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35

Inhibitors & Agonists

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-A0014
    Ramelteon
    Maximum Cited Publications
    12 Publications Verification

    TAK-375

    Melatonin Receptor Neurological Disease Endocrinology Cancer
    Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
    Ramelteon
  • HY-B0696A

    NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride

    GABA Receptor Neurological Disease
    Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine hydrochloride
  • HY-136661

    L-Phenylisopropyladenosine; L-PIA; R-PIA

    Adenosine Receptor Cardiovascular Disease Neurological Disease
    (-)-N6-phenylisopropyl adenosine (L-Phenylisopropyladenosine) is a selective A1 adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K +-induced Ca 2+ uptake with an IC50 value of 0.5 µM. (-)-N6-phenylisopropyl adenosine protects against ischemia-induced ventricular arrhythmias and atrial fibrillation, and exacerbates ethanol withdrawal symptoms. (-)-N6-phenylisopropyl adenosine also has analgesic effects .
    (-)-N6-Phenylisopropyl adenosine
  • HY-B0696

    NO050328; NO328; TGB

    GABA Receptor Neurological Disease
    Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine
  • HY-100903

    nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride

    Opioid Receptor Neurological Disease
    Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
    Norbinaltorphimine dihydrochloride
  • HY-117040
    nor-Binaltorphimine
    5+ Cited Publications

    Norbinaltorphimine; NorBNI

    Opioid Receptor Neurological Disease
    nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
    nor-Binaltorphimine
  • HY-B0424
    Nitrendipine
    3 Publications Verification

    BAY-E-5009

    Calcium Channel Apoptosis Cardiovascular Disease Neurological Disease Cancer
    Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .
    Nitrendipine
  • HY-B1052

    Baq-168; MDL-14042

    Adrenergic Receptor Imidazoline Receptor Neurological Disease Metabolic Disease
    Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine hydrochloride
  • HY-A0142A

    Adrenergic Receptor Endocrinology
    Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .
    Dapiprazole hydrochloride
  • HY-104006

    Opioid Receptor Neurological Disease
    CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
    CYM51010
  • HY-B1052A

    Baq-168 free base; MDL-14042 free base

    Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .
    Lofexidine
  • HY-A0014S1

    TAK-375-d3

    Melatonin Receptor Others
    Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
    Ramelteon-d3
  • HY-A0014S

    TAK-375-d5

    Isotope-Labeled Compounds Melatonin Receptor Neurological Disease Endocrinology Cancer
    Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
    Ramelteon-d5
  • HY-B0424S

    AY-E-5009-d5

    Isotope-Labeled Compounds Calcium Channel Apoptosis Cardiovascular Disease Neurological Disease Cancer
    Nitrendipine-d5 is the deuterium labeled Nitrendipine (HY-B0424). Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .
    Nitrendipine-d5
  • HY-A0142

    Adrenergic Receptor Endocrinology
    Dapiprazole is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole suppresses the opioid withdrawal symptoms. Dapiprazole is also used as eye drops for reversing mydriasis .
    Dapiprazole
  • HY-B1052S

    Baq-168-d4; MDL-14042-d4

    Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine-d4 hydrochloride (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine-d4 hydrochloride
  • HY-B0424R

    BAY-E-5009 (Standard)

    Reference Standards Calcium Channel Apoptosis Cardiovascular Disease Neurological Disease Cancer
    Nitrendipine (Standard) is the analytical standard of Nitrendipine (HY-B0424). This product is intended for research and analytical applications. Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .
    Nitrendipine (Standard)
  • HY-144609

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 4
  • HY-144607

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 2
  • HY-B0696B

    NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate

    GABA Receptor Neurological Disease
    Tiagabine (NO050328; NO328; TGB) hydrochloride hydrate is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride hydrate exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride hydrate is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine hydrochloride hydrate
  • HY-144608

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 3
  • HY-A0014R

    TAK-375 (Standard)

    Reference Standards Melatonin Receptor Neurological Disease Endocrinology Cancer
    Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
    Ramelteon (Standard)
  • HY-A0142AR

    Adrenergic Receptor Reference Standards Endocrinology
    Dapiprazole (hydrochloride) (Standard) is the analytical standard of Dapiprazole (hydrochloride). This product is intended for research and analytical applications. Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .
    Dapiprazole hydrochloride (Standard)
  • HY-B1052R

    Baq-168 (Standard); MDL-14042 (Standard)

    Adrenergic Receptor Reference Standards Neurological Disease Metabolic Disease
    Lofexidine (Baq-168) hydrochloride Standard is the analytical standard of Lofexidine hydrochloride (HY-B1052). This product is intended for research and analytical applications. Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .
    Lofexidine hydrochloride (Standard)
  • HY-B1052S1

    Baq-168 free base-d4; MDL-14042 free base-d4

    Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    Lofexidine-d4 (Baq-168 free base-d4) is deuterium labeled Lofexidine (HY-B1052A). Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .
    Lofexidine-d4
  • HY-170437

    Opioid Receptor Neurological Disease
    MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
    MOR modulator-1
  • HY-B0696S

    NO050328-d6; NO328-d6; TGB-d6

    Isotope-Labeled Compounds GABA Receptor Neurological Disease
    Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine-d6
  • HY-B0696AS

    NO050328-d4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride

    Isotope-Labeled Compounds GABA Receptor Neurological Disease
    Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine-d4 hydrochloride
  • HY-B0696AR

    NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)

    Reference Standards GABA Receptor Neurological Disease
    Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine hydrochloride (Standard)
  • HY-181605

    Opioid Receptor Neurological Disease
    MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder .
    MOR antagonist 2 hydrochloride
  • HY-104006R

    Reference Standards Opioid Receptor Neurological Disease
    CYM51010 (Standard) is the analytical standard of CYM51010 (HY-104006). This product is intended for research and analytical applications. CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
    CYM51010 (Standard)
  • HY-100903R

    nor-Binaltorphimine dihydrochloride (Standard); nor-BNI dihydrochloride (Standard)

    Opioid Receptor Reference Standards Neurological Disease
    Norbinaltorphimine dihydrochloride (Standard) is the analytical standard of Norbinaltorphimine dihydrochloride (HY-100903). This product is intended for research and analytical applications. Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
    Norbinaltorphimine dihydrochloride (Standard)
  • HY-105628

    CI-427

    Others Neurological Disease Inflammation/Immunology
    Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
    Prodilidine
  • HY-158252S

    NO050328-d5 hydrochloride; NO328-d5 hydrochloride; TGB-d5 hydrochloride

    Isotope-Labeled Compounds GABA Receptor Neurological Disease
    Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine-d5 hydrochloride
  • HY-B0696S1

    NO050328-d4; NO328-d4; TGB-d4

    Isotope-Labeled Compounds GABA Receptor Neurological Disease
    Tiagabine-d4 (NO050328-d4) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
    Tiagabine-d4

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