GPCR/G Protein

Items 3151-3200 of 5455

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. Dopamine Receptor

    FAUC 3019 is a partial agonist of the dopamine D4 receptor. This compound demonstrates a significant stimulatory effect on penile erection in male rats, particularly at low concentrations. FAUC 3019 is a valuable tool for exploring the physiological mechanisms underlying erectile function and has potential applications in the study of sexual health and related disorders.
  2. Dopamine D2 Receptor Antagonist

    Dehydrate haloperidol is a selective antagonist of the human dopamine D2 receptor, exhibiting a pKd of 8 and a pKi of 8. This compound is primarily utilized in research focused on schizophrenia and related disorders, providing insights into dopamine signaling pathways and their role in neuropsychiatric conditions.
  3. Dopamine Receptor

    BP14979 is a selective agonist of the dopamine D3 receptor, primarily utilized in the investigation of neurological disorders. Its structural properties allow for the modulation of D3 receptor efficacy, making it a valuable tool in the development of ligands with enhanced selectivity and affinity. By understanding the differences in efficacy compared to D3 receptor antagonists, BP14979 offers significant potential for optimizing therapeutic agents in drug development.
  4. Stable Isotope

    Pramipexole-d7-1 dihydrochloride is a deuterium-labeled analog of Pramipexole dihydrochloride, a selective agonist of dopamine D2-type receptors. This compound effectively penetrates the blood-brain barrier and exhibits Ki values of 2.2 nM, 3.9 nM, 0.5 nM, and 1.3 nM for the D2-type receptor, D2, D3, and D4 receptors, respectively. Pramipexole-d7-1 dihydrochloride is valuable for research on Parkinson's disease and restless legs syndrome, facilitating advanced studies in neuropharmacology and the pharmacokinetics of dopamine receptor interactions.
  5. D2 Receptor Partial Agonist

    Dopamine D2 receptor agonist-3 is a selective partial agonist for the D2 receptor, exhibiting a pEC50 of 8.3. Additionally, it acts as an antagonist at the D3 receptor with a pEC50 of less than 5.5. This compound is valuable for research into dopamine receptor signaling pathways and may provide insights into neuropsychiatric disorders.
  6. Stable Isotope

    Ropinirole-d7 hydrochloride is a deuterium-labeled analog of Ropinirole hydrochloride, functioning as a potent agonist for D2 and D3 dopamine receptors. With a Ki value of 29 nM for the D2 receptor, it demonstrates strong biological activity, exhibiting pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively, while showing no affinity for D1 receptors. This compound is particularly relevant in research focused on Parkinson's disease and neuropharmacology.
  7. Dopamine Receptor Antagonist

    Dopamine D3 receptor antagonist-2 is a selective antagonist for the dopamine D3 receptor, exhibiting a Ki value of 2.16 nM. This compound serves as a multitarget bitopic ligand and has potential applications in the study and treatment of various central nervous system disorders, including schizophrenia and addiction-related conditions. Its specificity for the D3 receptor makes it a valuable tool for research into dopamine-mediated neuropharmacology.
  8. Functionally Selective Ligand for Dopamine D2 Receptor

    UNC10099984A is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 value of 6.2 nM for β-arrestin. This compound is particularly valuable for investigating central nervous system disorders associated with D2 receptor modulation, facilitating research into dopamine signaling pathways and their therapeutic implications.
  9. Dopamine Receptor Inhibitor

    TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system.
  10. Dopamine Receptor Agonist

    BAM-1110 is a dopamine receptor agonist that demonstrates dose-dependent antiparkinsonian effects in MPTP-treated monkey models of Parkinson's disease. Its ability to activate dopamine receptors makes it a valuable tool for investigating Parkinson's disease and other neurological disorders. Additionally, BAM-1110 is characterized by minimal side effects, enhancing its suitability for research applications in this field.
  11. Dopamine Receptor Agonist

    CQP-201403 is a selective dopamine receptor agonist that activates dopamine receptors to modulate neurotransmission. This compound is primarily utilized in the study of neurological diseases, offering insights into dopaminergic signaling and potential therapeutic pathways. Its application in research facilitates the exploration of mechanisms underlying conditions such as Parkinson's disease and schizophrenia.
  12. Dopamine D3 Receptor Antagonist

    SB-414796 is a selective antagonist of the dopamine D3 receptor, exhibiting potent inhibitory activity with a Ki value of 4 nM. This compound demonstrates significantly lower affinity for the D2 receptor, noted at 400 nM. It is capable of crossing the blood-brain barrier, making it suitable for investigating the role of dopamine D3 receptors in neuropharmacology and potential therapeutic applications related to related neuropsychiatric disorders.
  13. D3R/MOR Antagonist

    D3R/MOR Antagonist 1, a dual antagonist targeting the D3 receptor and the mu-opioid receptor, exhibits affinities of Ki values at 46.5 nM and 691 nM, respectively. This compound is designed to potentially elicit analgesic effects while minimizing opioid misuse liability through D3R antagonism. Its unique mechanism makes it a valuable tool for research in pain management and substance use disorders.
  14. Dopamine D3 Receptor Antagonist

    NGB 2904 hydrochloride is a selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 1.4 nM. This compound demonstrates a strong preference for the D3 receptor over other targets, including D2, 5-HT2, α1, D4, D1, and D5 receptors, as evidenced by significantly higher Ki values. NGB 2904 hydrochloride effectively antagonizes Quinpirole-stimulated mitogenesis, making it a valuable tool for research in dopamine signaling and related neurological studies.
  15. D3 receptor antagonist

    U-99194 is a selective and potent antagonist of the dopamine D3 receptor. This compound effectively inhibits D3 receptor activation induced by endogenous dopamine and exogenous D3 agonists, as demonstrated by its ability to negate the IPSC-suppressive effects of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 also significantly suppresses nicotine-induced tremors in mice, making it a valuable tool for investigating dopamine D3 receptor-related motor disorders, especially those involving kinetic tremors.
  16. Dopamine D2 Receptor Antagonist

    Flupenthixol decanoate is a dopamine D2 receptor antagonist known for its antipsychotic properties. This compound is commonly utilized in research focused on schizophrenia and depression, enabling investigations into the underlying mechanisms of these psychiatric disorders. Its long-acting formulation supports studies on sustained therapeutic effects and dosing regimens.
  17. D3 Receptor Ligand

    Dopamine D3 receptor ligand-2 is a selective antagonist targeting the D3 dopamine receptor, exhibiting a Ki of 11.4 nM. This compound demonstrates high selectivity, showing minimal affinity for the D2 receptor with a Ki of 1228 nM. It is valuable for studies related to neurological disorders, addiction research, and the exploration of dopaminergic pathways.
  18. Dopamine Receptor Inhibitor

    Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile.
  19. D3/D2 Receptor Antagonist

    PF-4363467 is a selective antagonist of the dopamine D3 and D2 receptors, demonstrating a Ki value of 3.1 nM for D3R and 692 nM for D2R. This compound effectively reduces opioid drug-seeking behavior while minimizing the associated side effects typically linked to D2 receptor antagonism. PF-4363467 is valuable for research applications focused on addiction and neuropharmacology, providing insights into dopaminergic modulation in therapeutic contexts.
  20. D2R/SSTR2 Agonist

    Onzigolide is a chimeric compound that acts as a potent agonist at dopamine type 2 (D2R) and somatostatin type 2 (SSTR2) receptors. This dual receptor activation may play a crucial role in modulating neuroendocrine and neurological functions. It is particularly relevant in research focused on neuropsychiatric disorders and endocrine-related conditions, contributing to the understanding of receptor interactions and their implications in therapeutic contexts.
  21. D4R Antagonist

    D4R antagonist-2 is a selective antagonist of the D4 dopamine receptor, exhibiting an IC50 of 6.52 µM. This compound demonstrates favorable in vitro pharmacokinetic properties and effective brain penetration. D4R antagonist-2 is suitable for research applications related to Parkinson's disease and other neurological disorders.
  22. Antipsychotic Agent

    Pipotiazine palmitate is a dopamine receptor antagonist primarily used as an antipsychotic agent. As a long-acting phenothiazine derivative, it is suitable for intramuscular administration, providing sustained therapeutic effects. This compound is valuable in research applications focused on mental illnesses, particularly schizophrenia, facilitating studies into its neuropharmacological effects and treatment strategies.
  23. Dopamine D2 Receptor Agonist

    (-)-IHCH7041 is a selective and orally active agonist of the dopamine D2 receptor, exhibiting a Ki value of 22.44 nM. It effectively activates the Gαi1 protein and β-arrestin2 signaling pathways with EC50 values of 1.38 nM and 2.75 nM, respectively. This compound has demonstrated potential in enhancing cognitive function and memory capacity, making it valuable for research into neurological disorders, including Alzheimer's disease.
  24. D-2 Dopamine Receptor Agonist

    RU-24213 hydrochloride is a selective agonist for the D-2 dopamine receptor, known to modulate dopaminergic signaling. Additionally, it acts as an antagonist at the kappa-opioid receptor, contributing to its pharmacological profile. This compound has been observed to induce stereotyped behaviors, making it valuable for research in neuropharmacology and the exploration of dopamine-related conditions.
  25. α1-adrenergic Receptor Antagonist

    Butanserin is a selective antagonist of the α1-adrenergic receptor, primarily utilized in cardiovascular research. This compound modulates adrenergic signaling pathways, making it valuable for investigating the role of α1-adrenoceptors in various cardiovascular conditions. Its potency and specificity support its application in studies aimed at understanding hypertension and heart failure mechanisms.
  26. α2 Receptor Antagonist

    Napitane mesylate is a selective antagonist of presynaptic α2 adrenergic receptors, impacting norepinephrine reuptake inhibition. This compound demonstrates significant antidepressant activity, making it relevant for research in mood disorders and neuropharmacology. It is utilized to explore the modulation of noradrenergic neurotransmission and its effects on depressive states.
  27. α2-adrenergic Agonist

    Detomidine is a potent α2-adrenergic agonist characterized by its imidazole structure. Its primary mechanism involves the activation of α2-adrenergic receptors, leading to significant analgesic effects in a dose-dependent manner. This compound is commonly utilized in veterinary medicine for sedation and analgesia, as well as in research applications focused on examining α2-adrenergic signaling pathways.
  28. ADRB2 Agonist

    Indacaterol xinafoate is a potent β2-adrenergic receptor agonist known for its long-acting bronchodilatory effects. By inhibiting NF-κB activity in a β-arrestin2-dependent manner, it not only improves lung function but also mitigates further lung damage, making it relevant in the context of chronic obstructive pulmonary disease (COPD). This compound serves as a valuable tool for research into asthma and related respiratory disorders.
  29. Stable Isotope

    Tetrahydrozoline-d4 hydrochloride is a deuterium-labeled form of Tetrahydrozoline hydrochloride, an α-adrenergic agonist that targets α-adrenergic receptors to induce vasoconstriction. This stable isotope is utilized in research applications focusing on nasal and conjunctival congestion. Its unique isotopic labeling allows for enhanced tracking and quantification in various biochemical studies.
  30. β-adrenergic Blocker

    Bunitrolol hydrochloride is a β-adrenergic blocker known for its high affinity for β-adrenergic receptors and its significant antagonist activity. It also exhibits weak α1-blocking effects. This compound is primarily utilized in research related to cardiovascular diseases, including hypertension and angina pectoris, and is applicable in studies of placental transport.
  31. Silodosin Racemate

    (Rac)-Silodosin is a racemic mixture that targets the α1A-adrenergic receptor (α1A-AR) as a potent and selective antagonist. This compound is primarily utilized in research related to urology and the treatment of benign prostatic hyperplasia (BPH), contributing to the understanding of adrenergic signaling pathways. Its oral bioavailability makes it a significant candidate for pharmacological studies focusing on α1-adrenergic receptor modulation.
  32. Adrenergic Receptor

    2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide targets adrenergic receptors and is recognized as a genotoxic derivative of Atenolol. This compound has been shown to induce DNA fragmentation in rat hepatocytes at concentrations between 0.1 and 1 mM, making it a valuable tool for studying genotoxic mechanisms and the effects of adrenergic signaling in cellular contexts. Its applications extend to research involving DNA damage and repair pathways.
  33. Adrenergic Receptor Agonist

    Octopamine is a biogenic monoamine that functions as an adrenergic receptor agonist, primarily targeting alpha2-adrenoceptors. It serves as a neurohormone, neuromodulator, and neurotransmitter in invertebrates. In vitro studies demonstrate that Octopamine enhances glycogenolysis, glycolysis, oxygen uptake, and gluconeogenesis, along with increasing portal perfusion pressure. This compound is valuable for research in neurobiology, metabolism, and cardiovascular studies.
  34. Adrenergic Receptor Inhibitor

    Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions.
  35. α2 Agonist

    Apraclonidine dihydrochloride is a selective α2 adrenergic receptor agonist with weak activity at α1 receptors. This compound is primarily used to reduce intraocular pressure (IOP) in various ophthalmic conditions. Its effectiveness in lowering IOP makes it a valuable tool in the study of glaucoma and other eye disorders.
  36. β2-adrenergic Receptor Agonist

    Trantinterol hydrochloride is a potent agonist of the β2-adrenergic receptor, demonstrating significant efficacy in bronchial relaxation. It serves as a valuable tool in the investigation of asthma and other respiratory conditions. This compound may aid in understanding the mechanisms of bronchial hyperreactivity and support the development of therapeutic strategies targeting β2-adrenergic pathways.
  37. Adrenergic Receptor Agonist

    BFE-55 is a derivative of befunolol that acts as a β-adrenergic receptor partial agonist. This compound exhibits significant biological activity by modulating adrenergic signaling pathways. BFE-55 can be utilized in research focused on cardiovascular dynamics and therapeutic interventions targeting adrenergic receptors.
  38. Adrenoreceptor Agonist

    Colterol hydrochloride is an agonist of the adrenergic receptors, demonstrating significant affinity for the β1-adrenoreceptor and β2-adrenoreceptor, with respective IC50 values of 645 nM and 147 nM. It exhibits potent bronchodilator activity, making it valuable for research applications related to respiratory conditions. This compound can be utilized in studies investigating cardiovascular responses and airway reactivity, contributing to the understanding of adrenergic signaling pathways.
  39. Adrenergic Receptor Agonist

    Amibegron is a selective β3-adrenergic receptor agonist, demonstrating an EC50 of 3.5 nM for activation of β-adrenoceptors in rat colon tissues. This compound exhibits notable anxiolytic and antidepressant properties, making it a valuable tool for research in neuropharmacology and the study of mood disorders. Its specificity for β3-adrenergic receptors lends it potential applications in exploring metabolic and cardiovascular responses.
  40. β3-adrenergic Receptor Agonist

    SB251023 is a selective β3-adrenergic receptor agonist, exhibiting pEC50 values of 7.14 for the β3a and 6.91 for the β3b receptor subtypes. This compound effectively modulates intracellular cyclic AMP levels and influences extracellular acidification rates (EAR) in cellular systems. SB251023 is relevant for research into cardiovascular diseases and metabolic disorders, providing insights into the therapeutic potential of β3-adrenergic signaling in related pathologies.
  41. Drug Metabolite

    Deacetylmoxisylyte is an orally active drug metabolite derived from the prodrug Moxisylyte, primarily targeting alpha-1 and alpha-2 adrenoceptors. It demonstrates significant affinity and selectivity in rabbit corpus cavernosum and urethra tissues, with IC50 values of 400 nM and 1200 nM, respectively. This compound is valuable in pharmacological research focused on understanding adrenergic receptor interactions and their physiological effects.
  42. Adrenergic Receptor Antagonist

    Phenoprolamine hydrochloride is an adrenergic α1 receptor antagonist known for its potent antihypertensive properties. In addition to lowering blood pressure, it exhibits neuroprotective and cardioprotective activities. This compound also inhibits the enzymatic activity of CYP2D and CYP3A, resulting in the down-regulation of their mRNA transcription, which may have implications in drug metabolism studies and cardiovascular research.
  43. Metabolite

    4-Hydroxy xylazine O-glucuronide lithium is a metabolite derived from the α2-adrenergic receptor agonist xylazine. This compound serves as an important biochemical marker, aiding in the study of xylazine metabolism and its physiological effects. It can be synthesized from xylazine through the intermediate metabolite 4-hydroxy xylazine and is valuable in pharmacokinetic and toxicological research applications.
  44. β1/β2 Adrenergic Receptor Antagonist

    4-Hydroxypropranolol-d7 hydrochloride is a deuterated derivative of 4-Hydroxypropranolol, functioning as a potent β1/β2 adrenergic receptor antagonist. It exhibits equivalent potency to its parent compound Propranolol, with pA2 values of 8.24 and 8.26 for β1 and β2 receptors, respectively. This compound is characterized by its intrinsic sympathomimetic activity, membrane stabilizing effects, and significant antioxidant properties, making it valuable for various biochemical and pharmacological research applications.
  45. α-Adrenoreceptor Antagonist

    Taprizosin is an α-adrenoreceptor antagonist that selectively inhibits the activity of α1-adrenergic receptors. It has demonstrated efficacy in modulating vascular smooth muscle contraction and influencing blood pressure regulation. This compound is primarily utilized in cardiovascular research, particularly in studies focused on hypertension and related disorders.
  46. α-2B adrenergic receptor Agonist

    AGN-201781 is an orally active agonist of the α-2B adrenergic receptor. This compound exhibits significant biological activity in modulating adrenergic signaling pathways, making it a valuable tool for research into neuropathic pain mechanisms and potential therapeutic interventions. Its specificity for the α-2B receptor supports investigations into pain management and related neurological studies.
  47. α1-Adrenoceptor Ligand

    CHIR-2279 is a high-affinity ligand for the α1-adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 5 nM. This compound serves as a valuable tool for investigating the α1-adrenoceptor signaling pathways and has potential applications in drug development aimed at cardiovascular and other relevant disorders.
  48. β-Adrenergic Receptor Agonist

    Hexoprenaline sulfate is a selective β-adrenergic receptor agonist that promotes bronchodilation. This compound enhances adenylate cyclase activity, leading to an increased uptake of 14C-Aminopyrine. Additionally, Hexoprenaline sulfate exhibits anti-inflammatory and anti-infective properties, while also demonstrating effects on placental weight and blood flow. It is applicable in research areas including inflammation, immunology, infection, endocrinology, and the study of neurological diseases, such as asthma, chronic bronchitis, sepsis, and organophosphorus compound intoxication.
  49. Adrenergic Receptor Antagonist

    RU 52583 is an oral bioactive antagonist of the alpha-2 adrenergic receptor. This compound has been shown to enhance cognitive function in rodent models with septohippocampal system damage, indicating its potential utility in studying cognitive disorders. Its pharmacological profile may provide insights into the modulation of adrenergic signaling in various neurological research applications.
  50. Stable Isotope

    Solabegron-d8 is a deuterium-labeled derivative of Solabegron, a selective β3-adrenergic receptor agonist. It effectively stimulates cAMP accumulation in Chinese hamster ovary cells expressing human β3-adrenergic receptors, exhibiting an EC50 value of 22 nM. This compound is primarily utilized in research focused on the treatment of overactive bladder and irritable bowel syndrome, allowing for the investigation of β3-adrenergic signaling pathways in various biological contexts.

Items 3151-3200 of 5455

Page
per page
Set Descending Direction