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Christopher Swain

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Gregory J Hollingworth; Emma J Carlson; José L Castro; Gary G Chicchi; Natalie Clark; Laura C Cooper; Olivier Dirat; Jerry Di Salvo; Jason M Elliott; Ruth Kilburn; Marc M Kurtz; Wayne Rycroft; F David Tattersall; Kwei-Lan Tsao; Christopher J Swain
Novel lactam NK1 antagonists with anti-emetic activity.
Christopher G Thomson; Emma Carlson; Gary G Chicchi; Janusz J Kulagowski; Marc M Kurtz; Christopher J Swain; Kwei-Lan Tsao; Alan Wheeldon
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
Nadia M J Rupniak; Emma J Carlson; Sara Shepheard; Graham Bentley; Angela R Williams; Alastair Hill; Christopher J Swain; Sander G Mills; Jerry Di Salvo; Ruth Kilburn; Margaret A Cascieri; Marc M Kurtz; Kwei-Lan Tsao; Sandra L Gould; Gary G Chicchi
Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608.

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All Publications

2006: Gregory J Hollingworth; Emma J Carlson; José L Castro; Gary G Chicchi; Natalie Clark; Laura C Cooper; Olivier Dirat; Jerry Di Salvo; Jason M Elliott; Ruth Kilburn; Marc M Kurtz; Wayne Rycroft; F David Tattersall; Kwei-Lan Tsao; Christopher J Swain
Novel lactam NK1 antagonists with anti-emetic activity.
Bioorganic & medicinal chemistry letters 2006;16(5):1197-201.
2006: Christopher G Thomson; Emma Carlson; Gary G Chicchi; Janusz J Kulagowski; Marc M Kurtz; Christopher J Swain; Kwei-Lan Tsao; Alan Wheeldon
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
Bioorganic & medicinal chemistry letters 2006;16(4):811-4.
2003: Nadia M J Rupniak; Emma J Carlson; Sara Shepheard; Graham Bentley; Angela R Williams; Alastair Hill; Christopher J Swain; Sander G Mills; Jerry Di Salvo; Ruth Kilburn; Margaret A Cascieri; Marc M Kurtz; Kwei-Lan Tsao; Sandra L Gould; Gary G Chicchi
Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608.
Neuropharmacology 2003;45(2):231-41.
2002: Brian J Williams; Margaret A Cascieri; Gary G Chicchi; Timothy Harrison; Andrew P Owens; Simon N Owen; Nadia M J Rupniak; David F Tattersall; Angela Williams; Christopher J Swain
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Bioorganic & medicinal chemistry letters 2002;12(19):2719-22.
2002: Eileen M Seward; Emma Carlson; Timothy Harrison; Karen R Haworth; Richard Herbert; Fintan J Kelleher; Marc M Kurtz; Jonathan Moseley; Simon N Owen; Andrew P Owens; Sharon Sadowski; Christopher J Swain; Brian J Williams
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
Bioorganic & medicinal chemistry letters 2002;12(18):2515-8.
2002: Rachel K Conley; Michael J Cumberbatch; Glenn S Mason; David J Williamson; Timothy Harrison; Karen Locker; Christopher J Swain; Karen A Maubach; Ruth O'Donnell; Michael Rigby; Louise Hewson; David Smith; Nadia M J Rupniak
Substance P (neurokinin 1) receptor antagonists enhance dorsal raphe neuronal activity.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2002;22(17):7730-6.
2002: Laura C Cooper; Emma J Carlson; José L Castro; Gary G Chicchi; Kevin Dinnell; Jerry Di Salvo; Jason M Elliott; Gregory J Hollingworth; Marc M Kurtz; Mark P Ridgill; Wayne Rycroft; Kwei-Lan Tsao; Christopher J Swain
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
Bioorganic & medicinal chemistry letters 2002;12(13):1759-62.
2002: Jason M Elliott; José L Castro; Gary G Chicchi; Laura C Cooper; Kevin Dinnell; Gregory J Hollingworth; Mark P Ridgill; Wayne Rycroft; Marc M Kurtz; Duncan E Shaw; Christopher J Swain; Kwei-Lan Tsao; Lihu Yang
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
Bioorganic & medicinal chemistry letters 2002;12(13):1755-8.
2002: Karen A Maubach; Karine Martin; Gary G Chicchi; Timothy Harrison; Alan Wheeldon; Christopher J Swain; Michael J Cumberbatch; Nadia M J Rupniak; Guy R Seabrook
Chronic substance P (NK1) receptor antagonist and conventional antidepressant treatment increases burst firing of monoamine neurones in the locus coeruleus.
Neuroscience 2002;109(3):609-17.
2001: Duncan Shaw; Gary G Chicchi; Jason M Elliott; Marc M Kurtz; Denise Morrison; Mark P Ridgill; N Szeto; Alan P Watt; Angela R Williams; Christopher J Swain
2-Aryl indole NK(1) antagonists: optimisation of the amide substituent.
Bioorganic & medicinal chemistry letters 2001;11(23):3031-4.
2001: Timothy Harrison; Andrew P Owens; Brian J Williams; Christopher J Swain; A Williams; Emma J Carlson; Wayne Rycroft; F David Tattersall; Margaret A Cascieri; Gary G Chicchi; Sharon Sadowski; Nadia M J Rupniak; Richard Hargreaves
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
Journal of medicinal chemistry 2001;44(24):4296-9.
2001: Kevin Dinnell; Gary G Chicchi; M J Dhar; Jason M Elliott; Gregory J Hollingworth; Marc M Kurtz; Mark P Ridgill; Wayne Rycroft; Kwei-Lan Tsao; Angela R Williams; Christopher J Swain
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Bioorganic & medicinal chemistry letters 2001;11(9):1237-40.
2001: Laura C Cooper; Gary G Chicchi; Kevin Dinnell; Jason M Elliott; Gregory J Hollingworth; Marc M Kurtz; Karen Locker; Denise Morrison; Duncan E Shaw; Kwei-Lan Tsao; Alan P Watt; Angela R Williams; Christopher J Swain
2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
Bioorganic & medicinal chemistry letters 2001;11(9):1233-6.
2001: Janusz J Kulagowski; Neil R Curtis; Christopher J Swain; Brian J Williams
Stereocontrolled syntheses of epimeric 3-aryl-6-phenyl-1-oxa-7-azaspiro(4.5)decane NK-1 receptor antagonist precursors.
Organic letters 2001;3(5):667-70.
2000: Sarah J Harper; Michael Saporito; Louise Hewson; L Young; David Smith; Michael Rigby; P Jackson; Neil R Curtis; Christopher J Swain; Franz Hefti; Jeffry L Vaught; DJ Sirinathsinghji
CEP-1347 increases ChAT activity in culture and promotes cholinergic neurone survival following fimbria-fornix lesion.
Neuroreport 2000;11(10):2271-6.
1999: Sarah Harper; James Bilsland; L Young; Linda J Bristow; Susan Boyce; Glenn Mason; Michael Rigby; Louise Hewson; David Smith; Ruth O'Donnell; desmond oconnor; Raymond G Hill; D Evans; Christopher J Swain; B Williams; Franz Hefti
Analysis of the neurotrophic effects of GPI-1046 on neuron survival and regeneration in culture and in vivo.
Neuroscience 1999;88(1):257-67.
1998: GI Stevenson; Ian T Huscroft; Angus M MacLeod; Christopher J Swain; Margaret A Cascieri; Gary G Chicchi; M I Graham; Timothy Harrison; Fintan J Kelleher; Marc M Kurtz; Tammy Ladduwahetty; Kevin J Merchant; Joseph M Metzger; D Euan MacIntyre; Sharon Sadowski; Bindi Sohal; Andrew P Owens
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Journal of medicinal chemistry 1998;41(23):4623-35.
1998: Mark S Kramer; N Cutler; J Feighner; R Shrivastava; J Carman; J J Sramek; Scott A Reines; G Liu; Duane Snavely; E Wyatt-Knowles; Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Christopher J Swain; Timothy Harrison; Raymond G Hill; Franz Hefti; Edward M Scolnick; Margaret A Cascieri; Gary G Chicchi; Sharon Sadowski; Angela R Williams; Louise Hewson; David Smith; Emma J Carlson; Richard Hargreaves; Nadia M J Rupniak
Distinct mechanism for antidepressant activity by blockade of central substance P receptors.
Science (New York, N.Y.) 1998;281(5383):1640-5.
1998: Timothy Harrison; M P Korsgaard; Christopher J Swain; Margaret A Cascieri; Sharon Sadowski; Guy R Seabrook
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Bioorganic & medicinal chemistry letters 1998;8(11):1343-8.
1998: Andrew P Owens; Timothy Harrison; J D Moseley; Christopher J Swain; Sharon Sadowski; Margaret A Cascieri
High affinity phenylglycinol-based NK1 receptor antagonists.
Bioorganic & medicinal chemistry letters 1998;8(1):51-6.
1998: Christopher J Swain
Neurokinin receptor antagonists.
Progress in medicinal chemistry 1998;35():57-81.
1997: Nadia M J Rupniak; F David Tattersall; Angela R Williams; Wayne Rycroft; Emma J Carlson; Margaret A Cascieri; Sharon Sadowski; E Ber; Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Eileen M Seward; Ian T Huscroft; S Owen; Christopher J Swain; Raymond G Hill; Richard Hargreaves
In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists.
European journal of pharmacology 1997;326(2-3):201-9.
1996: Tung M Fong; H Yu; Ruey-Ruey C Huang; Margaret A Cascieri; Christopher J Swain
Relative contribution of polar interactions and conformational compatibility to the binding of neurokinin-1 receptor antagonists.
Molecular pharmacology 1996;50(6):1605-11.
1996: Tammy Ladduwahetty; R Baker; Margaret A Cascieri; M S Chambers; K Haworth; L E Keown; D Euan MacIntyre; Joseph M Metzger; S Owen; Wayne Rycroft; Sharon Sadowski; E M Seward; Sara Shepheard; Christopher J Swain; F David Tattersall; Alan P Watt; D W Williamson; Richard Hargreaves
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Journal of medicinal chemistry 1996;39(15):2907-14.
1996: F David Tattersall; Wayne Rycroft; B Francis; D Pearce; Kevin J Merchant; Angus M MacLeod; Tammy Ladduwahetty; L Keown; Christopher J Swain; R Baker; Margaret A Cascieri; E Ber; J Metzger; D Euan MacIntyre; Raymond G Hill; Richard Hargreaves
Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets.
Neuropharmacology 1996;35(8):1121-9.
1995: Christopher J Swain; E M Seward; Margaret A Cascieri; Tung M Fong; R Herbert; D Euan MacIntyre; Kevin J Merchant; S N Owen; Andrew P Owens; V Sabin
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
Journal of medicinal chemistry 1995;38(24):4793-805.
1995: Tung M Fong; R C Huang; H Yu; Christopher J Swain; D Underwood; Margaret A Cascieri; Catherine D Strader
Mutational analysis of neurokinin receptor function.
Canadian journal of physiology and pharmacology 1995;73(7):860-5.
1995: Margaret A Cascieri; LL Shiao; Sander G Mills; Malcolm MacCoss; Christopher J Swain; H Yu; E Ber; Sharon Sadowski; M T Wu; Catherine D Strader
Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists.
Molecular pharmacology 1995;47(4):660-5.
1994: Tung M Fong; H Yu; Margaret A Cascieri; D Underwood; Christopher J Swain; Catherine D Strader
Interaction of glutamine 165 in the fourth transmembrane segment of the human neurokinin-1 receptor with quinuclidine antagonists.
The Journal of biological chemistry 1994;269(21):14957-61.
1994: Angus M MacLeod; Kevin J Merchant; F Brookfield; F Kelleher; G Stevenson; Andrew P Owens; Christopher J Swain; M A Casiceri; Sharon Sadowski; E Ber
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Journal of medicinal chemistry 1994;37(9):1269-74.
1994: Margaret A Cascieri; Angus M MacLeod; D Underwood; LL Shiao; E Ber; Sharon Sadowski; H Yu; Kevin J Merchant; Christopher J Swain; Catherine D Strader
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.
The Journal of biological chemistry 1994;269(9):6587-91.
1994: Tung M Fong; H Yu; Margaret A Cascieri; D Underwood; Christopher J Swain; Catherine D Strader
The role of histidine 265 in antagonist binding to the neurokinin-1 receptor.
The Journal of biological chemistry 1994;269(4):2728-32.
1994: B E Francis; Christopher J Swain; V Sabin; H Donald Burns
Radioiodinated L-703,606: a potent, selective antagonist to the human NK1 receptor.
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine 1994;45(1):97-103.
1993: Angus M MacLeod; Kevin J Merchant; Margaret A Cascieri; Sharon Sadowski; E Ber; Christopher J Swain; R Baker
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Journal of medicinal chemistry 1993;36(14):2044-5.
1993: Tung M Fong; Margaret A Cascieri; H Yu; A Bansal; Christopher J Swain; Catherine D Strader
Amino-aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345.
Nature 1993;362(6418):350-3.
1992: Margaret A Cascieri; E Ber; Tung M Fong; Sharon Sadowski; A Bansal; Christopher J Swain; E Seward; B Frances; D Burns; Catherine D Strader
Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor.
Molecular pharmacology 1992;42(3):458-63.
1992: Christopher J Swain; R Baker; C Kneen; R Herbert; J Moseley; J Saunders; E M Seward; GI Stevenson; M Beer; J Stanton
Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)-oxazoles).
Journal of medicinal chemistry 1992;35(6):1019-31.
1991: Christopher J Swain; R Baker; C Kneen; J Moseley; J Saunders; E M Seward; G Stevenson; M Beer; J Stanton; K Watling
Novel 5-HT3 antagonists. Indole oxadiazoles.
Journal of medicinal chemistry 1991;34(1):140-51.
1990: Ruth M McKernan; N P Gillard; Kathleen Quirk; C O Kneen; GI Stevenson; Christopher J Swain; C Ian Ragan
Purification of the 5-hydroxytryptamine 5-HT3 receptor from NCB20 cells.
The Journal of biological chemistry 1990;265(23):13572-7.
1989: F Watjen; R Baker; M Engelstoff; R Herbert; A MacLeod; A Knight; Kevin J Merchant; J Moseley; J Saunders; Christopher J Swain
Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines.
Journal of medicinal chemistry 1989;32(10):2282-91.
1988: K J Watling; S Aspley; Christopher J Swain; J Saunders
[3H]quaternised ICS 205-930 labels 5-HT3 receptor binding sites in rat brain.
European journal of pharmacology 1988;149(3):397-8.