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Nicotinic acetylcholine receptor (nAChR) agonists, antagonists and modulators act on ligand-gated cation channels. Each receptor is a pentamer of subunits arranged around a central pore that opens when acetylcholine binds. A refined structure of the Torpedo receptor at 4 Å resolution, published in 2005, resolved its ligand-binding, membrane and cytoplasmic regions. Muscle-type receptors mediate neuromuscular transmission, while neuronal subtypes such as α7 and α4β2 are studied in attention, memory and nicotine dependence. Agonists include PNU 282987, which is selective for α7, and the partial agonist varenicline. PNU-120596, described in 2005, is a positive allosteric modulator of α7 that enhances acetylcholine-evoked currents. Vecuronium bromide, a neuromuscular blocking agent, acts on the muscle-type receptor.
Methyllycaconitine citrate is a potent antagonist for α7-containing neuronal nicotinic receptors (Ki = 1.4 nM). Interacts with α4β2 and α6β2 receptors at concentrations > 40 nM.
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
Synonyms: Novaban; SDZ-ICS 930
Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
Synonyms: Dehydrobenzperidol
Droperidol is a butyrophenone compound primarily acting as a dopamine receptor antagonist. It inhibits the activation of GABA(A) and neuronal nicotinic acetylcholine receptors (nAChR), demonstrating IC50 values of 12.6 nM and 5.8 μM, respectively. This compound exhibits notable anesthetic and sedative properties, making it useful in research related to neuropharmacology and anesthesiology.
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity.
Synonyms: Inversine; Mecamine hydrochloride Mecamylamine HCl; Mevasin
Mecamylamine hydrochloride is a nAChR antagonist previously used to treat hypertension. It displays a wide variety of activities, including reducing depression-like behaviors in subjects with Tourette's syndrome and improving rates of smoking cessation.
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
Mecamylamine is a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). It functions as a ganglionic blocker and is capable of crossing the blood-brain barrier. Mecamylamine is utilized in research focused on neuropsychiatric disorders, hypertension, and the development of antidepressant therapies.
Synonyms: PF-00520904
Derquantel is a spirocyclic anthelmintic that functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs). It inhibits acetylcholine-induced depolarization with an IC50 of 0.22 μM, leading to flaccid paralysis of nematode somatic muscles. This mechanism effectively dislodges parasites from the host gastrointestinal tract, making Derquantel a valuable tool in research related to Haemonchus contortus and Ascaris suum infections.
GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels.
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Waglerin-1 is a 22-amino acid peptide that acts as a competitive antagonist of the muscle nicotinic acetylcholine receptor (nAChR). It effectively inhibits nAChR-mediated signaling, making it a valuable tool for studying neuromuscular transmission and muscle physiology. This peptide is utilized in various research applications, including the investigation of synaptic mechanisms and the development of therapeutic strategies for neuromuscular disorders.
Synonyms: DHβE hydrobromide
Dihydro-β-erythroidine hydrobromide is a competitive antagonist specifically targeting neuronal nicotinic acetylcholine receptors (nAChRs). It demonstrates notable selectivity for the α4β4 and α4β2 nAChR subtypes, with IC50 values of 0.19 μM and 0.37 μM, respectively. This compound is utilized in research exploring its potential antidepressant-like effects and its role in understanding nAChR-mediated signaling pathways.
Coclaurine is a tetrahydroisoquinoline alkaloid and a potent antagonist of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticancer activity by downregulating EFHD2-related NOX4-ABCC1 signaling, thereby enhancing the sensitivity of cancer cells to Cisplatin. Coclaurine also suppresses the stemness and metastatic potentials of non-small cell lung cancer (NSCLC) cells through the disruption of the FOXG1-EFHD2 promoter interaction, leading to reduced EFHD2 transcription. This compound serves as a valuable tool for research focused on cancer therapy and the modulation of nAChR signaling.
AT 1001 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), with a high affinity characterized by a Ki value of 2.64 nM. This compound effectively reverses inward currents triggered by Epibatidine in HEK cells expressing α3β4 nAChR. AT 1001 demonstrates dose-dependent inhibition of nicotine self-administration in rat models, while sparing food-reinforced responding, making it a valuable tool in nicotine addiction and smoking cessation therapy research.
Chlorisondamine diiodide is a potent antagonist of the nicotinic acetylcholine receptor (nAChR), functioning as a ganglion blocker. It effectively inhibits specific central actions of nicotine with notable potency and pharmacological selectivity. This compound is valuable in research applications exploring neural signaling, autonomic regulation, and addiction pathways.
Synonyms: (2S,6S)-HNK hydrochloride
(2S,6S)-Hydroxynorketamine hydrochloride is an antagonist of the α7-nicotinic acetylcholine receptor (nAChR). It exhibits potential neurorelaxant, antidepressant, and analgesic effects, facilitating the activation of the mTOR pathway and promoting increased phosphorylation of downstream targets. This compound is of particular interest in neurological research, particularly in the exploration of therapeutic avenues for mood disorders and pain management.
CVN417 is an orally active antagonist of the α6 subunit-containing nicotinic acetylcholine receptors (nAChRs). This inhibitor modulates phasic dopaminergic neurotransmission in an impulse-dependent manner and exhibits inhibitory effects on Ca(2+) efflux through various nAChR subunits, with IC50 values of 0.086 μM for α6, 2.56 μM for α3, and 0.657 μM for α4. CVN417 has demonstrated efficacy in reducing resting tremors in rodent models and may offer therapeutic potential for improving movement dysfunction associated with Parkinson's disease.
Pentapeptide-3 is a pentapeptide derived from the neurotoxin waglerin-1, sourced from Temple Viper venom. It functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), effectively blocking nerve transmission at the post-synaptic membrane. Due to its ability to inhibit nAChRs, Pentapeptide-3 exhibits potential anti-aging effects and is often utilized in conjunction with other cosmetic peptides for research applications related to skin rejuvenation.
SUVN-911 is a select, potent antagonist of the neuronal nicotinic acetylcholine α4β2 receptor, demonstrating a Ki of 1.5 nM and capable of effective brain penetration. This compound shows promising antidepressant activity and is valuable for research applications targeting mood disorders and neuropharmacology. Its oral bioavailability further enhances its utility in preclinical studies.
Synonyms: (-)-(S)-Coclaurine hydrochloride; L-Coclaurine hydrochloride; l-Coclaurine
(-)-Coclaurine hydrochloride is a tetrahydroisoquinoline alkaloid that functions as a nicotinic acetylcholine receptor (nAChR) antagonist. This compound exhibits significant biological activity in modulating nAChR-related pathways, making it valuable for research into neuropharmacology and the development of therapeutic strategies for conditions involving cholinergic signaling. Its potential applications include studies on cognitive function, addiction, and various neurological disorders.
Flupyrimin is a potent antagonist of the insect nicotinic acetylcholine receptor (nAChR), exerting insecticidal activity by disrupting normal neural signaling in insects. This compound is utilized in research focused on understanding insect physiology and the mechanisms of action of insecticides. Flupyrimin's ability to inhibit nAChR function makes it a valuable tool for studying insect neurobiology and developing targeted pest control strategies.
(S)-UFR2709 hydrochloride is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with a higher affinity for the α4β2 subtype compared to the α7 subtype. This compound has demonstrated anxiolytic properties, effectively reducing anxiety levels and decreasing both ethanol consumption and preference in alcohol-preferring rat models. (S)-UFR2709 hydrochloride serves as a valuable tool for research into nicotine addiction and related neuropharmacological studies.
Synonyms: Stilonium iodide
MG624 is a potent and selective antagonist of the neuronal α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 106 nM. This compound primarily inhibits α7 nAChR-mediated signaling, making it a valuable tool for research investigating cholinergic neurotransmission and related neurological disorders. MG624 can be utilized in studies exploring the role of α7 nAChR in synaptic plasticity, cognitive function, and neurodegenerative disease mechanisms.
bPiDDB is a potent antagonist of nicotinic acetylcholine receptors (nAChRs), specifically targeting α6β2-containing subtypes. It demonstrates significant inhibitory activity on nicotine-induced striatal dopamine release, with an IC50 value of 2 nM. This compound is valuable for research focused on nAChR-mediated signaling pathways and the role of dopamine in neurological studies.
