-
1
-
-
0028966647
-
Neurokinin Receptors
-
(a) Longmore, J.; Swain, C. J.; Hill, R. G. Neurokinin Receptors. Drug News Perspect, 1995, 8, 5-23.
-
(1995)
Drug News Perspect.
, vol.8
, pp. 5-23
-
-
Longmore, J.1
Swain, C.J.2
Hill, R.G.3
-
2
-
-
0027339655
-
Non-Peptide NK1-Receptor Antagonist, RP 67580, Inhibits Neurogenic Inflammation Postsynaptically
-
(b) Moussaoui, S. M.; Montier, F.; Carruette, A.; Blanchard, J. C.; Laduron, P. M.; Garret, C. A. Non-Peptide NK1-Receptor Antagonist, RP 67580, Inhibits Neurogenic Inflammation Postsynaptically. Br. J. Pharmacol. 1993, 109, 259-264.
-
(1993)
Br. J. Pharmacol.
, vol.109
, pp. 259-264
-
-
Moussaoui, S.M.1
Montier, F.2
Carruette, A.3
Blanchard, J.C.4
Laduron, P.M.5
Garret, C.A.6
-
3
-
-
0023783617
-
Substance P Antagonists and Analgesia: A Review of the Hypothesis
-
(c) Vaught, J. L. Substance P Antagonists and Analgesia: A Review of the Hypothesis. Life Sci. 1988, 43, 1419-1431.
-
(1988)
Life Sci.
, vol.43
, pp. 1419-1431
-
-
Vaught, J.L.1
-
4
-
-
0028206333
-
Preliminary Findings on the Role of Neuropeptide Suppression by Topical Agents in the Management of Rheumatoid Arthritis
-
Weisman, M. H.; Hagaman, C.; Yaksh, T. L.; Lotz, M. Preliminary Findings on the Role of Neuropeptide Suppression by Topical Agents in the Management of Rheumatoid Arthritis. Semin. Arthritis Rheum. 1994, 23, 18-24.
-
(1994)
Semin. Arthritis Rheum.
, vol.23
, pp. 18-24
-
-
Weisman, M.H.1
Hagaman, C.2
Yaksh, T.L.3
Lotz, M.4
-
5
-
-
0028226031
-
Sensory Neuropeptides and the Human Lower Airways: Present State and Future Directions
-
Joos, G. F.; Germonpre, P. R.; Kips, J. C.; Peleman, R. A.; Pauwels, R. A. Sensory Neuropeptides and the Human Lower Airways: Present State and Future Directions. Eur. Respir. J. 1994, 7, 1161-1171.
-
(1994)
Eur. Respir. J.
, vol.7
, pp. 1161-1171
-
-
Joos, G.F.1
Germonpre, P.R.2
Kips, J.C.3
Peleman, R.A.4
Pauwels, R.A.5
-
6
-
-
0028339649
-
Involvement of Neurokinin 1 and 2 Receptors in Viscerosensitive Response to Rectal Distension in Rats
-
Julia, V.; Morteau, O.; Bueno, L. Involvement of Neurokinin 1 and 2 Receptors in Viscerosensitive Response to Rectal Distension in Rats. Gastroenterology 1994, 107, 94-102.
-
(1994)
Gastroenterology
, vol.107
, pp. 94-102
-
-
Julia, V.1
Morteau, O.2
Bueno, L.3
-
7
-
-
0028589913
-
Receptors and Antagonists for Substance P and Related Peptides
-
Regoli, D.; Boudon, A.; Fauchere, J.-L. Receptors and Antagonists for Substance P and Related Peptides. Pharm. Rev. 1994, 46, 551-599.
-
(1994)
Pharm. Rev.
, vol.46
, pp. 551-599
-
-
Regoli, D.1
Boudon, A.2
Fauchere, J.-L.3
-
8
-
-
0026099914
-
A Potent Non-Peptide Antagonist of the Substance P (NK1) Receptor
-
Snider, R. M.; Constantine, J. W.; Lowe, J. A.; Longo, K. P.; Lebel, W. S.; Woody, H. A.; Drozda, S. E.; Desai, M. C.; Vinick, F. J.; Spencer, R. W.; Hess, H. J. A Potent Non-Peptide Antagonist of the Substance P (NK1) Receptor. Science 1991, 251, 435-437.
-
(1991)
Science
, vol.251
, pp. 435-437
-
-
Snider, R.M.1
Constantine, J.W.2
Lowe, J.A.3
Longo, K.P.4
Lebel, W.S.5
Woody, H.A.6
Drozda, S.E.7
Desai, M.C.8
Vinick, F.J.9
Spencer, R.W.10
Hess, H.J.11
-
9
-
-
0028273239
-
Recent Advances in the Discovery and Characterization of Substance P Antagonists
-
and references therein
-
Desai, M. C. Recent Advances in the Discovery and Characterization of Substance P Antagonists. Exp. Opin. Ther. Patents 1994, 4, 315-321 and references therein.
-
(1994)
Exp. Opin. Ther. Patents
, vol.4
, pp. 315-321
-
-
Desai, M.C.1
-
10
-
-
0028123558
-
Cardiovascular Effects of CP-96,345, A Non-Peptide Blocker of Tachykinin NK-1 Receptors
-
(a) Constantine, J. W.; Lebel, W S.; Woody, H. A.; Benoit, P. A.; Wolfgang, E. A.; Knight, D. R. Cardiovascular Effects of CP-96,345, A Non-Peptide Blocker of Tachykinin NK-1 Receptors. Eur. J. Pharmacol. 1994, 252, 275-282.
-
(1994)
Eur. J. Pharmacol.
, vol.252
, pp. 275-282
-
-
Constantine, J.W.1
Lebel, W.S.2
Woody, H.A.3
Benoit, P.A.4
Wolfgang, E.A.5
Knight, D.R.6
-
13
-
-
0026739051
-
Non-Specific Activity of (±)-CP-96,345 in Models of Pain and Inflammation
-
(d) Nagahisa, A.; Asai, R.; Kanai, Y.; Murase, A.; Tsuchiya-Nakgaki, M.; Nakagaki, T.; Shieh, T.-C.; Taniguchi, K. Non-Specific Activity of (±)-CP-96,345 in Models of Pain and Inflammation. Br. J. Pharmacol. 1992, 107, 273-275.
-
(1992)
Br. J. Pharmacol.
, vol.107
, pp. 273-275
-
-
Nagahisa, A.1
Asai, R.2
Kanai, Y.3
Murase, A.4
Tsuchiya-Nakgaki, M.5
Nakagaki, T.6
Shieh, T.-C.7
Taniguchi, K.8
-
14
-
-
0027237031
-
CP-99,994, A Nonpeptide Antagonist of the Tachykinin NK1 Receptor
-
(a) McLean, S.; Snider, R. M.; Desai, M. C.; Rosen, T.; Bryce, D. K.; Longo, K. P.; Schmidt, A. W.; Heym, J. CP-99,994, A Nonpeptide Antagonist of the Tachykinin NK1 Receptor. Regul. Pept. 1993, 46, 329-331.
-
(1993)
Regul. Pept.
, vol.46
, pp. 329-331
-
-
McLean, S.1
Snider, R.M.2
Desai, M.C.3
Rosen, T.4
Bryce, D.K.5
Longo, K.P.6
Schmidt, A.W.7
Heym, J.8
-
15
-
-
0027420750
-
Pharmacology of CP-99,994; a Nonpeptide Antagonist of the Tachykinin Neurokinin-1 Receptor
-
(b) McLean, S.; Ganong, A.; Seymour, P. A.; Snider, R. M.; Desai, M. C.; Rosen, T.; Bryce, D. K.; Longo, K. P.; Reynolds, L. S.; Robinson, G.; Schmidt, A. W.; Siok, C.; Heym, J. Pharmacology of CP-99,994; a Nonpeptide Antagonist of the Tachykinin Neurokinin-1 Receptor. J. Pharmacol. Exp. Ther. 1993, 267, 472-479.
-
(1993)
J. Pharmacol. Exp. Ther.
, vol.267
, pp. 472-479
-
-
McLean, S.1
Ganong, A.2
Seymour, P.A.3
Snider, R.M.4
Desai, M.C.5
Rosen, T.6
Bryce, D.K.7
Longo, K.P.8
Reynolds, L.S.9
Robinson, G.10
Schmidt, A.W.11
Siok, C.12
Heym, J.13
-
16
-
-
0027997928
-
Piperidine-Ether Based hNK1 Antagonists 1: Determination of the Relative and Absolute Stereochemical Requirements
-
Harrison, T.; Williams, B. J.; Swain, C. J.; Ball, R. G. Piperidine-Ether Based hNK1 Antagonists 1: Determination of the Relative and Absolute Stereochemical Requirements. Bioorg. Med. Chem. Lett. 1994, 4, 2545-2550.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 2545-2550
-
-
Harrison, T.1
Williams, B.J.2
Swain, C.J.3
Ball, R.G.4
-
17
-
-
0028821240
-
Piperidine-Ether Based h-NK1 Antagonists 2: Investigation of the Effect of N-Substitution
-
(a) Harrison, T.; Owens, A. P.; Williams, B. J.; Swain, C. J.; Baker, R.; Hutson, P. H.; Sadowski, S.; Cascieri, M. A. Piperidine-Ether Based h-NK1 Antagonists 2: Investigation of the Effect of N-Substitution. Bioorg. Med. Chem. Lett. 1995, 5, 209-212.
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 209-212
-
-
Harrison, T.1
Owens, A.P.2
Williams, B.J.3
Swain, C.J.4
Baker, R.5
Hutson, P.H.6
Sadowski, S.7
Cascieri, M.A.8
-
18
-
-
5544298173
-
N-Heteroaryl-2-Phenyl-3-Benzyloxypiperidines: A Novel Class of Potent, Orally Active Human NK-1 Antagonists
-
Manuscript submitted
-
(b) Ladduwahetty, T.; Baker, R.; Cascieri, M. A.; Chambers, M. S.; Haworth, K.; Keown, L.; MacIntyre, D. E.; Metzger, J. M.; Owen, S.; Rycroft, W.; Sadowski, S.; Seward, E. M.; Shepeard, S.; Swain, C. J.; Tattersall, F. D.; Williamson, D.; Hargreaves, R. J. N-Heteroaryl-2-Phenyl-3-Benzyloxypiperidines: A Novel Class of Potent, Orally Active Human NK-1 Antagonists. Manuscript submitted to J. Med. Chem.
-
J. Med. Chem.
-
-
Ladduwahetty, T.1
Baker, R.2
Cascieri, M.A.3
Chambers, M.S.4
Haworth, K.5
Keown, L.6
MacIntyre, D.E.7
Metzger, J.M.8
Owen, S.9
Rycroft, W.10
Sadowski, S.11
Seward, E.M.12
Shepeard, S.13
Swain, C.J.14
Tattersall, F.D.15
Williamson, D.16
Hargreaves, R.J.17
-
19
-
-
0024564925
-
Synthesis, Physicochemical Properties and Biological Studies of Some Substituted 2-Alkoxy-4-Methyl-Morpholines
-
Rekka, A.; Kourounakis, P. Synthesis, Physicochemical Properties and Biological Studies of Some Substituted 2-Alkoxy-4-Methyl-Morpholines. Eur. J. Med. Chem. 1989, 24, 179-185.
-
(1989)
Eur. J. Med. Chem.
, vol.24
, pp. 179-185
-
-
Rekka, A.1
Kourounakis, P.2
-
20
-
-
0000431388
-
1-Benzylamine
-
1-Benzylamines.) Helv. Chim. Acta 1966, 49, 2481-2489.
-
(1966)
Helv. Chim. Acta
, vol.49
, pp. 2481-2489
-
-
Gerlach, H.1
-
21
-
-
37049082063
-
Synthesis and Reaction of Optically Active Morpholinones
-
Kashima, C.; Harada, K. Synthesis and Reaction of Optically Active Morpholinones. J. Chem. Soc., Perkin Trans. I 1988, 1521.
-
(1988)
J. Chem. Soc., Perkin Trans. I
, pp. 1521
-
-
Kashima, C.1
Harada, K.2
-
22
-
-
0000889518
-
Nouvelle Methode de Benzylation D'Hydroxyles Glucidiques Encombres
-
Czernecki, S.; Georgoulis, C.; Provelenghiou, C. Nouvelle Methode de Benzylation D'Hydroxyles Glucidiques Encombres. (Novel Method for the Benzyl Protection of Carbohydrate Hydroxyl Groups.) Tetrahedron Lett. 1976, 3535-3536.
-
(1976)
Tetrahedron Lett.
, pp. 3535-3536
-
-
Czernecki, S.1
Georgoulis, C.2
Provelenghiou, C.3
-
23
-
-
37949055837
-
Recent Developments in the Synthesis of Glycoconjugates
-
Schmidt, R. R. Recent Developments in the Synthesis of Glycoconjugates. Pure Appl. Chem. 1989, 61, 1257-1270.
-
(1989)
Pure Appl. Chem.
, vol.61
, pp. 1257-1270
-
-
Schmidt, R.R.1
-
24
-
-
0021287857
-
Histamine H2 Receptor Antagonists. 1. Synthesis of N-Cyano and N-Carbamoyl Amidine Derivatives and Their Biological Activities
-
Yanagisawa, I.; Hirata, Y.; Ishii, Y. Histamine H2 Receptor Antagonists. 1. Synthesis of N-Cyano and N-Carbamoyl Amidine Derivatives and Their Biological Activities. J. Med. Chem. 1984, 27, 849-857.
-
(1984)
J. Med. Chem.
, vol.27
, pp. 849-857
-
-
Yanagisawa, I.1
Hirata, Y.2
Ishii, Y.3
-
25
-
-
0028274616
-
-
The stereochemical purity was determined by supercritical fluid chromatography (SFC) using a novel two-column (achiral and chiral column in series) approach. For details, see the Supporting Information. For a review of chiral SFC, see: Petersson, P.; Markides, K E. J. Chromatogr. A 1994, 666, 381-394.
-
(1994)
J. Chromatogr. A
, vol.666
, pp. 381-394
-
-
Petersson, P.1
Markides, K.E.2
-
26
-
-
0027065565
-
Characterization of the Binding of a Potent, Selective Radioiodinated Antagonist to the Human Neurokinin-1 Receptor
-
Cascieri, M. A.; Ber, E.; Fong, T. M.; Sadowski, S.; Bansal, A.; Swain, S.; Seward, E.; Frances, B.; Burns, D.; Strader, C. D. Characterization of the Binding of a Potent, Selective Radioiodinated Antagonist to the Human Neurokinin-1 Receptor. Mol. Pharmacol. 1992, 42, 458-465.
-
(1992)
Mol. Pharmacol.
, vol.42
, pp. 458-465
-
-
Cascieri, M.A.1
Ber, E.2
Fong, T.M.3
Sadowski, S.4
Bansal, A.5
Swain, S.6
Seward, E.7
Frances, B.8
Burns, D.9
Strader, C.D.10
-
28
-
-
0022559089
-
3H]-Desmethoxyverapamil Labels Multiple Calcium Channel Modulator Receptors in Brain and Skeletal Muscle Membranes: Differentiation by Temperature and Dihydropyridines
-
3H]-Desmethoxyverapamil Labels Multiple Calcium Channel Modulator Receptors in Brain and Skeletal Muscle Membranes: Differentiation by Temperature and Dihydropyridines. J. Pharmacol. Exp. Ther. 1986, 237, 731-738.
-
(1986)
J. Pharmacol. Exp. Ther.
, vol.237
, pp. 731-738
-
-
Reynolds, I.J.1
Snowman, A.M.2
Snyder, S.H.3
-
29
-
-
0028017410
-
Acyclic NK-1 Antagonists: 2-Benzhydryl-2-Aminoethyl Ethers
-
(a) Williams, B. J.; Teall, M.; McKenna, J.; Harrison, T.; Swain, C. J.; Cascieri, M. A.; Sadowski, S.; Strader, C.; Baker, R. Acyclic NK-1 Antagonists: 2-Benzhydryl-2-Aminoethyl Ethers. Bioorg. Med. Chem. Lett. 1994, 4, 1903-1908.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 1903-1908
-
-
Williams, B.J.1
Teall, M.2
McKenna, J.3
Harrison, T.4
Swain, C.J.5
Cascieri, M.A.6
Sadowski, S.7
Strader, C.8
Baker, R.9
-
30
-
-
0028964676
-
1,2,4-Triacylpiperidine Substance P Antagonists: Separation of the Affinities for the NK-1 Receptor and the L-Type Calcium Channel
-
(b) Mills, S. G.; MacCoss, M.; Cascieri, M. A.; Sadowski, S.; Patel, S.; Chapman, K. L.; Hutson, P. H. 1,2,4-Triacylpiperidine Substance P Antagonists: Separation of the Affinities for the NK-1 Receptor and the L-Type Calcium Channel. Bioorg. Med. Chem. Lett. 1995, 5, 599-604.
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 599-604
-
-
Mills, S.G.1
MacCoss, M.2
Cascieri, M.A.3
Sadowski, S.4
Patel, S.5
Chapman, K.L.6
Hutson, P.H.7
-
31
-
-
5544239486
-
-
The United States Pharmacopeia (USP 23/NF 18), 1995, p 2053; United States Pharmacopeial Conventions, Inc., Rockville, MD
-
The United States Pharmacopeia (USP 23/NF 18), 1995, p 2053; United States Pharmacopeial Conventions, Inc., Rockville, MD.
-
-
-
-
32
-
-
5544241257
-
-
The limits of detection of either standard compound by HPLC was determined to be ∼2%
-
The limits of detection of either standard compound by HPLC was determined to be ∼2%.
-
-
-
-
33
-
-
0028305221
-
Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK-1 Receptor
-
MacLeod, A. M.; Merchant, K. J.; Brookfield, F.; Kelleher, F.; Stevenson, G.; Owens, A. P.; Swain, C. J.; Cascieri, M. A.; Sadowski, S.; Ber, E.; Strader, C. D.; MacIntyre, D. E.; Metzger, J. M.; Ball, R. G.; Baker, R. Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK-1 Receptor. J. Med. Chem. 1994, 37, 1269.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 1269
-
-
MacLeod, A.M.1
Merchant, K.J.2
Brookfield, F.3
Kelleher, F.4
Stevenson, G.5
Owens, A.P.6
Swain, C.J.7
Cascieri, M.A.8
Sadowski, S.9
Ber, E.10
Strader, C.D.11
MacIntyre, D.E.12
Metzger, J.M.13
Ball, R.G.14
Baker, R.15
-
34
-
-
0029585287
-
Discovery of an Orally Bioavailable NK-1 Receptor Antagonist, (2S,3S)-2-Methoxy-5-tetrazol-l-ylbenzyl-(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity
-
Ward, et al. have noted that CP 99,994 is rapidly metabolized in dog hepatic microsomes and have suggested that first-pass metabolism is largely responsible for the low systemic plasma levels of this compound that are observed after oral dosing; see: Ward, P.; Armour, D. R.; Bays, D. E.; Evans, B.; Giblin, G. M. P.; Heron, N.; Hubbard, T.; Liang, K.; Middlemiss, D.; Mordaunt, J.; Naylor, A.; Pegg, N. A.; Vinader, V.; Watson, S. P.; Bountra, C.; Evans, D. C. Discovery of an Orally Bioavailable NK-1 Receptor Antagonist, (2S,3S)-2-Methoxy-5-tetrazol-l-ylbenzyl)-(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity. J. Med. Chem 1995, 38, 4985.
-
(1995)
J. Med. Chem
, vol.38
, pp. 4985
-
-
Ward, P.1
Armour, D.R.2
Bays, D.E.3
Evans, B.4
Giblin, G.M.P.5
Heron, N.6
Hubbard, T.7
Liang, K.8
Middlemiss, D.9
Mordaunt, J.10
Naylor, A.11
Pegg, N.A.12
Vinader, V.13
Watson, S.P.14
Bountra, C.15
Evans, D.C.16
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