Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

被引：18

作者：

Manetti, Dina ^{[1
]}

Dei, Silvia ^{[1
]}

Arias, Hugo R. ^{[2
]}

Braconi, Laura ^{[1
]}

Gabellini, Alessio ^{[1
]}

Teodori, Elisabetta ^{[1
]}

Romanelli, Maria Novella ^{[1
]}

机构：

[1] Univ Florence, NEUROFARBA Dept, Sect Pharmaceut & Nutraceut Sci, I-50019 Florence, Italy

[2] Oklahoma State Univ, Coll Osteopath Med, Dept Pharmacol & Physiol, Tahlequah, OK 74464 USA

来源：

MOLECULES | 2023年 / 28卷 / 03期

关键词：

positive allosteric modulator; negative allosteric modulator; desensitization; alpha; 7; 4; beta; 2; nicotinic acetylcholine receptor; BINDING-SITES; PHARMACOLOGICAL CHARACTERIZATION; ALTERNATE STOICHIOMETRIES; MECAMYLAMINE ENANTIOMERS; SUBUNIT INTERFACES; IN-VITRO; ALPHA-7; ALPHA-4-BETA-2; ACTIVATION; POTENTIATION;

D O I：

10.3390/molecules28031270

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric modulatory sites distinct from the orthosteric sites. This survey is focused on the compounds that have been shown or have been designed to interact with nicotinic receptors as allosteric modulators of different subtypes, mainly alpha 7 and alpha 4 beta 2. Minimal chemical changes can cause a different pharmacological profile, which can then lead to the design of selective modulators. Experimental evidence supports the use of allosteric modulators as therapeutic tools for neurological and non-neurological conditions.

引用

收藏

页数：24

相关论文

共 132 条

[21] Nicotine addiction: the possible role of functional upregulation [J].

Buisson, B ;

Bertrand, D .

TRENDS IN PHARMACOLOGICAL SCIENCES, 2002, 23 (03) :130-136

[22] Evidence for Alpha7 Nicotinic Receptor Activation During the Cough Suppressing Effects Induced by Nicotine and Identification of ATA-101 as a Potential Novel Therapy for the Treatment of Chronic Cough [J].

Canning, Brendan J. ;

Liu, Qi ;

Tao, Mayuko ;

DeVita, Robert ;

Perelman, Michael ;

Hay, Douglas W. ;

Dicpinigaitis, Peter, V ;

Liang, Jing .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2022, 380 (02) :94-103

[23] The nicotinic acetylcholine receptor and its prokaryotic homologues: Structure, conformational transitions & allosteric modulation [J].

Cecchini, Marco ;

Changeux, Jean-Pierre .

NEUROPHARMACOLOGY, 2015, 96 :137-149

[24] α7 neuronal nicotinic acetylcholine receptors are negatively regulated by tyrosine phosphorylation and Src-family kinases [J].

Charpantier, E ;

Wiesner, A ;

Huh, KH ;

Ogier, R ;

Hoda, JC ;

Allaman, G ;

Raggenbass, M ;

Feuerbach, D ;

Bertrand, D ;

Fuhrer, C .

JOURNAL OF NEUROSCIENCE, 2005, 25 (43) :9836-9849

[25] Allosteric modulation of nicotinic acetylcholine receptors [J].

Chatzidaki, Anna ;

Millar, Neil S. .

BIOCHEMICAL PHARMACOLOGY, 2015, 97 (04) :408-417

[26] The influence of allosteric modulators and transmembrane mutations on desensitisation and activation of α7 nicotinic acetylcholine receptors [J].

Chatzidaki, Anna ;

D'Oyley, Jarryl M. ;

Gill-Thind, JasKiran K. ;

Sheppard, Tom D. ;

Millar, Neil S. .

NEUROPHARMACOLOGY, 2015, 97 :75-85

[27] Repeated administration of α7 nicotinic acetylcholine receptor (nAChR) agonists, but not positive allosteric modulators, increases α7 nAChR levels in the brain [J].

Christensen, Ditte Z. ;

Mikkelsen, Jens D. ;

Hansen, Henrik H. ;

Thomsen, Morten S. .

JOURNAL OF NEUROCHEMISTRY, 2010, 114 (04) :1205-1216

[28] REGIONS OF BETA-2 AND BETA-4 RESPONSIBLE FOR DIFFERENCES BETWEEN THE STEADY-STATE DOSE-RESPONSE RELATIONSHIPS OF THE ALPHA-3-BETA-2 AND ALPHA-3-BETA-4 NEURONAL NICOTINIC RECEPTORS [J].

COHEN, BN ;

FIGL, A ;

QUICK, MW ;

LABARCA, C ;

DAVIDSON, N ;

LESTER, HA .

JOURNAL OF GENERAL PHYSIOLOGY, 1995, 105 (06) :745-764

[29] Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders [J].

Conn, P. Jeffrey ;

Christopoulos, Arthur ;

Lindsley, Craig W. .

NATURE REVIEWS DRUG DISCOVERY, 2009, 8 (01) :41-54

[30] 1,3-diphenylpropan-1-ones as allosteric modulators of α7 nACh receptors with analgesic and antioxidant properties [J].

Criado, Manuel ;

Balsera, Beatriz ;

Mulet, Jose ;

Sala, Salvador ;

Sala, Francisco ;

de la Torre-Martinez, Roberto ;

Fernandez-Carvajal, Asia ;

Ferrer-Montiel, Antonio ;

Moreno-Fernandez, Silvia ;

Miguel, Marta ;

Perez de Vega, Maria Jesus ;

Gonzalez-Muniz, Rosario .

FUTURE MEDICINAL CHEMISTRY, 2016, 8 (07) :731-749

← 1 2 3 4 5 6 7 8 9 10 →