GPCR/G Protein

Items 1801-1850 of 5455

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  1. 5-HT1A Receptor Antagonist

    MM 77 dihydrochloride is a selective antagonist of the 5-HT1A receptor, primarily exhibiting an inhibitory effect on postsynaptic serotonin signaling. This compound demonstrates notable anxiolytic-like properties, making it valuable for research exploring anxiety disorders and related neuropharmacological mechanisms. Its specificity for the 5-HT1A receptor positions it as a useful tool in investigating serotonin receptor functions and therapeutic interventions in psychiatric conditions.
  2. 5-HT4 Receptor Antagonist

    SC-53606 is a potent and selective antagonist of the 5-HT4 receptor, exhibiting a pA2 value of 8.13. It effectively inhibits the 5-HT4 receptor-mediated relaxation in Carbachol-induced contractions, making it valuable for studying gastrointestinal motility and related disorders. This compound is useful in research focused on neuropharmacology and the serotonergic system.
  3. Piperazine

    1-(3-Fluorophenyl)piperazine (hydrochloride) is a selective blocker of the 5-HT receptor 1A and an adrenergic receptor antagonist. This compound exhibits significant biological activity relevant to research in neuropharmacology, particularly in the study of serotonergic and adrenergic signaling pathways. It can be utilized in various applications, including the investigation of anxiety, depression, and other mood disorders.
  4. 5-HT Receptor

    WAY-100135 is a serotonergic compound that acts primarily as a potent antagonist of the 5-HT1A receptor and a partial agonist of the 5-HT1D receptor, exhibiting minimal activity at the 5-HT1B receptor. This compound is valuable in research applications focused on serotonin receptor signaling and its implications in neuropharmacology. WAY-100135 is commonly used to investigate the role of serotonergic pathways in various physiological and pathological conditions.
  5. 5-HT1B Agonist

    CP94253 is a selective agonist of the serotonin receptor 1B (5-HT1B) that operates through competitive binding at the receptor site. This compound demonstrates notable biological activities including inducing satiety, anorexia, weight loss, and hyperlocomotion in rat models. Its binding affinities to various serotonin receptors, including 5-HT1A, 5-HT1D, 5-HT1C, and 5-HT2, make it valuable for research in appetite regulation and behavioral studies.
  6. (5-HT)3-receptor Antagonist

    YM114 is a highly selective antagonist of the 5-HT3 receptor, demonstrating notable potency in inhibiting receptor activity. It has been shown to disrupt the Bezold-Jarisch reflex induced by 2-methyl-5-HT without affecting bradycardia resulting from Veratridine or electrical stimulation in anesthetized rats. This compound offers valuable insights into cardiovascular and neuropharmacological research applications, particularly in understanding the role of 5-HT3 receptors in vagal afferent nerve signaling.
  7. 5-HT2B Inhibtor

    EGIS-7625 is a selective competitive inhibitor of the 5-HT2B receptor, exhibiting pKi values of 9.0 for 5-HT2B, and 6.2 and 7.7 for 5-HT2A and 5-HT2C, respectively. This compound has been shown to partially counteract m-chlorophenylpiperazine-induced hypomotility and hypophagia. EGIS-7625 is a valuable tool for investigating the role of 5-HT2B in various physiological and pathological processes, making it suitable for research in neuropharmacology and behavioral studies.
  8. 5-HT1B/1D Receptor Agonist

    Avitriptan is a selective agonist of the 5-HT1B and 5-HT1D receptors, exhibiting pKis of 7.44 for 5-HT1B in rats, 7.68 for 5-HT1B in humans, and 8.36 for 5-HT1D in humans. This compound induces vasoconstriction in isolated coronary arteries, suggesting its relevance in cardiovascular research. Avitriptan is primarily utilized in the treatment of migraines, providing insights into serotonergic pathways and their role in headache disorders.
  9. 5-HT1A Receptor Agonist

    Osemozotan hydrochloride is a selective 5-HT1A receptor agonist, known for its ability to modulate serotonin signaling. This compound has been shown to reduce the number of c-Fos-positive cells induced by MAMP in murine models, indicating its potential neuroprotective effects. Osemozotan hydrochloride is primarily utilized in research related to depressive disorders.
  10. 5-HT2A Agonist

    VU6067416 is a highly potent agonist of the 5-HT2A receptor, exhibiting an EC50 of 189 nM. Its ability to penetrate the blood-brain barrier makes it particularly valuable for neuropharmacological studies. This compound is useful for investigating the role of 5-HT2A receptor activation in various neurological and psychiatric disorders.
  11. 5-HT2 Receptor Antagonist

    Sergolexole maleate is a potent antagonist of the 5-HT2 receptor, which plays a crucial role in various serotonin-mediated physiological processes. This compound exhibits significant inhibitory effects on serotonin-enhanced platelet aggregation, making it relevant for research into cardiovascular function and platelet behavior. Its role in modulating serotonin activity positions Sergolexole maleate as a valuable tool for exploring mechanisms associated with mood disorders and thrombotic conditions.
  12. 5-HT Receptor Antagonist

    JNJ-18038683 free base is a potent antagonist of the 5-Hydroxytryptamine Type 7 (5-HT7) receptor, demonstrating pKis of 8.19 and 8.20 for rat and human 5-HT7 receptors, respectively, in HEK293 cell assays. This compound exhibits significant biological activity relevant for the investigation of psychiatric disorders and neuropharmacology. It serves as a valuable tool for researchers exploring the therapeutic potential of 5-HT7 receptor modulation.
  13. 5-HT2C Agonist

    5-HT2C agonist-4 is a selective agonist for the 5-HT2C receptor with an EC50 of 5.7 nM. This compound has demonstrated the ability to reduce locomotor activity in zebrafish larval models, making it a valuable tool for studies on neuropharmacology and behavior. Its use in research may facilitate investigations into the role of serotonin receptors in various physiological and pathological processes.
  14. 5-HT2A Agonist

    AC-90179 is a selective 5-HT2A receptor agonist, exhibiting a Ki value of 2.1 nM. This compound also acts as a 5-HT2C antagonist, suggesting its potential utility in the development of antipsychotic therapies. Its modulation of serotonergic signaling supports its application in investigating psychiatric disorders and related biological processes.
  15. 5-HT Receptor

    NAN-190 is a selective antagonist of the serotonin 5-HT receptor, primarily targeting the 5-HT1A subtype. It exhibits significant biological activity by blocking serotonin-mediated signaling, making it a valuable tool for investigating the role of serotonin in various physiological processes. NAN-190 is commonly utilized in research related to neuropharmacology and anxiety disorders, providing insights into the effects of serotonin modulation on behavior and mood regulation.
  16. 5-HT1F Receptor Ligand

    LY302148 is a partial agonist of the 5-HT1F receptor, demonstrating significant interaction with this target. In the [35S]GTPγS binding assay for human 5-HT1F receptors, it exhibits a potent EC50 value of 5.23 nM. This compound is of interest for research applications related to migraine pathophysiology and the potential development of therapeutic strategies.
  17. 5-HT Receptor Agonist

    VRX-03011 is a selective 5-HT receptor agonist that has shown promise in enhancing memory and modulating acetylcholine release in the hippocampus. This compound may influence APP metabolism, making it a valuable tool for research in neuropharmacology and cognitive function studies. Notably, VRX-03011 is associated with minimal gastrointestinal side effects, providing a safer alternative for in vivo applications.
  18. 5HT1A Receptor Agonist

    Piclozotan is a selective 5HT1A receptor agonist that has demonstrated potential in the treatment of motor complications associated with Parkinson's disease. By activating the 5HT1A receptor, Piclozotan may enhance dopaminergic transmission and alleviate symptoms in relevant preclinical models. This compound serves as a valuable tool for research into neurodegenerative disorders and the modulation of serotonergic pathways.
  19. 5-HT1A Agonist

    S-14671 is a potent agonist of the 5-HT1A receptor, exhibiting a high affinity with a pKi of 9.3. This compound plays a crucial role in the study of neurological disorders, particularly in the exploration of therapeutic strategies for anxiety and depression. Its specific targeting of the 5-HT1A receptor makes it a valuable tool for advancing research in neuropharmacology and related fields.
  20. 5-HT4 Antagonist

    SB 204070A is a selective antagonist of the 5-hydroxytryptamine receptor subtype 4 (5-HT4). It effectively inhibits 5-HT4 receptor activity, making it valuable for studies investigating serotonergic signaling pathways. Additionally, SB 204070A can be utilized to assess the functional roles of 5-HT4 receptors in various biological systems, contributing to research on gastrointestinal motility and cognitive function.
  21. 5HT-4/5HT-3 Antagonist

    Lintopride hydrochloride is a benzamide derivative that acts as a potent antagonist of the 5HT-4 receptor and exhibits moderate antagonistic effects on the 5HT-3 receptor. This compound enhances gastric emptying, stimulates antral and duodenal motility, and accelerates intestinal transit in preclinical models. Additionally, Lintopride hydrochloride significantly elevates the basal tone of the lower esophageal sphincter, making it valuable for research on gastrointestinal motility and related disorders.
  22. 5-HT6 Receptor Antagonist

    SB-773812 is a high-affinity antagonist of the serotonin 5-HT6 receptor, exhibiting a pKi of 8.1. Additionally, it demonstrates moderate to high affinity for dopamine receptors 2 and 3, with pKi values of 7.4 and 8.5, respectively. This compound is primarily used in research investigating central nervous system disorders, particularly those involving serotonin and dopamine signaling pathways. Its profile suggests potential applications in studying neuropharmacology and related therapeutic areas.
  23. 5-HT1D Receptor Agonist

    L 775,606 is a potent and selective agonist of the 5-HT1D receptor. This compound is primarily utilized in the investigation of migraine headache mechanisms and therapeutic approaches, demonstrating its significant role in modulating serotonergic signaling pathways relevant to headaches. Its specificity for the 5-HT1D receptor makes it an important tool in pharmacological research on migraine treatments.
  24. 5-HT3/6 Receptor Antagonist

    FPPQ is a dual-acting antagonist of the 5-HT3 and 5-HT6 receptors, demonstrating high affinity with Ki values of 0.9 nM and 3 nM, respectively. This compound exhibits significant antipsychotic and procognitive effects, making it a valuable tool for research into neuropsychiatric disorders. Its ability to modulate serotonergic signaling positions FPPQ as a promising candidate for studies focused on cognitive enhancement and the treatment of mental health conditions.
  25. 5-HT2C Antagonist

    FR260010 free base is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 1.1 nM. This compound is instrumental in research applications focused on elucidating the role of 5-HT2C receptors in various physiological and pathological processes, including anxiety and mood disorders. Its specificity makes it a valuable tool for investigating serotonergic signaling pathways and developing therapeutic strategies targeting the serotonergic system.
  26. 5-HT1A receptor Agonist

    CSP-2503 is a highly selective agonist of the 5-HT1A receptor, exhibiting an EC50 of 0.15 μM and a Ki value of 4.1 nM. This compound demonstrates significant selectivity against α1-adrenoceptors, 5-HT4 receptors, and benzodiazepine receptors, with Ki values exceeding 1000 nM. CSP-2503 reduces cAMP levels in vitro and displays anxiolytic effects in vivo, making it a valuable tool for investigating anxiety-related disorders.
  27. 5-HT7 Antagonist

    DR4485 hydrochloride is a selective antagonist of the 5-HT7 receptor, demonstrating a potent pKi of 8.14. This compound is utilized in various research applications focused on neuropharmacology and the modulation of serotonergic signaling pathways. Its oral bioavailability makes it a valuable tool for in vivo studies investigating the role of the 5-HT7 receptor in neurological disorders.
  28. 5-HT1A Receptor Antagonist

    S14063 is a potent antagonist of the 5-HT1A receptor. It selectively inhibits this receptor without exhibiting β-adrenoceptor blocking properties. S14063 is utilized in research applications focusing on serotonergic signaling and its implications in neuropharmacology.
  29. 5-HT6R Agonist

    EMD 386088 free base is a potent agonist of the serotonin 6 receptor (5-HT6R). It has been shown to induce cell death and modulate ERK1/2 activity, making it a valuable tool in the study of neurodegenerative disorders. This reagent is particularly relevant for research applications related to Alzheimer's disease and schizophrenia, where 5-HT6R signaling plays a significant role.
  30. 5-HT2A Receptor Agonist

    5-HT2A receptor agonist-5 is a potent agonist that targets the 5-HT2A receptor, exhibiting a Ki value of 0.017 µM. It has been shown to demonstrate antidepressant activity, making it a valuable tool for research into mood disorders and the mechanisms of serotonergic signaling. This compound may be beneficial in studies aimed at understanding the therapeutic potential of 5-HT2A receptor modulation.
  31. Stable Isotope

    Deulumateperone is a deuterated derivative of Lumateperone, serving as a stable isotope for research applications. Lumateperone acts as a selective antagonist of the 5-HT2A receptor (Ki = 0.54 nM) and modulates dopamine receptors, demonstrating significant antipsychotic and antineoplastic properties. This reagent is valuable for studies involving receptor interactions, pharmacokinetics, and metabolic profiling in various biological systems.
  32. 5-HT6 Receptor Antagonist

    SB357134 is a potent and selective antagonist of the 5-HT6 receptor, demonstrating significant brain penetration and oral bioavailability. This compound has been shown to enhance memory and learning capabilities while increasing seizure thresholds in rodent models. It is valuable for research applications focused on neuropharmacology, cognitive function, and the modulation of serotonergic signaling pathways.
  33. Light-Activated Caged 5-HT

    BHQ-O-5HT is a light-activated caged form of serotonin (5-HT), utilizing a BHQ group for protection. Upon irradiation with light at wavelengths of either 365 or 740 nm, BHQ-O-5HT undergoes photolytic cleavage, releasing 5-HT via one or two-photon excitation. This reagent is valuable for time- and spatially-resolved studies, enabling researchers to investigate the multifaceted roles of 5-HT in mood regulation, appetite control, memory processes, learning, and other cognitive functions.
  34. 5-HT Receptor Antagonist

    Elzasonan is a selective antagonist of the 5-hydroxytryptamine 1B (5-HT1B) receptor. This compound exhibits significant biological activity by inhibiting 5-HT1B receptor signaling, which plays a crucial role in the regulation of mood and anxiety. Elzasonan is primarily utilized in research focused on the pathophysiology of depression and the development of novel antidepressant therapies.
  35. 5-HT Receptor

    (R)-RS 56812 hydrochloride is a selective antagonist of the 5-HT3 receptor, demonstrating significant effects on cognitive function. Research shows that the (R) isomer provides more consistent enhancements in performance on delayed matching tasks in primates compared to its (S) counterpart. This compound presents potential therapeutic applications in conditions associated with cognitive decline.
  36. 5-HT7 Receptor Ligand

    PZ-1129 is a selective ligand for the 5-HT7 receptor, exhibiting a Ki of 7 nM, with moderate affinity for 5-HT1A and D2 receptors (Ki values of 159 nM and 24 nM, respectively). This compound effectively inhibits constitutive cAMP production via the Gs signaling pathway, with an EC50 of 13.7 nM. PZ-1129 is suitable for research into emotional disorders, including depression and bipolar disorder, providing a valuable tool for understanding the underlying mechanisms of these conditions.
  37. 5-HT1A Receptor Antagonist

    UH 301 hydrochloride is a selective antagonist of the 5-HT1A receptor. This compound has been shown to modulate the consolidation of learning processes in both normal and cognitively impaired rodent models. UH 301 hydrochloride is primarily utilized in research applications focused on Alzheimer's disease and various forms of amnesia, providing insights into therapeutic interventions for cognitive enhancement.
  38. Dopamine/5-HT Receptor Inhibitor

    Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways.
  39. 5-HT1A Receptor Partial Agonist

    Adatanserin hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting high affinity with a Ki value of 1 nM. Additionally, it acts as a moderate affinity antagonist at the 5-HT2 receptor with a Ki of 73 nM. This compound demonstrates significant anxiolytic and antidepressant effects, making it valuable for research into anxiety and depression models.
  40. 5-HT Receptor Antagonist

    Alverine hydrochloride is a potent antagonist of the 5-HT1A receptor, exhibiting an IC50 value of 101 nM. This compound is primarily utilized in gastrointestinal research to investigate its effects on smooth muscle contraction and motility. Its role in modulating serotonin signaling makes it valuable for studies related to gastrointestinal disorders and therapeutic interventions targeting 5-HT receptors.
  41. 5-HT Receptor Agonist

    Flesinoxan hydrochloride is a selective agonist for the 5-hydroxytryptamine 1A (5-HT1A) receptor, exhibiting high affinity with an EC50 value of 24 nM. It demonstrates significant anxiolytic and antidepressant properties, contributing to its potential as a therapeutic agent in mood and anxiety disorders. This compound is valuable for research focused on neuropharmacology and the modulation of serotonergic pathways.
  42. 5-HT1 Receptor Antagonist

    SB-272183 is a selective antagonist of the 5-HT1A, 5-HT1B, and 5-HT1D receptors, demonstrating high binding affinity with pKi values of 8.0, 8.1, and 8.7, respectively, in both human recombinant and native tissues. Its primary mechanism targets serotonin receptors, making it a valuable tool for studying the role of serotonin signaling in various biological processes. SB-272183 is particularly relevant in antidepressant research, aiding in the exploration of potential therapeutic pathways for mood disorders.
  43. 5-HT3 Receptor Partial Agonist

    RS-56812 is a partial agonist of the 5-HT3 receptor, known to significantly enhance colonic propulsive peristalsis. By indirectly promoting cholinergic neurotransmission, RS-56812 has also been shown to improve working memory performance in non-human primates. This compound is utilized in research investigating diarrheal disorders, colon motility, and cognitive impairments, including Alzheimer's disease.
  44. 5-HT2A Agonist

    25N-N1-Nap is a β-arrestin-biased agonist of the 5-HT2A receptor. It has demonstrated the ability to antagonize phencyclidine-induced hyperactivity in male C57BL/6 J mice, indicating its potential use in research on psychostimulant behaviors. This compound is valuable for studies investigating serotonin receptor signaling and its implications in neuropsychiatric disorders.
  45. 5-HT2 Antagonist

    Methiothepin maleate is a potent and non-selective antagonist of the 5-HT2 receptor family, demonstrating affinity with pKis of 8.50 for 5-HT2A, 8.68 for 5-HT2B, and 8.35 for 5-HT2C. This compound effectively inhibits various serotonin receptor subtypes, including 5-HT1A through 5-HT7, making it a valuable tool for studying serotonin signaling pathways. Methiothepin maleate is commonly used in neuropharmacology research to investigate the role of serotonin in mood regulation, psychosis, and related disorders.
  46. 5-HT1A Receptor Agonist

    SSR-181507 hydrochloride is a selective 5-HT1A receptor agonist with additional activity as a dopamine D2 receptor antagonist. It has demonstrated the ability to inhibit Apomorphine-induced climbing behavior in mice and reduce stereotypic behaviors in rats. This compound is employed in research focused on understanding and treating conditions such as depression and anxiety.
  47. 5-HT Receptor Antagonist

    Alprenolol benzoate serves as a non-selective β-adrenoceptor antagonist with an additional mechanism as a 5-HT1A and 5-HT1B receptor antagonist. This compound exhibits significant biological activity in reducing blood pressure, alleviating angina, and managing arrhythmias. It is essential for research focused on cardiovascular conditions and the modulation of serotonin receptors in various physiological and pathological contexts.
  48. 5-HT1A Receptor Modulator

    Galanin (1-15) (porcine, rat) is a peptide fragment consisting of the N-terminal 15 amino acids of the neuropeptide galanin, primarily acting as a modulator of the 5-HT1A receptor. This compound has been shown to interact with the 5-HT1A receptors in the dorsal hippocampus of the rat brain, effectively reducing their affinity and influencing serotonin neuronal networks. Galanin (1-15) is valuable for research applications related to neurobiology, particularly in studies investigating serotonin modulation and its effects on mood and anxiety disorders.
  49. 5-HT2 Receptor Antagonist

    DOAM is a selective antagonist of the 5-HT2 receptor, modulating serotonergic signaling pathways. This compound is primarily utilized in research focused on neuropharmacology and psychiatric disorders, providing insights into the effects of serotonin in various biological systems. Its inhibition of 5-HT2 receptor activity makes it a valuable tool for studying the mechanisms underlying mood regulation and related pharmacological interventions.
  50. 5-HT1A Receptor Antagonist

    S-14489 is a selective antagonist of the postsynaptic 5-HT1A receptor, exhibiting a high affinity with a pKi of 9.2. This compound can function as an agonist at 5-HT1A autoreceptors and effectively inhibit the accumulation of 5-hydroxytryptophan in the striatum. S-14489 is primarily employed in neurological research, particularly for studying disorders related to serotonin signaling.

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