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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
121 Results for "
presynaptic
" in MedChemExpress (MCE) Product Catalog:
Products (121)
121 Results for "presynaptic" in MCE Product Catalog:
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Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist with blood-brain barrier permeability. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
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13 Publications Verification
Cat. No.: HY-B0007C
CAS No.: 28311-31-1
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Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .
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Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
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7 Cited Publications
Cat. No.: HY-110032
CAS No.: 113170-86-8
Synonyms: LTG isethionate; BW430C isethionate
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Lamotrigine (BW430C) isethionate is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine isethionate selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine isethionate can be used for the research of epilepsy, focal seizure, et al .
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5 Cited Publications
Synonyms: Disodium clodronate tetrahydrate
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Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
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3 Cited Publications
Cat. No.: HY-W247131
CAS No.: 3785-01-1
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Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
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2 Cited Publications
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GV-58 is a novel N- and P/Q-type calcium (Ca 2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca 2+ entry during activity. GV-58 can be used in lambert-eaton myasthenic syndrome (LEMS) research .
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Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
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1 Cited Publications
Synonyms: α-Lobeline hydrochloride; L-Lobeline hydrochloride
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1 Cited Publications
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LY310762 is a selective 5-HT1D receptor antagonist with a Ki value of 249 nM for the guinea pig receptor. LY310762 blocks presynaptic 5-HT1D autoreceptors and enhances potassium-stimulated [ 3H]5-HT outflow from guinea pig cortical slices. LY310762 abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT1D receptors. LY310762 potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 is used in research related to depression and diabetic nephropathy .
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1 Cited Publications
Cat. No.: HY-W040555
CAS No.: 111974-74-4
Synonyms: N-Desalkylquetiapine dihydrochloride
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Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation .
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Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .
Category:
Infection Microorganisms Antibiotics Disease Research Antibacterial Disease Research Fields Other Antibiotics
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Cat. No.: HY-17637
CAS No.: 313368-91-1
Synonyms: ITI-007
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Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
Cat. No.: HY-19733
CAS No.: 1187020-80-9
Synonyms: ITI-007 tosylate
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Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .
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Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space .
Synonyms: NLX-112; F13640
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Befiradol (NLX-112) is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol attenuates sedative agent-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of sedative agent-induced analgesia and sedation in adult rats. Befiradol can be used in studies related to opioid-induced respiratory depression .
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MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
