Neuronal Signaling

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  1. mAChR Inhibitor

    Camylofine is an antimuscarinic compound that selectively inhibits muscarinic acetylcholine receptors (mAChRs). It functions as a smooth muscle relaxant, making it useful in various research applications related to muscle contraction and neurotransmission. This compound is valuable for studying the physiological effects of cholinergic signaling and exploring potential therapeutic interventions for conditions related to smooth muscle hyperactivity.
  2. mAChR Antagonist

    Propantheline bromide is a selective antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits notable effects in the management of smooth muscle dysfunction, including conditions such as excessive sweating, abdominal cramps, and involuntary urination. With limited ability to cross the blood-brain barrier, propantheline bromide is valuable in studies that require peripheral mAChR modulation without central nervous system effects.
  3. Antispastic Agent, Muscle Relaxant, P2X7 Receptor Antagonist

    Eperisone hydrochloride primarily acts as a P2X7 receptor antagonist and is recognized for its antispastic and muscle relaxant properties. This compound is effective in alleviating muscle stiffness and pain, showcasing vasodilatory effects. In addition to its action on skeletal muscles, Eperisone hydrochloride also exhibits antagonistic effects on human P2X3 receptors, contributing to improved circulation and the suppression of myotonia-related pain reflexes, making it valuable for muscle-related research applications.
  4. GABAA Receptor Antagonist

    Thiocolchicoside is a competitive antagonist of the γ-aminobutyric acid type A (GABAA) receptor, and acts as a glycine receptor agonist within the central nervous system. This semisynthetic sulfur derivative of colchicoside exhibits muscle relaxant properties, along with significant anti-inflammatory and analgesic effects. Thiocolchicoside is valuable in research for its potential applications in studying neuromuscular relaxation and pain management.
  5. AChE Inhibitor

    Acotiamide is a selective and reversible inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 1.79 μM. It has demonstrated the ability to enhance gastric contractility and promote accelerated gastric emptying. This compound is valuable for investigating functional dyspepsia related to gastric motility dysfunction and intestinal inflammation.
  6. COX-1/COX-2 Inhibitor

    6-Methoxy-2-naphthoic acid is a potent inhibitor of COX-1 and COX-2 enzymes. It effectively inhibits the synthesis of gastric mucosal prostaglandin E2, making it relevant in studies related to inflammation and pain-related conditions. Additionally, 6-Methoxy-2-naphthoic acid serves as an impurity in Naproxen and can be utilized in the synthesis of various active compounds, contributing to diverse research applications in pharmaceutical development.
  7. COX-2 Inhibitor

    Parecoxib Sodium is a selective COX-2 inhibitor that effectively penetrates the blood-brain barrier and serves as a proagent for Valdecoxib. This nonsteroidal anti-inflammatory drug (NSAID) inhibits prostaglandin synthesis, making it suitable for the relief of acute postoperative pain as well as for managing symptoms associated with chronic inflammatory conditions, including osteoarthritis and rheumatoid arthritis. It has important applications in both clinical and preclinical research focused on pain management and inflammation.
  8. mAChR Antagonist

    Atropine sulfate is a competitive antagonist of the muscarinic acetylcholine receptors (mAChR), exhibiting IC50 values of 0.39 nM for human mAChR M4 and 0.71 nM for chicken mAChR M4. This compound effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. Atropine sulfate is utilized in research related to anti-myopia and the management of bradycardia.
  9. NMDA Receptor Antagonist

    Orphenadrine hydrochloride is a non-competitive antagonist of the NMDA receptor, effectively crossing the blood-brain barrier with a Ki of 6.0 μM. This compound demonstrates significant biological activity in alleviating stiffness, pain, and discomfort related to muscle strains, sprains, and injuries. Additionally, it serves as an adjunct therapy for tremors in Parkinson’s disease and exhibits neuroprotective properties, making it valuable in research on neurodegenerative disorders.
  10. Neuromuscular Blocking Agent

    Mivacurium dichloride is a short-acting non-depolarizing neuromuscular blocking agent that acts as a skeletal muscle relaxant. It exerts its pharmacological effects by binding to the nicotinic acetylcholine receptor (nAChR), thereby inhibiting the depolarizing action of acetylcholine at the neuromuscular junction. This compound is utilized in clinical settings for facilitating intubation and providing muscle relaxation during surgical procedures.
  11. mAChR Antagonist

    Racanisodamine is a non-selective muscarinic antagonist that modulates the activity of muscarinic acetylcholine receptors (mAChR). It exhibits pharmacological effects similar to its parent compound, anisodamine, and is primarily utilized in formulations for myopic control in ophthalmic applications. This compound is valuable for research into the mechanisms of muscarinic receptor modulation and its implications in vision science.
  12. AChEI Inhibitor, XO Inhibitor, Thromboxane Inhibitor

    Imidazole acts as an inhibitor of acetylcholinesterase (AChEI), xanthine oxidase (XO), and thromboxane. This heterocyclic aromatic compound exhibits significant biological activities, including antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic properties. By inhibiting the conversion of endoperoxides (PGG2 and PGH2) to thromboxane A2, Imidazole plays a role in cardiovascular research. Additionally, its derivatives have shown potential in inhibiting the SARS-CoV-2 3CLPro enzyme, making it a valuable candidate for studies related to Alzheimer's disease, gout, COVID-19, and thrombo-embolic conditions.
  13. nAChR Inhibitor

    (+)-Sparteine is a natural alkaloid that functions as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). By blocking these receptors in neurons, it serves as a ganglionic blocking agent, impacting neurotransmission. This compound is utilized in research applications related to neurotransmitter signaling and the study of ganglionic transmission.
  14. Cholinesterase (ChE) Inhibitor

    Demecarium Bromide is a potent cholinesterase (ChE) inhibitor, exhibiting an apparent affinity (Kiapp) of 0.15 μM. It primarily functions by inhibiting the enzyme cholinesterase, thereby increasing acetylcholine levels. This compound is widely utilized in research related to glaucoma treatment and the study of acetylcholine metabolism, providing valuable insights into neurodegenerative diseases and neurotransmission pathways.
  15. Antidepressant Agent

    Protriptyline hydrochloride is a potent tricyclic antidepressant with a primary mechanism of action involving the inhibition of acetylcholinesterase (AChE), with an IC50 of 0.06 mM, as well as the reduction of amyloid beta (Aβ) self-assembly. This compound exhibits significant antidepressant activity and is valuable for research related to depression and Alzheimer's disease. It serves as a useful reagent for studying neurochemical pathways implicated in mood disorders and neurodegenerative conditions.
  16. COX Inhibitor

    Tolmetin sodium dihydrate is a potent non-steroidal anti-inflammatory drug (NSAID) that primarily targets cyclooxygenase (COX) enzymes, exhibiting IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. This compound is commonly utilized in research related to inflammation and pain modulation. Its ability to effectively inhibit COX activity makes it valuable for studying various inflammatory pathways and developing new therapeutic strategies in pain management.
  17. mAChR Inhibitor

    Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions.
  18. P2Y2 Receptor Agonist

    Diquafosol tetrasodium is a potent P2Y2 receptor agonist. It enhances fluid and mucin secretion on the ocular surface, making it an effective topical therapeutic option for the management of dry eye disease. This compound is valuable for research applications focused on ocular health and pharmacological interventions for dry eye conditions.
  19. Acetylcholinesterase Inhibitor

    Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, primarily targeting the peripheral nervous system. This compound enhances cholinergic transmission by preventing the breakdown of acetylcholine, resulting in increased neurotransmitter levels at the neuromuscular junction. It is widely used in research applications related to neuromuscular disorders and pharmacological studies of cholinergic function.
  20. Muscarinic Receptor Antagonist

    Solifenacin hydrochloride is a muscarinic receptor antagonist that selectively inhibits the activity of M1, M2, and M3 muscarinic receptors, displaying pKis of 7.6, 6.9, and 8.0, respectively. This compound is primarily utilized in research to study the modulation of cholinergic signaling and its implications in urological conditions. Its antagonistic properties make it a valuable tool for investigating the pharmacology of bladder overactivity and other related disorders.
  21. Monoamine Oxidase Inhibitor

    Minaprine dihydrochloride is a selective monoamine oxidase inhibitor that penetrates the blood-brain barrier. It exhibits biological activity by reducing intraneuronal dopamine metabolism, lowering levels of striatal homovanillic acid and dihydroxyphenylacetic acid, while increasing levels of 3-methoxytyramine and 5-hydroxytryptamine in the striatum. Additionally, Minaprine dihydrochloride weakly inhibits acetylcholinesterase activity and displays both convulsant and antidepressant properties, making it a valuable reagent for research in neuropharmacology and mood disorder studies.
  22. Amyloid-β Inhibitor

    Dihydroergocristine mesylate is a potent inhibitor of γ-secretase, targeting the enzyme responsible for the generation of amyloid-β peptides implicated in Alzheimer’s disease. It effectively reduces the production of these peptides by binding directly to γ-secretase and Nicastrin, exhibiting equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively. This compound can be utilized in research aimed at unraveling the mechanisms of Alzheimer’s pathology and developing potential therapeutic strategies.
  23. Anticholinergic Agent

    Pridinol mesylate is an anticholinergic agent that targets muscarinic acetylcholine receptors (mAChRs) to provide muscle relaxation. It effectively reduces impulse conduction to spinal motor neurons, exhibiting significant muscle relaxant properties. Pridinol mesylate is useful in research related to musculoskeletal diseases, particularly for investigating skeletal muscle contractures arising from both central and peripheral origins. Its blood-brain permeability facilitates its application in studies involving central nervous system effects.
  24. mAChR Inhibitor

    Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling.
  25. AChE Inhibitor

    Ambenonium chloride is a potent, reversible inhibitor of acetylcholinesterase (AChE), demonstrating a high affinity for the enzyme. With an IC50 value of 0.7 nM for human AChE, this compound effectively enhances cholinergic transmission. It is primarily utilized in research applications focused on neurological disorders, particularly those involving impaired cholinergic function.
  26. mAChR Antagonist

    Homatropine is a muscarinic acetylcholine receptor (mAChR) antagonist with significant anticholinergic properties. This compound exhibits capacity to modulate activities mediated by the mAChR pathway, making it useful in various pharmacological studies. Homatropine is commonly employed in research applications focused on neurology and pharmacology to investigate cholinergic signaling and its implications for therapeutic approaches.
  27. Organophosphorus (OP) Pesticide

    Dichlofenthion is an organophosphorus (OP) pesticide that functions by inhibiting acetylcholinesterase, leading to the accumulation of acetylcholine at nerve synapses. This mechanism results in heightened nerve signal transmission, making it effective in pest control. Dichlofenthion is primarily utilized for managing sheep maggot fly populations, contributing to agricultural pest management strategies.
  28. Pesticide

    Pyrolan is a carbamate ester pesticide that acts by inhibiting acetylcholinesterase, leading to an accumulation of acetylcholine in synapses. This mechanism results in heightened neurotransmission, which ultimately disrupts normal physiological processes in target pests. Pyrolan is primarily utilized in agricultural settings for pest control in various crops, contributing to effective management of pest populations. Its use supports research into pesticide efficacy and resistance mechanisms within target species.
  29. mAChR Agonist

    Muscarine is a selective agonist of muscarinic acetylcholine receptors (mAChRs), predominantly affecting the parasympathetic nervous system. This compound is recognized for its ability to stimulate various biological responses such as increased glandular secretions and smooth muscle contraction. Muscarine is utilized in research applications to investigate cholinergic signaling pathways and the physiological effects of parasympathetic activation.
  30. COX Inhibitor

    Hamaudol is a chromone derived from Saposhnikovia divaricata, acting as a potent inhibitor of cyclooxygenase (COX)-1 and COX-2, with IC50 values of 0.30 mM and 0.57 mM, respectively. This compound exhibits significant analgesic and anti-inflammatory properties, making it a valuable tool in research focused on pain relief and inflammation modulation. Hamaudol is suitable for investigations into COX inhibition and related biological pathways.
  31. 5-HT Receptor Agonist

    Serotonin is a monoamine neurotransmitter that acts as an endogenous agonist at 5-HT receptors. It plays a critical role in various physiological processes, including mood regulation and cognitive function. Additionally, serotonin functions as a catechol O-methyltransferase (COMT) inhibitor, exhibiting a Ki value of 44 μM. This compound is essential for studies related to neuroscience, pharmacology, and the understanding of mood disorders.
  32. Antidepressant

    Depramine, a tricyclic antidepressant, primarily targets neurotransmitter reuptake mechanisms, elevating levels of norepinephrine and serotonin in the synaptic cleft. It exhibits significant biological activity through the inhibition of acetylcholinesterase, Mg2+-ATPase, and Na+/K+ ATPase. Depramine is utilized in research focused on depression and related mood disorders, facilitating studies on neurotransmitter dynamics and cellular signaling pathways involved in antidepressant efficacy.
  33. AChE Inhibitor

    1,1'-Bi-2-naphthol is a potent acetylcholinesterase (AChE) inhibitor, demonstrating an IC50 value of 21.9 μM against human AChE. This compound also exhibits cytotoxic effects on Artemia nauplii, making it valuable for studies in neuropharmacology and toxicology. Its dual functionality positions it as a useful reagent in researching cholinergic signaling and the potential effects of AChE inhibition.
  34. Cholinesterase (ChE) Inhibitor

    Physostigmine, a reversible acetylcholinesterase (AChE) inhibitor, effectively increases acetylcholine levels in the central nervous system by crossing the blood-brain barrier. This compound enhances cholinergic neurotransmission and has been shown to reverse memory deficits in transgenic mice models of Alzheimer's disease. Additionally, Physostigmine serves as a critical antidote for anticholinergic poisoning, providing valuable insights for neuropharmacological research and therapeutic applications.
  35. Fenthion Metabolite

    Fenthoxon is a metabolite of fenthion, an organophosphate insecticide that primarily acts by inhibiting acetylcholinesterase activity. This inhibition leads to the accumulation of acetylcholine at synapses, resulting in neurotoxic effects on insect populations. Fenthoxon is utilized in research to study the environmental impact and metabolic pathways of organophosphate compounds, as well as their neurotoxic mechanisms in various biological systems.
  36. Insecticide

    Phorate sulfone, a metabolite of phorate, primarily targets acetylcholinesterase, exhibiting inhibitory activity with an IC50 of 40 μM. This results in the accumulation of acetylcholine at both cellular and subcellular levels. Phorate sulfone is valuable for researching the mechanisms and effects associated with severe phorate poisoning.
  37. Fenthion Insecticide

    Fenthion sulfoxide is a metabolite of the organophosphate insecticide Fenthion, primarily involved in the inhibition of acetylcholinesterase activity. This compound is relevant in studies investigating pesticide metabolism and environmental impacts, particularly concerning its formation on agricultural products such as grapes. Research applications include toxicology assessments and investigations into the persistence and degradation of organophosphate residues in the environment.
  38. Disulfoton Metabolite

    Disulfoton sulfone is a metabolic byproduct of the organophosphorus pesticide Disulfoton, primarily targeting acetylcholinesterase. This compound exhibits significant biological activity as an inhibitor of cholinesterase, which can lead to increased levels of acetylcholine at synapses. Researchers utilize Disulfoton sulfone in studies focused on neurotoxicity, pesticide metabolism, and mechanisms of organophosphate toxicity, contributing to our understanding of their effects on human health and the environment.
  39. Central Cholinoreceptor Modulator

    Eucatropine hydrochloride is a potent inhibitor of muscarinic acetylcholine receptors (mAChRs), exhibiting an IC50 value of 0.583 μM. As an anticholinergic agent, it modifies cholinergic signaling, leading to significant behavioral effects. This compound is particularly relevant for research applications focused on central cholinoreceptor modulation and its effects on physiological and behavioral outcomes in animal models.
  40. nAChRs Resensitizer

    MB327 is a bipyridine nonoxime compound that functions as a resensitizer of nicotinic acetylcholine receptors (nAChRs). It effectively restores neuromuscular function by reversing carbachol-induced desensitization in a typical type II positive allosteric modulatory manner. Additionally, MB327 has potential applications in neutralizing nerve agent poisoning, making it valuable for research in neuropharmacology and toxicology.
  41. ChE Inhibitor

    Flavonol is a cholinesterase (ChE) inhibitor, demonstrating an IC50 of 120 μM and a Ki value of 74 μM. This compound exhibits notable antioxidant, free radical-scavenging, and antibacterial activities, while also modulating immune responses. Flavonol effectively inhibits the PriA helicase in Staphylococcus aureus and reduces nitric oxide (NO) production in LPS-activated RAW 264.7 cells by downregulating iNOS expression. Its protective and analgesic effects in murine models suggest potential applications in research focused on tumors and atherosclerosis.
  42. mAChR Agonist

    Muscarine chloride is a potent agonist of muscarinic acetylcholine receptors (mAChRs). As a biologically active compound, it simulates the parasympathetic nervous system, making it a valuable tool in neuropharmacological research. Muscarine chloride is utilized in studies examining neurotransmission, receptor signaling pathways, and the effects of cholinergic modulation in various biological systems.
  43. nAChR Inhibitor

    Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 1.9 μM for α1, 1.8 μM for α3β4, 3.7 μM for α4β2, and 6.3 μM for α4β4. This compound demonstrates significant anticonvulsant properties, making it valuable for studies related to seizure disorders and neuropharmacology. Its selective action on various nAChR subtypes positions Adiphenine as a useful tool for exploring the role of these receptors in different biological contexts.
  44. Drug Derivative

    Bornyval is a chemical derivative of valerian, primarily targeting the modulation of GABA receptors. It exhibits sedative and anxiolytic properties, making it valuable for research applications focused on neuropharmacology and the study of sleep disorders. Bornyval can facilitate the investigation of potential therapeutic strategies for anxiety and related conditions.
  45. COX Inhibitor

    Methylhydroquinone is a potent COX inhibitor with noted activity against ovine COX-1 and human recombinant COX-2, exhibiting IC50 values of 480.7 μM and 52.2 μM, respectively. This compound demonstrates anti-inflammatory properties primarily through the inhibition of prostaglandin synthesis. Additionally, it has been associated with potential DNA-damaging effects, including the induction of DNA single-strand breaks. Methylhydroquinone functions by competitively binding to the active sites of COX-1, engaging in non-covalent interactions to exert its biological activities.
  46. Acetylated Alkaloid

    O-Acetylgalanthamine is an acetylated alkaloid derived from the natural source Narcissus pseudonarcissus. This compound is known for its potential to inhibit acetylcholinesterase, thereby enhancing cholinergic neurotransmission. Its biological activity makes O-Acetylgalanthamine valuable in neuroscience research, particularly in studies related to Alzheimer's disease and other cognitive disorders.
  47. Fenothiocarb is a carbamate insecticide that functions as a potent acetylcholinesterase inhibitor. It exhibits biological activity by disrupting the normal function of the nervous system in target insects, leading to paralysis and death. This compound is primarily utilized in research focused on pesticide residue analysis and environmental monitoring of agrochemicals. Its role in studying the impact of pesticide exposure on ecosystems and non-target organisms makes it a valuable tool in toxicological assessments.
  48. AChE Inhibitor

    Buphanidrine is an acetylcholinesterase (AChE) inhibitor with an IC50 of 52.8 μM. This compound, isolated from Brunsvigia josephinae, demonstrates significant potential in the study of neurodegenerative diseases, particularly Alzheimer's disease. Its ability to modulate cholinergic signaling makes it a valuable tool for understanding the pathophysiology of cognitive decline and exploring therapeutic strategies.
  49. Anticonvulsant Agent

    CHF-2993 is an orally active anticonvulsant agent that functions primarily through the antagonism of GABA receptor modulators, specifically Bicuculline and Picrotoxin, to inhibit tonic convulsions in murine models. It shows no effect on Pentylenetetrazole-induced clonic convulsions but partially decreases Veratridine-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 serves as a valuable tool in the investigation of epilepsy and related neurological disorders.
  50. Caffeic Acid Ester Compound

    3-Methyl-3-butenyl (E)-Caffeate is a caffeic acid ester compound known for its antioxidant and anticholinesterase activities. This compound, derived from Algerian propolis, can be utilized in research aimed at understanding its potential neuroprotective properties and its role in combating oxidative stress. Its diverse biological activities make it a valuable reagent for studies focused on natural product chemistry and pharmacological applications.

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