Effect of nicotine and alpha‐7 nicotinic modulators on visceral pain‐induced conditioned place aversion in mice

Bağdaş, Deniz; Meade, Julie A.; Alkhlaif, Yasmin; Muldoon, Pretal P.; Carroll, F. Ivy; Damaj, M. Imad

doi:10.1002/ejp.1231

Cited by 12 publications

(4 citation statements)

References 56 publications

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“…LL-00066471, JWX-A0108 (Sun et al, 2019), andJNJ-1930942 (Dinklo et al, 2011) improved acoustic startle reflex or genetic defects believed to be associated with hippocampal auditory gating. PAM2 (Arias et al, 2020), 1-(2',5 0 -dihydroxyphenyl)-3-(2-fluoro-4-hydroxyphenyl)-1-propanone (Perez de Vega et al, 2019), TQS (Abbas et al, 2017), and PNU-120596 (Bagdas et al, 2018b) were effective in models of inflammatory or neuropathic pain. Some PAMs are advancing toward Fig.…”

Section: A7-positive Allosteric Modulatorsmentioning

confidence: 99%

Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors

Papke

Horenstein

2021

Pharmacol Rev

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Section: A7-positive Allosteric Modulatorsmentioning

confidence: 99%

Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors

Papke

Horenstein

2021

Pharmacol Rev

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“…α9 nAChRs, located on DRG neurons, have been shown to play a role in chronic pain perception in several models of neuropathic pain and after a traumatic nerve injury [178,179]. In addition, accumulating evidence suggests that agonists and modulators of α7 nAChRs may be promising in the treatment of pain conditions, including visceral pain [180,181]. However, despite these efforts, no nAChR modulator has yet been approved as an analgesic, principally owing to safety concerns around possible cardiovascular and gastrointestinal side effects [182].…”

Section: Chronic Abdominal Visceral Pain: Focus On Marine Toxins Amentioning

confidence: 99%

Marine Toxins and Nociception: Potential Therapeutic Use in the Treatment of Visceral Pain Associated with Gastrointestinal Disorders

Baj

Bistoletti

Bosi

et al. 2019

Toxins

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Visceral pain, of which the pathogenic basis is currently largely unknown, is a hallmark symptom of both functional disorders, such as irritable bowel syndrome, and inflammatory bowel disease. Intrinsic sensory neurons in the enteric nervous system and afferent sensory neurons of the dorsal root ganglia, connecting with the central nervous system, represent the primary neuronal pathways transducing gut visceral pain. Current pharmacological therapies have several limitations, owing to their partial efficacy and the generation of severe adverse effects. Numerous cellular targets of visceral nociception have been recognized, including, among others, channels (i.e., voltage-gated sodium channels, VGSCs, voltage-gated calcium channels, VGCCs, Transient Receptor Potential, TRP, and Acid-sensing ion channels, ASICs) and neurotransmitter pathways (i.e., GABAergic pathways), which represent attractive targets for the discovery of novel drugs. Natural biologically active compounds, such as marine toxins, able to bind with high affinity and selectivity to different visceral pain molecular mediators, may represent a useful tool (1) to improve our knowledge of the physiological and pathological relevance of each nociceptive target, and (2) to discover therapeutically valuable molecules. In this review we report the most recent literature describing the effects of marine toxin on gastrointestinal visceral pain pathways and the possible clinical implications in the treatment of chronic pain associated with gut diseases.

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“…α7 nAChRs are activated by various types of ligands including natural small molecules such as choline and nicotine, as well as synthetic compounds such as PNU-282987. − α7 nAChRs are also activated by peptides of varying sequence lengths and structural conformations. For example, proteins exhibiting a three-finger toxin (3ftx) receptor-targeting fold are shown to bind tightly to nAChRs including α7 homopentamers. , Such proteins include protoxins, such as lynx1, and neurotoxins, such as α-conotoxin ImI and α-bungarotoxin (Bgtx). , A 3ftx-fold has also been suggested within some human disease-causing proteins including the SARS-CoV2 spike glycoprotein …”

Section: Introductionmentioning

confidence: 99%

Protein Painting Mass Spectrometry in the Discovery of Interaction Sites within the Acetylcholine Binding Protein

Graur,

Haymond,

Lee

et al. 2024

ACS Chem. Neurosci.

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Nicotinic acetylcholine receptors (nAChRs) are a family of ligand-gated ion channel receptors that contribute to cognition, memory, and motor control in many organisms. The pharmacological targeting of these receptors, using small molecules or peptides, presents an important strategy for the development of drugs that can treat important human diseases, including neurodegenerative disorders. The Aplysia californica acetylcholine binding protein (Ac-AChBP) is a structural surrogate of the nAChR with high homology to the extracellular ligand binding domain of homopentameric nAChRs. In this study, we optimized protein-painting-based mass spectrometry to identify regions of interaction between the Ac-AChBP and several nAChR ligands. Using molecular dyes that adhere to the surface of a solubilized Ac-AChBP complex, we identified amino acid residues that constitute a contact site within the Ac-AChBP for α-bungarotoxin, choline, nicotine, and amyloid-β 1−42. By integrating innovation in protein painting mass spectrometry with computational structural modeling, we present a new experimental tool for analyzing protein interactions of the nAChR.

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Effect of nicotine and alpha‐7 nicotinic modulators on visceral pain‐induced conditioned place aversion in mice

Abstract: The present results suggest that allosteric modulation of α7 nAChR may provide new strategies in affective aspects of nociception.

Cited by 12 publications

References 56 publications

Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors

Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors

Marine Toxins and Nociception: Potential Therapeutic Use in the Treatment of Visceral Pain Associated with Gastrointestinal Disorders

Protein Painting Mass Spectrometry in the Discovery of Interaction Sites within the Acetylcholine Binding Protein

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