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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
57 Results for "
presynaptic receptor
" in MedChemExpress (MCE) Product Catalog:
Products (57)
57 Results for "presynaptic receptor" 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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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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1 Cited Publications
Synonyms: α-Lobeline hydrochloride; L-Lobeline hydrochloride
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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 .
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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 .
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 .
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.
Synonyms: (S)-3,4-Dicarboxyphenylglycine
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(S)-3,4-DCPG ((S)-3,4-Dicarboxyphenylglycine) is a potent and selective mGlu8a receptor agonist with an EC50 of 31 nM for human mGlu8a. (S)-3,4-DCPG inhibits Forskolin (HY-15371)-stimulated cAMP formation by activating mGlu8, and modulates presynaptic glutamatergic transmission and synaptic plasticity. (S)-3,4-DCPG can be used in research on inflammatory pain, neuropathic pain, autism spectrum disorder, and glutamatergic synaptic plasticity .
Synonyms: KW-3902
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Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
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LY 165163 is a potent 5-HT presynaptic receptor agonist. LY 165163 significantly decreases 5-HTP accumulation and increases DOPA accumulation in the cortex and striatum .
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XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms .
Cat. No.: HY-W795507
CAS No.: 69906-85-0
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Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
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WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties .
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Cat. No.: HY-W052508S
CAS No.: 1189866-35-0
Synonyms: N-Desalkylquetiapine-d8
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S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety .
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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
