Results 11 to 20 of about 1,665 (158)

Single-Disulfide Conopeptide Czon1107, an Allosteric Antagonist of the Human α3β4 Nicotinic Acetylcholine Receptor

open access: yesMarine Drugs, 2022
Conopeptides are peptides in the venom of marine cone snails that are used for capturing prey or as a defense against predators. A new cysteine-poor conopeptide, Czon1107, has exhibited non-competitive inhibition with an undefined allosteric mechanism in
Yuan Ma   +9 more
doaj   +2 more sources

The crystal structure of Ac-AChBP in complex with α-conotoxin LvIA reveals the mechanism of its selectivity towards different nAChR subtypes [PDF]

open access: yesProtein & Cell, 2017
The α3* nAChRs, which are considered to be promising drug targets for problems such as pain, addiction, cardiovascular function, cognitive disorders etc., are found throughout the central and peripheral nervous system.
Manyu Xu   +5 more
doaj   +2 more sources

AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. [PDF]

open access: yesBr J Pharmacol, 2015
The α3β4 subtype of nicotinic acetylcholine receptors (nAChRs) has been implicated in mediating nicotine reinforcement processes. AT-1001 has been recently described as a high-affinity and selective α3β4 nAChR antagonist that blocks nicotine self ...
Cippitelli A   +13 more
europepmc   +2 more sources

The α3β4 nAChR partial agonist AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. [PDF]

open access: yesBehav Brain Res, 2017
The strong reinforcing effects of nicotine and the negative symptoms such as anxiety experienced during a quit attempt often lead to relapse and low success rates for smoking cessation.
Yuan M   +5 more
europepmc   +2 more sources

Nicotinic Receptors in the Medial Habenula to Interpeduncular Nucleus Pathway: Modulators of Reward, Aversion and Emotion. [PDF]

open access: yesEur J Neurosci
ABSTRACT The medial habenula–interpeduncular nucleus pathway is a highly conserved and densely innervated brain circuit known for its unique cholinergic transmission and exceptional expression of nicotinic acetylcholine receptors. This pathway plays a critical role in regulating motivational and emotional processes, particularly those related to ...
Ciscato M, Chouvaeff M, Mourot A.
europepmc   +2 more sources

Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior

open access: yes, 2023
Growing evidence suggests that inhibition of the α3β4 nicotinic acetylcholine receptor (nAChR) represents a promising therapeutic strategy to treat cocaine use disorder.
Andrea Cippitelli (194306)   +11 more
core   +3 more sources

Single amino acid substitution in α-conotoxin TxID reveals a specific α3β4 nicotinic acetylcholine receptor antagonist

open access: yes, 2018
The α3β4 nicotinic acetylcholine receptor (nAChR) is an important target implicated in various disease states. α-Conotoxin TxID (1) is the most potent antagonist of α3β4 nAChR, but it also exhibits inhibition of α6/α3β4 nAChR.
Luo, Sulan   +6 more
core   +4 more sources

Nicotinic Acetylcholine Receptor Pathways in Cancer: From Psychiatric Clues to Therapeutic Opportunities. [PDF]

open access: yesCancer Rep (Hoboken)
ABSTRACT Background The prevalence of cancer poses significant challenges to treatment, largely because of drug resistance along with other side effects. Current studies have been investigating the growth factors more than other biologic tumor features, such as neurobiologic features.
Azadi MH   +3 more
europepmc   +2 more sources

Nicotinic Acetylcholine Receptors in the Respiratory Tract

open access: yesMolecules, 2021
Nicotinic acetylcholine receptors (nAChR) are widely distributed in neuronal and non-neuronal tissues, where they play diverse physiological roles. In this review, we highlight the recent findings regarding the role of nAChR in the respiratory tract with
Monika I. Hollenhorst   +1 more
doaj   +1 more source

Basic Residues at Position 11 of α‑Conotoxin LvIA Influence Subtype Selectivity between α3β2 and α3β4 Nicotinic Receptors via an Electrostatic Mechanism

open access: yes, 2023
Understanding the determinants of α-conotoxin (α-CTX) selectivity for different nicotinic acetylcholine receptor (nAChR) subtypes is a prerequisite for the design of tool compounds to study nAChRs.
Guy Kamnesky (2821153)   +12 more
core   +4 more sources

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