Search Result
Results for "
sedation
" in MedChemExpress (MCE) Product Catalog:
9
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0649
-
-
-
- HY-17034A
-
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(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Infection
Cancer
|
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Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
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-
-
- HY-12719
-
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(+)-Medetomidine; (S)-Medetomidine
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
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Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .
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-
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- HY-N0528
-
-
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- HY-17416
-
|
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Adrenergic Receptor
|
Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
|
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Guanfacine hydrochloride is an orally active and blood-brain barrier permeability noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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-
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- HY-B1240
-
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Dehydrobenzperidol
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Dopamine Receptor
GABA Receptor
nAChR
|
Neurological Disease
|
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Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
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- HY-17416A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
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Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
|
-
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- HY-13575
-
-
-
- HY-12752A
-
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Trimeprazine hemitartrate
|
Histamine Receptor
Influenza Virus
|
Neurological Disease
Inflammation/Immunology
Cancer
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Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice .
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- HY-113413
-
|
Imidazolyl-4-acetic acid
|
Endogenous Metabolite
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
|
-
-
- HY-B1470
-
|
R-1929
|
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent .
|
-
-
- HY-N7126
-
|
|
Environmental Pollutants
Potassium Channel
|
Neurological Disease
|
|
Citronellal is a monoterpene that can be found in the essential oils in various aromatic species of plants, with antiinflammatory and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K+ channel pathway. Citronellal induces reduction of spontaneuous activity, ataxia, analgesia, and sedation in vivo. Citronellal can attenuate mechanical nociception response in mouse model .
|
-
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- HY-14785
-
|
NLX-112; F13640
|
5-HT Receptor
|
Neurological Disease
|
|
Befiradol (NLX-112) is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol can be used in studies related to opioid-induced respiratory depression .
|
-
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- HY-16728
-
|
GLYX-13
|
iGluR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma .
|
-
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- HY-113346
-
|
Tetrahydro-11-deoxycorticosterone
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
|
-
-
- HY-U00051
-
|
|
Histamine Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Propiomazine is an orally active antihistamine agent. Propiomazine is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia .
|
-
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- HY-16728B
-
|
GLYX-13 Trifluoroacetate
|
iGluR
mTOR
ERK
|
Neurological Disease
|
|
Rapastinel (GLYX-13) Trifluoroacetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel Trifluoroacetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel Trifluoroacetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel Trifluoroacetate is applicable to the research of major depressive disorder and hepatocellular carcinoma .
|
-
-
- HY-12719R
-
|
(+)-Medetomidine (Standard); (S)-Medetomidine (Standard)
|
Reference Standards
Adrenergic Receptor
|
Neurological Disease
Cancer
|
|
Dexmedetomidine (Standard) is the analytical standard of Dexmedetomidine. This product is intended for research and analytical applications. Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
-
- HY-N15001
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Gabaculine is an amino acid neurotoxin and blood-brain barrier-permeable GABA transaminase inhibitor, with an IC50 of 1 μM in beef and Pseudomonas ovalis. Gabaculine elevates endogenous synaptic and brain GABA levels and enhances GABA activity. Gabaculine induces sedation, hypothermia, loss of righting reflex, and prevents convulsions in mice. Gabaculine is applicable to research related to neurological disorders .
|
-
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- HY-17034AR
-
|
(+)-Medetomidine hydrochloride (Standard); (S)-Medetomidine hydrochloride (Standard)
|
Reference Standards
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
-
- HY-14196
-
|
MD 69276
|
Monoamine Oxidase
|
Neurological Disease
|
|
Toloxatone (MD 69276) is a reversible, selective MAO-A inhibitor that can cross the blood-brain barrier. Toloxatone increases the levels of serotonin (5-HT) and norepinephrine in the brain. Toloxatone reduces the immobility time in the forced swimming test in mice, inhibits killing behavior in rats without causing sedation, and shows a correlation between its free plasma concentration and cerebrospinal fluid concentration. Toloxatone is widely used in research related to depression, depressive disorders and Parkinson's disease .
|
-
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- HY-119456A
-
-
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- HY-19057
-
|
MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
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-
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- HY-148146
-
-
-
- HY-B0649R
-
|
2,6-Diisopropylphenol (Standard)
|
Reference Standards
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
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- HY-119456
-
-
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- HY-W749797
-
|
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GABA Receptor
|
Neurological Disease
|
|
Nitrazolam is a benzodiazepine compound, that may exhibit CNS depressant properties as traditional benzodiazepines, including sedation, hypnosis, anxiolysis, and anticonvulsant effects, by acting on GABA receptors .
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-
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- HY-17416R
-
|
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Guanfacine (hydrochloride) (Standard) is the analytical standard of Guanfacine (hydrochloride). This product is intended for research and analytical applications. Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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-
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- HY-B1470S
-
|
R-1929-d4
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Azaperone-d4 (R-1929-d4) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.
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- HY-16505
-
|
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Endogenous Metabolite
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Neurological Disease
|
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Triclofos sodium is a drug used to suppress insomnia and for sedation and has sedative activity. Triclofos sodium is used in children for sedation during painless medical procedures, particularly in children with neurocognitive disorders. Triclofos sodium has similar physiological and pharmacological properties to chloral and therefore can be used as a substitute when necessary. The safety and efficacy of Triclofos sodium have been demonstrated in pediatric populations with high rates of neurocognitive disorders .
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- HY-N0528R
-
-
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- HY-14785A
-
|
NLX-112 hydrochloride; F 13640 hydrochloride
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Befiradol (NLX-112) hydrochloride is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression .
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- HY-17034AS
-
|
(+)-Medetomidine-13C,d3 hydrochloride; (S)-Medetomidine-13C,d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
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- HY-17416AS
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
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Guanfacine- 13C, 15N3 is the 13C and 15N labeled Guanfacine . Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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-
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- HY-19266
-
-
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- HY-13575R
-
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AD-5423 (Standard)
|
Reference Standards
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Sigma Receptor
|
Neurological Disease
|
|
Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension .
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- HY-103496
-
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GABA Receptor
|
Neurological Disease
|
|
U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .
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- HY-17416S2
-
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Adrenergic Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
Endocrinology
|
|
Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
|
-
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- HY-17416AS1
-
|
|
Adrenergic Receptor
Isotope-Labeled Compounds
|
Neurological Disease
Endocrinology
|
|
Guanfacine- 15N3, 13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
|
-
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- HY-117257
-
-
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- HY-B1470R
-
|
R-1929 (Standard)
|
Reference Standards
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Azaperone (R-1929) (Standard) is the analytical standard of Azaperone (HY-B1470). This product is intended for research and analytical applications. Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.
|
-
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- HY-19006
-
|
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GABA Receptor
|
Neurological Disease
|
|
ZK-91296 is a GABA receptor agonist with anxiolytic activity. ZK-91296 can reduce anxiety in animals without causing sedation. ZK-91296 may have pharmacological selectivity for interaction with specific types of benzodiazepine receptors .
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- HY-106820
-
|
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Dopamine Receptor
|
Neurological Disease
|
|
BRL 34778 is a potent, selective and orally active dopamine D2 receptor antagonist with a Ki of 2.14 nM. BRL 34778 exhibits antipsychotic activity with low activity for extrapyramidal effects and sedation. BRL 34778 can be used for the research of neurological disease, such as schizophrenia .
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-
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- HY-167865
-
-
-
- HY-13575A
-
-
-
- HY-W707528
-
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2,6-Diisopropylphenol-d14
|
Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
|
-
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- HY-U00051A
-
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Histamine Receptor
|
Neurological Disease
|
|
Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia .
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-
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- HY-U00051AS1
-
|
|
Isotope-Labeled Compounds
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Neurological Disease
|
|
(R)-Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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- HY-U00051AS
-
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Isotope-Labeled Compounds
Histamine Receptor
|
Neurological Disease
|
|
Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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-
-
- HY-U00051AS2
-
|
|
Isotope-Labeled Compounds
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Neurological Disease
|
|
(S)-Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
|
-
- HY-N7126R
-
|
|
Reference Standards
Potassium Channel
|
Neurological Disease
|
|
Citronellal (Standard) is the analytical standard of Citronellal. This product is intended for research and analytical applications.Citronellal is a monoterpene that can be found in the essential oils in various aromatic species of plants, with antiinflammatory and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K+ channel pathway. Citronellal induces reduction of spontaneuous activity, ataxia, analgesia, and sedation in vivo. Citronellal can attenuate mechanical nociception response in mouse model .
|
-
- HY-113413R
-
|
Imidazolyl-4-acetic acid (Standard)
|
Reference Standards
Endogenous Metabolite
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
|
-
- HY-123525
-
|
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GABA Receptor
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Neurological Disease
|
|
COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
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- HY-159924
-
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Opioid Receptor
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Neurological Disease
|
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DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .
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- HY-16728A
-
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GLYX-13 acetate
|
iGluR
mTOR
ERK
|
Neurological Disease
|
|
Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma .
|
-
- HY-111136
-
|
|
GABA Receptor
5-HT Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
|
|
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
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-
- HY-105881
-
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Biglumide; K 2004
|
Others
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Neurological Disease
|
|
Taglutimide (Biglumide; K 2004) is an orally active hypnotic agent. Taglutimide lowers plasma levels of diphenhydramine in rats and shortens the duration of anesthesia. Taglutimide is used in research on neurological disorders such as sedation and hypnosis .
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-
- HY-115359
-
-
- HY-U00051B
-
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Histamine Receptor
Dopamine Receptor
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Neurological Disease
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Propiomazine maleate is an orally active antihistamine agent. Propiomazine maleate is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine maleate is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia .
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- HY-15080
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LY 293606
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iGluR
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Cardiovascular Disease
Neurological Disease
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GYKI 53405 is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia .
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- HY-181878
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Z7149
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Serotonin Transporter
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .
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Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1470S
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Azaperone-d4 (R-1929-d4) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.
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- HY-17034AS
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Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
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- HY-17416AS
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Guanfacine- 13C, 15N3 is the 13C and 15N labeled Guanfacine . Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-17416S2
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Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-17416AS1
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Guanfacine- 15N3, 13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-W707528
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Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
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- HY-U00051AS1
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(R)-Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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- HY-U00051AS
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Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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- HY-U00051AS2
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(S)-Propiomazine-d6 hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.
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