Christopher Langmead

Dr

20012020

Research output per year

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Research Output

2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Budzik, B., Garzya, V., Shi, D., Foley, J. J., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T. & Jin, JI., 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 12, p. 3540-3544 5 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling

Budzik, B., Garzya, V., Shi, D., Walker, G., Lauchart, Y., Lucas, A. J., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T. & Jin, JI., 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 12, p. 3545-3549 5 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Acetylcholine Muscarinic M4 Receptors as a Therapeutic Target for Alcohol Use Disorder: Converging Evidence From Humans and Rodents

Walker, L. C., Berizzi, A. E., Chen, N. A., Rueda, P., Perreau, V. M., Huckstep, K., Srisontiyakul, J., Govitrapong, P., Xiaojian, J., Lindsley, C. W., Jones, C. K., Riddy, D. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 28 Feb 2020, (Accepted/In press) In : Biological Psychiatry. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Lebon, G., Warne, T., Edwards, P. C., Bennett, K. A., Langmead, C. J., Leslie, A. G. W. & Tate, C. G., 23 Jun 2011, In : Nature. 474, 7352, p. 521-526 6 p.

Research output: Contribution to journalArticleResearchpeer-review

598 Citations (Scopus)

Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

Langmead, C. J. & Christopoulos, A., 2006, In : Trends in Pharmacological Sciences. 27, 9, p. 475 - 481 7 p.

Research output: Contribution to journalArticleResearchpeer-review

104 Citations (Scopus)

Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands

Mould, R., Brown, J., Marshall, F. H. & Langmead, C. J., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 351-363 13 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes S

Bradley, S. J., Molloy, C., Bundgaard, C., Mogg, A. J., Thompson, K. J., Dwomoh, L., Sanger, H. E., Crabtree, M. D., Brooke, S. M., Sexton, P. M., Felder, C. C., Christopoulos, A., Broad, L. M., Tobin, A. B. & Langmead, C. J., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 645-656 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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10 Citations (Scopus)

Characterisation of the binding of [ 3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor

Langmead, C. J., Jerman, J. C., Brough, S. J., Scott, C., Porter, R. A. & Herdon, H. J., 1 Jan 2004, In : British Journal of Pharmacology. 141, 2, p. 340-346 7 p.

Research output: Contribution to journalArticleResearchpeer-review

117 Citations (Scopus)

Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1

Langmead, C. J., Austin, N. E., Branch, C. L., Brown, J. T., Buchanan, K. A., Davies, C. H., Forbes, I. T., Fry, V. A. H., Hagan, J. J., Herdon, H. J., Jones, G. A., Jeggo, R. D., Kew, J. N. C., Mazzali, A., Melarange, R. A., Patel, N., Pardoe, J., Randall, A. D., Roberts, C. J., Roopun, A. K. & 6 others, Starr, K. R., Teriakidis, A., Wood, M. D., Whittington, M. A., Wu, Z. & Watson, J. M., 2008, In : British Journal of Pharmacology. 154, 5, p. 1104 - 1115 12 p.

Research output: Contribution to journalArticleResearchpeer-review

96 Citations (Scopus)

Characterization of the binding of [ 125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor

Langmead, C. J., Szekeres, P. G., Chambers, J. K., Ratcliffe, S. J., Jones, D. N. C., Hirst, W. D., Price, G. W. & Herdon, H. J., 1 Jan 2001, In : British Journal of Pharmacology. 131, 4, p. 683-688 6 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research

Riddy, D. M., Goy, E., Delerive, P., Summers, R. J. & Langmead, C. J., 1 May 2018, In : PLoS ONE. 13, 5, 19 p., e0197177.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Contrasting effects of allosteric and orthosteric agonists on M1 muscarinic acetylcholine receptor internalization and down-regulation

Thomas, R. L., Langmead, C. J., Wood, M. D. & Challiss, R. A. J., Dec 2009, In : Journal of Pharmacology and Experimental Therapeutics. 331, 3, p. 1086-1095 10 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Crystal structure of the M5 muscarinic acetylcholine receptor

Vuckovic, Z., Gentry, P. R., Berizzi, A. E., Hirata, K., Varghese, S., Thompson, G., van der Westhuizen, E. T., Burger, W. A. C., Rahmani, R., Valant, C., Langmead, C. J., Lindsley, C. W., Baell, J. B., Tobin, A. B., Sexton, P. M., Christopoulos, A. & Thal, D. M., 17 Dec 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 51, p. 26001-26007 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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3 Citations (Scopus)

Determining allosteric modulator mechanism of action: Integration of radioligand binding and functional assay data

Langmead, C. J., 2011, In : Methods in Molecular Biology. 746, p. 195-209 15 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

Bender, A. M., Cho, H. P., Nance, K. D., Lingenfelter, K. S., Luscombe, V. B., Gentry, P. R., Voigtritter, K., Berizzi, A. E., Sexton, P. M., Langmead, C. J., Christopoulos, A., Locuson, C. W., Bridges, T. M., Chang, S., O'Neill, J. C., Zhan, X., Niswender, C. M., Jones, C. K., Conn, P. J. & Lindsley, C. W., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1572-1581 10 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Discovery of 1,2,4-triazine derivatives as adenosine A2A antagonists using structure based drug design

Congreve, M., Andrews, S. P., Dore, A. S., Hollenstein, K., Hurrell, E., Langmead, C. J., Mason, J. S., Ng, I. W., Tehan, B. G., Zhukov, A., Weir, M. & Marshall, F. H., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 1898 - 1903 6 p.

Research output: Contribution to journalArticleResearchpeer-review

231 Citations (Scopus)

Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties

Christopher, J. A., Aves, S. J., Brown, J., Errey, J. C., Klair, S. S., Langmead, C. J., Mace, O. J., Mould, R., Patel, J. C., Tehan, B. G., Zhukov, A., Marshall, F. H. & Congreve, M., 1 May 2015, In : MedChemComm. 6, 5, p. 947-955 9 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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7 Citations (Scopus)

Evaluation of expression and function of the H+/myo-inositol transporter HMIT

Di Daniel, E., Mok, M. H. S., Mead, E., Mutinelli, C., Zambello, E., Caberlotto, L., Pell, T. J., Langmead, C. J., Shah, A. J., Duddy, G., Kew, J. N. C. & Maycox, P. R., 16 Jul 2009, In : BMC Cell Biology. 10, 54.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

From orphans to orexins: An arousing fifteen years

Langmead, C. J., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 281-282 2 p.

Research output: Contribution to journalEditorialOtherpeer-review

Functional and structural perspectives on allosteric modulation of GPCRs

Langmead, C. J. & Christopoulos, A., 2014, In : Current Opinion in Cell Biology. 27, 1, p. 94 - 101 8 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

G protein-coupled receptors as anabolic drug targets in osteoporosis

Diepenhorst, N., Rueda, P., Cook, A. E., Pastoureau, P., Sabatini, M. & Langmead, C. J., 1 Apr 2018, In : Pharmacology and Therapeutics. 184, p. 1-12 12 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

4 Citations (Scopus)

G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus

Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. & Langmead, C. J., 1 Jan 2018, In : Pharmacological Reviews. 70, 1, p. 39-67 29 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

29 Citations (Scopus)

G protein coupling and signaling pathway activation by M1 muscarinic acetylcholine receptor orthosteric and allosteric agonists

Thomas, R. L., Mistry, R., Langmead, C. J., Wood, M. D. & Challiss, R. A. J., 2008, In : Journal of Pharmacology and Experimental Therapeutics. 327, 2, p. 365 - 374 10 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Gαo1 by the ghrelin receptor

Bennett, K. A., Langmead, C. J., Wise, A. & Milligan, G., Oct 2009, In : Molecular Pharmacology. 76, 4, p. 802-811 10 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

High throughput, quantitative analysis of human osteoclast differentiation and activity

Diepenhorst, N., Nowell, C., Rueda, P., Henriksen, K., Pierce, T., Cook, A., Pastoureau, P., Sabatini, M., Charman, W., Christopoulos, A., Summers, R., Sexton, P. & Langmead, C., 15 Feb 2017, In : Analytical Biochemistry. 519, p. 51-56 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Identification of novel adenosine A2A receptor antagonists by virtual screening

Langmead, C. J., Andrews, S. P., Congreve, M., Errey, J. C., Hurrell, E., Marshall, F. H., Mason, J. S., Richardson, C. M., Robertson, N., Zhukov, A. & Weir, M., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 1904 - 1909 6 p.

Research output: Contribution to journalArticleResearchpeer-review

99 Citations (Scopus)

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R., Pin, J. P., Sexton, P., Kenakin, T. P., Ehlert, F. J., Spedding, M. & Langmead, C. J., 2014, In : Pharmacological Reviews. 66, 4, p. 918 - 947 30 p.

Research output: Contribution to journalArticleResearchpeer-review

119 Citations (Scopus)

In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics

Dawson, L. A., Langmead, C. J., Dada, A., Watson, J. M., Wu, Z., de la Flor, R., Jones, G. A., Cluderay, J. E., Southam, E., Murkitt, G. S., Hill, M. D., Jones, D. N. C., Davies, C. H., Hagan, J. J. & Smith, P. W., 10 Feb 2010, In : European Journal of Pharmacology. 627, 1-3, p. 106-114 9 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Isoform-specific biased agonism of histamine H3 receptor agonists

Riddy, D. M., Cook, A. E., Diepenhorst, N. A., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Feb 2017, In : Molecular Pharmacology. 91, 2, p. 87-99 13 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Isoform-specific bias of histamine H3 receptor agonists

Riddy, D., Cook, A. E., Diepenhorst, N., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R., Charman, W., Sexton, P. M., Christopoulos, A. & Langmead, C., 2016.

Research output: Contribution to conferencePoster

Ligand properties and behaviours in an allosteric age

Langmead, C. J., Dec 2012, In : Trends in Pharmacological Sciences. 33, 12, p. 621-622 2 p.

Research output: Contribution to journalLetterOtherpeer-review

5 Citations (Scopus)

Matching models to data: A receptor pharmacologist's guide

Hall, D. A. & Langmead, C. J., Nov 2010, In : British Journal of Pharmacology. 161, 6, p. 1276-1290 15 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

15 Citations (Scopus)

Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators

Berizzi, A. E., Gentry, P. R., Rueda, P., Hoedt, S. D., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 1 Oct 2016, In : Molecular Pharmacology. 90, 4, p. 427-436 10 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Molecular pharmacology of GPCRs

Langmead, C. J. & Summers, R. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4005-4008 4 p.

Research output: Contribution to journalEditorialOther

Open Access
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3 Citations (Scopus)

Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment

Hutchings, C. J., Cseke, G., Osborne, G., Woolard, J., Zhukov, A., Koglin, M., Jazayeri, A., Pandya-Pathak, J., Langmead, C. J., Hill, S. J., Weir, M. & Marshall, F. H., Jan 2014, In : mAbs. 6, 1, p. 246-261 16 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
27 Citations (Scopus)

Muscarinic acetylcholine receptors as CNS drug targets

Langmead, C. J., Watson, J. M. & Reavill, C., 2008, In : Pharmacology and Therapeutics. 117, 2, p. 232 - 243 12 p.

Research output: Contribution to journalArticleResearchpeer-review

303 Citations (Scopus)

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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13 Citations (Scopus)

Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors

Lebon, G., Langmead, C. J., Tehan, B. G. & Hulme, E. C., 2009, In : Molecular Pharmacology. 75, 2, p. 331 - 341 11 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

N-desmethylclozapine (NDMC) is an antagonist at the human native muscarinic M1 receptor

Thomas, D. R., Dada, A., Jones, G. A., Deisz, R. A., Gigout, S., Langmead, C. J., Werry, T. D., Hendry, N., Hagan, J. J., Davies, C. H. & Watson, J. M., 1 Jun 2010, In : Neuropharmacology. 58, 8, p. 1206-1214 9 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within the 7-transmembrane domain

Josephs, T. M., Keller, A. N., Khajehali, E., DeBono, A., Langmead, C. J., Conigrave, A. D., Capuano, B., Kufareva, I., Gregory, K. J. & Leach, K., Apr 2020, In : British Journal of Pharmacology. 177, 8, p. 1917-1930 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Neurochemical changes in LPA1 receptor deficient mice - A putative model of schizophrenia

Roberts, C., Winter, P., Shilliam, C. S., Hughes, Z. A., Langmead, C., Maycox, P. R. & Dawson, L. A., 1 Mar 2005, In : Neurochemical Research. 30, 3, p. 371-377 7 p.

Research output: Contribution to journalArticleResearchpeer-review

44 Citations (Scopus)

Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone

Hughes, Z. A., Starr, K. R., Langmead, C. J., Hill, M., Bartoszyk, G. D., Hagan, J. J., Middlemiss, D. N. & Dawson, L. A., 7 Mar 2005, In : European Journal of Pharmacology. 510, 1-2, p. 49-57 9 p.

Research output: Contribution to journalArticleResearchpeer-review

94 Citations (Scopus)