Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor

Peter Keov; Celine Valant; Shane M. Devine; J. Robert Lane; Peter J. Scammells; Patrick M. Sexton; Arthur Christopoulos

doi:10.1124/mol.113.087320

Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor

Molecular Pharmacology ◽

10.1124/mol.113.087320 ◽

2013 ◽

Vol 84 (3) ◽

pp. 425-437 ◽

Cited By ~ 23

Author(s):

Peter Keov ◽

Celine Valant ◽

Shane M. Devine ◽

J. Robert Lane ◽

Peter J. Scammells ◽

...

Keyword(s):

Reverse Engineering ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Muscarinic Acetylcholine ◽

Modes Of Action ◽

Selective Agonist ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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5-HT2A receptor- and M1 muscarinic acetylcholine receptor-mediated Galpha(q) signalling in patients with psychiatric disorders

10.26226/morressier.5b68175eb56e9b005965c3a3 ◽

2018 ◽

Author(s):

Yuji Odagaki

Keyword(s):

Psychiatric Disorders ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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5-HT2A receptor- and M1 muscarinic acetylcholine receptor-mediated activation of Gαq/11 in postmortem dorsolateral prefrontal cortex of opiate addicts

Pharmacological Reports ◽

10.1007/s43440-021-00248-w ◽

2021 ◽

Author(s):

Yuji Odagaki ◽

Masakazu Kinoshita ◽

J. Javier Meana ◽

Luis F. Callado ◽

Jesús A. García-Sevilla

Keyword(s):

Prefrontal Cortex ◽

Acetylcholine Receptor ◽

Dorsolateral Prefrontal Cortex ◽

Muscarinic Acetylcholine Receptor ◽

Muscarinic Acetylcholine ◽

Dorsolateral Prefrontal ◽

Opiate Addicts ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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Pharmacological Assessment of M1 Muscarinic Acetylcholine Receptor-Gq/11 Protein Coupling in Membranes Prepared from Postmortem Human Brain Tissue

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.108.137968 ◽

2008 ◽

Vol 325 (3) ◽

pp. 869-874 ◽

Cited By ~ 20

Author(s):

Hasib Salah-Uddin ◽

David R. Thomas ◽

Ceri H. Davies ◽

Jim J. Hagan ◽

Martyn D. Wood ◽

...

Keyword(s):

Human Brain ◽

Brain Tissue ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Human Brain Tissue ◽

Postmortem Human Brain ◽

Protein Coupling ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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Direct SUMOylation of M1 muscarinic acetylcholine receptor increases its ligand‐binding affinity and signal transduction

The FASEB Journal ◽

10.1096/fj.201800936r ◽

2018 ◽

Vol 33 (3) ◽

pp. 3237-3251 ◽

Cited By ~ 3

Author(s):

Jianrong Xu ◽

Panpan Tan ◽

Hui Li ◽

Yongyao Cui ◽

Yu Qiu ◽

...

Keyword(s):

Signal Transduction ◽

Ligand Binding ◽

Binding Affinity ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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The m1 muscarinic acetylcholine receptor transactivates the EGF receptor to modulate ion channel activity

The EMBO Journal ◽

10.1093/emboj/16.15.4597 ◽

1997 ◽

Vol 16 (15) ◽

pp. 4597-4605 ◽

Cited By ~ 144

Author(s):

W. Tsai

Keyword(s):

Ion Channel ◽

Acetylcholine Receptor ◽

Egf Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Channel Activity ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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P2-317: Suvn-i1312004, a novel M1 muscarinic acetylcholine receptor-positive allosteric modulator: Potential for the treatment of Alzheimer's disease

Alzheimer s & Dementia ◽

10.1016/j.jalz.2015.06.859 ◽

2015 ◽

Vol 11 (7S_Part_13) ◽

pp. P615-P616

Author(s):

Renny Abraham ◽

Ramkumar Subramanian ◽

Rajesh Babu Medapati ◽

Ravirala Venkateshwarlu ◽

Sumanth Yathavakilla ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Allosteric Modulator ◽

Positive Allosteric Modulator ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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Activation of m1 muscarinic acetylcholine receptor induces surface transport of KCNQ channels through a CRMP-2-mediated pathway

Journal of Cell Science ◽

10.1242/jcs.175547 ◽

2015 ◽

Vol 128 (22) ◽

pp. 4235-4245 ◽

Cited By ~ 8

Author(s):

L. Jiang ◽

A. Kosenko ◽

C. Yu ◽

L. Huang ◽

X. Li ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Surface Transport ◽

Kcnq Channels ◽

Muscarinic Acetylcholine ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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The M1-muscarinic acetylcholine receptor subtype is linked to the inositide cycle in rat brain synaptosomes

Biochemical Society Transactions ◽

10.1042/bst0141261 ◽

1986 ◽

Vol 14 (6) ◽

pp. 1261-1262

Author(s):

LUCIO A. A. VAN ROOIJEN ◽

WOLFGANG U. DOMPERT ◽

ERVIN HORVÁTH ◽

DAVID G. SPENCER ◽

JÖRG TRABER

Keyword(s):

Rat Brain ◽

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Receptor Subtype ◽

Rat Brain Synaptosomes ◽

Muscarinic Acetylcholine ◽

Brain Synaptosomes ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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Author response for "M1 muscarinic acetylcholine receptor‐mediated inhibition of GABA release from striatal medium spiny neurons onto cholinergic interneurons"

10.1111/ejn.15074/v3/response1 ◽

2020 ◽

Author(s):

Etsuko Suzuki ◽

Toshihiko Momiyama

Keyword(s):

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Gaba Release ◽

Author Response ◽

Medium Spiny Neurons ◽

Muscarinic Acetylcholine ◽

Cholinergic Interneurons ◽

Spiny Neurons ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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Review for "M1 muscarinic acetylcholine receptor‐mediated inhibition of GABA release from striatal medium spiny neurons onto cholinergic interneurons"

10.1111/ejn.15074/v2/review1 ◽

2020 ◽

Author(s):

Giuseppe Sciamanna

Keyword(s):

Acetylcholine Receptor ◽

Muscarinic Acetylcholine Receptor ◽

Gaba Release ◽

Medium Spiny Neurons ◽

Muscarinic Acetylcholine ◽

Cholinergic Interneurons ◽

Spiny Neurons ◽

M1 Muscarinic Acetylcholine Receptor ◽

M1 Muscarinic

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