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MJ Sheardown

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Thøger Rasmussen; Anders Fink-Jensen; Per Sauerberg; MD Swedberg; C Thomsen; MJ Sheardown; Lone Jeppesen; David O Calligaro; Neil DeLapp; CA Whitesitt; JS Ward; Harlan E Shannon; Frank P Bymaster
The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidance.
Thøger Rasmussen; Per Sauerberg; EB Nielsen; MD Swedberg; C Thomsen; MJ Sheardown; Lone Jeppesen; David O Calligaro; Neil DeLapp; CA Whitesitt; JS Ward; Harlan E Shannon; Frank P Bymaster; Anders Fink-Jensen
Muscarinic receptor agonists decrease cocaine self-administration rates in drug-naive mice.
Harlan E Shannon; Kurt Rasmussen; Frank P Bymaster; J C Hart; Steven C Peters; MD Swedberg; Lone Jeppesen; MJ Sheardown; Per Sauerberg; Anders Fink-Jensen
Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice.

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All Publications

2001: Thøger Rasmussen; Anders Fink-Jensen; Per Sauerberg; MD Swedberg; C Thomsen; MJ Sheardown; Lone Jeppesen; David O Calligaro; Neil DeLapp; CA Whitesitt; JS Ward; Harlan E Shannon; Frank P Bymaster
The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidance.
Schizophrenia research 2001;49(1-2):193-201.
2000: Thøger Rasmussen; Per Sauerberg; EB Nielsen; MD Swedberg; C Thomsen; MJ Sheardown; Lone Jeppesen; David O Calligaro; Neil DeLapp; CA Whitesitt; JS Ward; Harlan E Shannon; Frank P Bymaster; Anders Fink-Jensen
Muscarinic receptor agonists decrease cocaine self-administration rates in drug-naive mice.
European journal of pharmacology 2000;402(3):241-6.
2000: Harlan E Shannon; Kurt Rasmussen; Frank P Bymaster; J C Hart; Steven C Peters; MD Swedberg; Lone Jeppesen; MJ Sheardown; Per Sauerberg; Anders Fink-Jensen
Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice.
Schizophrenia research 2000;42(3):249-59.
1999: Lars Knutsen; J Lau; H Petersen; C Thomsen; J U Weis; M Shalmi; Martin Judge; A J Hansen; MJ Sheardown
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Journal of medicinal chemistry 1999;42(18):3463-77.
1999: Harlan E Shannon; J C Hart; Frank P Bymaster; David O Calligaro; Neil DeLapp; Charles H Mitch; JS Ward; Anders Fink-Jensen; Per Sauerberg; Lone Jeppesen; MJ Sheardown; MD Swedberg
Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats.
The Journal of pharmacology and experimental therapeutics 1999;290(2):901-7.
1999: Lone Jeppesen; Preben Olesen; L Hansen; MJ Sheardown; C Thomsen; Thøger Rasmussen; A F Jensen; M S Christensen; Karin Rimvall; JS Ward; CA Whitesitt; David O Calligaro; Frank P Bymaster; Neil DeLapp; Christian Felder; Harlan E Shannon; Per Sauerberg
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.
Journal of medicinal chemistry 1999;42(11):1999-2006.
1999: Frank P Bymaster; Harlan E Shannon; Kurt Rasmussen; Neil DeLapp; JS Ward; David O Calligaro; Charles H Mitch; CA Whitesitt; TS Ludvigsen; MJ Sheardown; MD Swedberg; Thøger Rasmussen; Preben Olesen; Lone Jeppesen; Per Sauerberg; Anders Fink-Jensen
Potential role of muscarinic receptors in schizophrenia.
Life sciences 1999;64(6-7):527-34.
1998: Anders Fink-Jensen; P Kristensen; Harlan E Shannon; David O Calligaro; Neil DeLapp; CA Whitesitt; JS Ward; C Thomsen; T Rasmusseen; MJ Sheardown; Lone Jeppesen; Per Sauerberg; Frank P Bymaster
Muscarinic agonists exhibit functional dopamine antagonism in unilaterally 6-OHDA lesioned rats.
Neuroreport 1998;9(15):3481-6.
1998: Per Sauerberg; Lone Jeppesen; Preben Olesen; Thøger Rasmussen; MD Swedberg; MJ Sheardown; Anders Fink-Jensen; C Thomsen; H Thøgersen; Karin Rimvall; JS Ward; David O Calligaro; Neil DeLapp; Frank P Bymaster; Harlan E Shannon
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
Journal of medicinal chemistry 1998;41(22):4378-84.
1998: Per Sauerberg; Lone Jeppesen; Preben Olesen; MJ Sheardown; Anders Fink-Jensen; Thøger Rasmussen; Karin Rimvall; Harlan E Shannon; Frank P Bymaster; Neil DeLapp; David O Calligaro; JS Ward; CA Whitesitt; C Thomsen
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.
Bioorganic & medicinal chemistry letters 1998;8(20):2897-902.
1998: Frank P Bymaster; Harlan E Shannon; Kurt Rasmussen; Neil DeLapp; Charles H Mitch; JS Ward; David O Calligaro; TS Ludvigsen; MJ Sheardown; Preben Olesen; MD Swedberg; Per Sauerberg; Anders Fink-Jensen
Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane .
European journal of pharmacology 1998;356(2-3):109-19.
1998: Frank P Bymaster; Petra A Carter; Steven C Peters; Wei Zhang; JS Ward; Charles H Mitch; David O Calligaro; CA Whitesitt; Neil DeLapp; Harlan E Shannon; Karin Rimvall; Lone Jeppesen; MJ Sheardown; Anders Fink-Jensen; Per Sauerberg
Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects.
Brain research 1998;795(1-2):179-90.
1998: GM Castillo; J A Cummings; W Yang; Martin Judge; MJ Sheardown; Karin Rimvall; J B Hansen; AD Snow
Sulfate content and specific glycosaminoglycan backbone of perlecan are critical for perlecan's enhancement of islet amyloid polypeptide (amylin) fibril formation.
Diabetes 1998;47(4):612-20.
1998: Neil DeLapp; S Wu; R Belagaje; E Johnstone; S Little; Harlan Shannon; Frank P Bymaster; David O Calligaro; Charles H Mitch; CA Whitesitt; J Ward; MJ Sheardown; Anders Fink-Jensen; Lone Jeppesen; C Thomsen; Per Sauerberg
Effects of the M1 agonist xanomeline on processing of human beta-amyloid precursor protein (FAD, Swedish mutant) transfected into Chinese hamster ovary-m1 cells.
Biochemical and biophysical research communications 1998;244(1):156-60.
1998: JS Ward; L Merritt; David O Calligaro; Frank P Bymaster; Harlan E Shannon; Charles H Mitch; CA Whitesitt; D Brunsting; MJ Sheardown; Preben Olesen; MD Swedberg; Lone Jeppesen; Per Sauerberg
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
Journal of medicinal chemistry 1998;41(3):379-92.
1998: Per Sauerberg; Preben Olesen; MJ Sheardown; Karin Rimvall; H Thøgersen; Harlan E Shannon; BD Sawyer; JS Ward; Frank P Bymaster; Neil DeLapp; David O Calligaro; MD Swedberg
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.
Journal of medicinal chemistry 1998;41(1):109-16.
1997: Harlan E Shannon; MJ Sheardown; Frank P Bymaster; David O Calligaro; Neil DeLapp; J Gidda; Charles H Mitch; BD Sawyer; Peter stengel; JS Ward; David T Wong; Preben Olesen; PD Suzdak; Per Sauerberg; MD Swedberg
Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053): a novel analgesic with mixed muscarinic receptor agonist and antagonist activity.
The Journal of pharmacology and experimental therapeutics 1997;281(2):884-94.
1997: MD Swedberg; MJ Sheardown; Per Sauerberg; Preben Olesen; PD Suzdak; Kristian Tage Hansen; Frank P Bymaster; JS Ward; Charles H Mitch; David O Calligaro; Neil DeLapp; Harlan E Shannon
Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic.
The Journal of pharmacology and experimental therapeutics 1997;281(2):876-83.
1997: MJ Sheardown; Harlan E Shannon; MD Swedberg; PD Suzdak; Frank P Bymaster; Preben Olesen; Charles H Mitch; JS Ward; Per Sauerberg
M1 receptor agonist activity is not a requirement for muscarinic antinociception.
The Journal of pharmacology and experimental therapeutics 1997;281(2):868-75.
1997: Charles H Mitch; T J Brown; Frank P Bymaster; David O Calligaro; Donna K Dieckman; L Merrit; Steven C Peters; Steven J Quimby; Harlan E Shannon; L A Shipley; JS Ward; K Hansen; Preben Olesen; Per Sauerberg; MJ Sheardown; MD Swedberg; PD Suzdak; B Greenwood
Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome.
Journal of medicinal chemistry 1997;40(4):538-46.
1997: Harlan E Shannon; DE Womer; Frank P Bymaster; David O Calligaro; N C DeLapp; Charles H Mitch; JS Ward; CA Whitesitt; MD Swedberg; MJ Sheardown; Anders Fink-Jensen; Preben Olesen; Karin Rimvall; Per Sauerberg
In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist.
Life sciences 1997;60(13-14):969-76.
1996: MJ Sheardown; C Thomsen
Phenylglycines can evoke quisqualate-primed depolarizations in rat cingulate cortex: an effect associated with [3H]DL-AP4 uptake.
The European journal of neuroscience 1996;8(12):2599-604.
1995: JS Ward; L Merritt; David O Calligaro; Frank P Bymaster; Harlan E Shannon; BD Sawyer; Charles H Mitch; J B Deeter; Steven C Peters; MJ Sheardown
Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles.
Journal of medicinal chemistry 1995;38(18):3469-81.
1995: Per Sauerberg; Preben Olesen; MJ Sheardown; PD Suzdak; Harlan E Shannon; Frank P Bymaster; David O Calligaro; Charles H Mitch; JS Ward; MD Swedberg
Muscarinic agonists as analgesics. Antinociceptive activity versus M1 activity: SAR of alkylthio-TZTP's and related 1,2,5-thiadiazole analogs.
Life sciences 1995;56(11-12):807-14.
1994: C Thomsen; H Klitgaard; MJ Sheardown; H C Jackson; K Eskesen; P Jacobsen; S Treppendahl; PD Suzdak
(S)-4-carboxy-3-hydroxyphenylglycine, an antagonist of metabotropic glutamate receptor (mGluR) 1a and an agonist of mGluR2, protects against audiogenic seizures in DBA/2 mice.
Journal of neurochemistry 1994;62(6):2492-5.
1994: Frank P Bymaster; David T Wong; Charles H Mitch; JS Ward; David O Calligaro; Darryle D Schoepp; Harlan E Shannon; MJ Sheardown; Preben Olesen; PD Suzdak
Neurochemical effects of the M1 muscarinic agonist xanomeline (LY246708/NNC11-0232).
The Journal of pharmacology and experimental therapeutics 1994;269(1):282-9.
1994: Harlan E Shannon; Frank P Bymaster; David O Calligaro; B Greenwood; Charles H Mitch; BD Sawyer; JS Ward; David T Wong; Preben Olesen; MJ Sheardown
Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors.
The Journal of pharmacology and experimental therapeutics 1994;269(1):271-81.
1993: PD Suzdak; MJ Sheardown
Effect of the non-NMDA receptor antagonist, 2,3-dihydro-6-nitro-7-sulfamoylbenzo(f)quinoxaline, on local cerebral glucose uptake in the limbic forebrain.
Journal of neurochemistry 1993;61(4):1577-80.
1993: MJ Sheardown; PD Suzdak; L Nordholm
AMPA, but not NMDA, receptor antagonism is neuroprotective in gerbil global ischaemia, even when delayed 24 h.
European journal of pharmacology 1993;236(3):347-53.
1993: PD Suzdak; MJ Sheardown; T Honoré
Characterization of the metabotropic glutamate receptor in mouse cerebellar granule cells: lack of effect of 2,3-dihydroxy-6-nitro-7-sulphamoylbenzo(F)-quinoxaline (NBQX).
European journal of pharmacology 1993;245(3):215-20.
1992: Nils Henrik Diemer; M B Jørgensen; Flemming Fryd Johansen; MJ Sheardown; T Honoré
Protection against ischemic hippocampal CA1 damage in the rat with a new non-NMDA antagonist, NBQX.
Acta neurologica Scandinavica 1992;86(1):45-9.
1992: Per Sauerberg; Preben Olesen; S Nielsen; S Treppendahl; MJ Sheardown; T Honoré; Charles H Mitch; JS Ward; A J Pike; Frank P Bymaster
Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines .
Journal of medicinal chemistry 1992;35(12):2274-83.
1991: Martin Judge; MJ Sheardown; P Jacobsen; T Honoré
Protection against post-ischemic behavioral pathology by the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX) in the gerbil.
Neuroscience letters 1991;133(2):291-4.
1991: Per Sauerberg; J W Kindtler; L Nielsen; MJ Sheardown; T Honoré
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships.
Journal of medicinal chemistry 1991;34(2):687-92.
1990: MJ Sheardown; E O Nielsen; A J Hansen; P Jacobsen; T Honoré
2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: a neuroprotectant for cerebral ischemia.
Science (New York, N.Y.) 1990;247(4942):571-4.
1990: T Honore; MJ Sheardown; E O Nielsen; Jørgen Drejer; A J Hansen
Specific quisqualate receptor ligand blocks both kainate and quisqualate responses.
Advances in experimental medicine and biology 1990;268():65-71.
1989: MJ Sheardown; Jørgen Drejer; LH Jensen; C E Stidsen; T Honoré
A potent antagonist of the strychnine insensitive glycine receptor has anticonvulsant properties.
European journal of pharmacology 1989;174(2-3):197-204.
1989: Jørgen Drejer; MJ Sheardown; E O Nielsen; T Honoré
Glycine reverses the effect of HA-966 on NMDA responses in cultured rat cortical neurons and in chick retina.
Neuroscience letters 1989;98(3):333-8.