h postdose) with those of {2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethyl}pyrrolidine (254 and 263 ng/mL at 0.5 and 2 h pastdose).
-
-
-
-
42
-
-
37049116588
-
Transaminations of N,N-dimethylformamide azine
-
Bartlett, R. K.; Humphrey, I. R. Transaminations of N,N-Dimethylformamide Azine. J. Chem. Soc. C 1967, 1664-1666.
-
(1967)
J. Chem. Soc. C
, pp. 1664-1666
-
-
Bartlett, R.K.1
Humphrey, I.R.2
-
43
-
-
84920305052
-
-
EP 0373 891 A2
-
Hughes, L. R.; Oldfield, J.; Pegg, S. J.; Barker, A. J.; Marsham, P. R. Anti-tumour Agents. EP 0373 891 A2.
-
Anti-tumour Agents
-
-
Hughes, L.R.1
Oldfield, J.2
Pegg, S.J.3
Barker, A.J.4
Marsham, P.R.5
-
44
-
-
0000191820
-
Tertiary carbinamines by addition of organocerium reagents to nitriles and ketimines
-
Ciganek, E. Tertiary Carbinamines by Addition of Organocerium Reagents to Nitriles and Ketimines. J. Org. Chem. 1992, 57, 4521-4527.
-
(1992)
J. Org. Chem.
, vol.57
, pp. 4521-4527
-
-
Ciganek, E.1
-
45
-
-
0000917207
-
GPCRDB: An information system for G protein coupled receptors
-
Horn, F.; Weare, J.; Beukers, M. W.; Horsch, S.; Bairoch, A.; Chen, W.; Edvardsen, O.; Campagne, F.; Vriend, G. GPCRDB: an information system for G protein coupled receptors. Nucleic Acids Res. 1988, 26, 277-281.
-
(1988)
Nucleic Acids Res.
, vol.26
, pp. 277-281
-
-
Horn, F.1
Weare, J.2
Beukers, M.W.3
Horsch, S.4
Bairoch, A.5
Chen, W.6
Edvardsen, O.7
Campagne, F.8
Vriend, G.9
|