Search Result
Results for "
dorsal
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W013712
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Potassium Channel
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Neurological Disease
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GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
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- HY-155017
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Sodium Channel
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Neurological Disease
Cancer
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6-Iodoamiloride is a potent acid-sensing ion channel 1 (ASIC1) inhibitor with an IC50 of 88 nM. 6-Iodoamiloride inhibits ASIC3-mediated currents from rat dorsal root ganglion neurons with an IC50 of 230 nM .
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- HY-P1134
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5-HT Receptor
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Neurological Disease
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Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
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- HY-108425
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Sodium Channel
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Neurological Disease
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AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
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- HY-19432
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iGluR
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Neurological Disease
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UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 .
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- HY-107037
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RX71107
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Vasopressin Receptor
Angiotensin Receptor
Adrenergic Receptor
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Cardiovascular Disease
|
Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina .
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- HY-130358
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Calcium Channel
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Neurological Disease
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PDDHV is a calcium absorption inducer and may achieve 45Ca 2+ influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
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- HY-123708
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Galectin
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Others
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SNAP 398299 is a Gal3 receptor antagonist with potential anxiolytic and antidepressant effects. SNAP 398299 can partially reverse the neuropeptide Galanin-induced inhibition of dorsal raphe cell firing and the Galanin-induced hyperpolarizing current.
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- HY-P10029
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Serotonin Transporter
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Neurological Disease
|
Sakura-6 is a SERT-nnos interaction promoter that significantly increases the SERT-nnos complex, but reduces the level of SERT on the cell surface. Acute injection of Sakura-6 into the dorsal raphe nucleus (DRN) causes depression-like behavior in mice .
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- HY-P5179
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HWTX-I
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Calcium Channel
Sodium Channel
|
Neurological Disease
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively .
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- HY-P5773
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Sodium Channel
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Neurological Disease
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Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC50 of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons .
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- HY-P5180
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Sodium Channel
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Neurological Disease
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Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
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- HY-N0145
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- HY-P5868
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Sodium Channel
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Neurological Disease
|
mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC50 of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages .
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- HY-P3679
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Neuropeptide Y Receptor
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Neurological Disease
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Neuropeptide Y (1-24) (human) is a neuropeptide with potencies in inhibiting the electricity stimulated twitch response of rat vas deferens. Neuropeptide Y (1-24) (human) stimulates N-methyl-D-aspartate (NMDA)-induced neuronal activation in the rat CA3 region of the dorsal hippocampus in vivo .
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- HY-108671
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P2X Receptor
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Neurological Disease
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NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons .
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- HY-P1422
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Spadin
1 Publications Verification
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .
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- HY-121122
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TRP Channel
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Others
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A778317 is a TRPV1 antagonists. A778317 can block changes in intracellular calcium levels mediated by TRPV1 receptors, with a pIC50 value of 8.31. A-778317 can also block the activation of natural rat TRPV1 receptors in dorsal root ganglion neurons by capsaicin and acid .
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- HY-P1422A
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Potassium Channel
5-HT Receptor
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Neurological Disease
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Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .
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- HY-148417
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Serotonin Transporter
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Neurological Disease
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ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD) .
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- HY-P5770
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Sodium Channel
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Neurological Disease
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Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC50 of 604.2 nM) .
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- HY-118504
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nAChR
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Neurological Disease
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Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens .
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- HY-118504R
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nAChR
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Neurological Disease
|
Sulfoxaflor (Standard) is the analytical standard of Sulfoxaflor. This product is intended for research and analytical applications. Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens .
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- HY-N6825
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- HY-N6825R
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TRP Channel
Endogenous Metabolite
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Neurological Disease
|
Hydroxy-α-sanshool (Standard) is the analytical standard of Hydroxy-α-sanshool. This product is intended for research and analytical applications. Hydroxy-α-sanshool is a transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50s of 69 and 1.1 μM, respectively. Hydroxy-α-sanshool can be used for pain research .
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- HY-121119
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Adenosine Receptor
Calcium Channel
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .
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- HY-W014421
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|
TRP Channel
|
Neurological Disease
|
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
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- HY-N9506
-
|
GABA Receptor
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Neurological Disease
|
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM .
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- HY-P3071
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Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
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- HY-19858
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iGluR
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Neurological Disease
|
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
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- HY-P10358
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Calcium Channel
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Neurological Disease
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TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-P3162
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- HY-108425B
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(Rac)-AMG8380
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Sodium Channel
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Neurological Disease
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(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
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- HY-P3162A
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- HY-108576
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DuP 996 dihydrochloride
|
TRP Channel
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Neurological Disease
|
Linopirdine dihydrochloride is a agonist of capsaicin receptor TRPV1. Linopirdine increases the intracellular calcium concentration in HEK293 cells. Linopirdine dihydrochloride exerts an excitatory action on mammalian nociceptors .
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- HY-N6789
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KT5720
3 Publications Verification
|
PKA
|
Neurological Disease
Cancer
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
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- HY-103430
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Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
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Neurological Disease
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SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation .
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- HY-100057
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6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215
|
5-HT Receptor
Drug Metabolite
Dopamine Receptor
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Neurological Disease
|
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
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- HY-168758
-
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GABA Receptor
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Neurological Disease
|
Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
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- HY-103430A
-
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation .
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-
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- HY-162872
-
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CRFR
|
Neurological Disease
|
NBI-35965 is an antagonist of corticotropin-releasing factor receptor 1 (CRF-R1). NBI-35965 can be used in nervous system related research .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1422
-
Spadin
1 Publications Verification
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .
|
-
- HY-P1422A
-
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .
|
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- HY-P1134
-
|
5-HT Receptor
|
Neurological Disease
|
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
|
-
- HY-P10029
-
|
Serotonin Transporter
|
Neurological Disease
|
Sakura-6 is a SERT-nnos interaction promoter that significantly increases the SERT-nnos complex, but reduces the level of SERT on the cell surface. Acute injection of Sakura-6 into the dorsal raphe nucleus (DRN) causes depression-like behavior in mice .
|
-
- HY-P5179
-
HWTX-I
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively .
|
-
- HY-P5773
-
|
Sodium Channel
|
Neurological Disease
|
Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC50 of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons .
|
-
- HY-P5180
-
|
Sodium Channel
|
Neurological Disease
|
Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
|
-
- HY-P5868
-
|
Sodium Channel
|
Neurological Disease
|
mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC50 of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages .
|
-
- HY-P3679
-
|
Neuropeptide Y Receptor
|
Neurological Disease
|
Neuropeptide Y (1-24) (human) is a neuropeptide with potencies in inhibiting the electricity stimulated twitch response of rat vas deferens. Neuropeptide Y (1-24) (human) stimulates N-methyl-D-aspartate (NMDA)-induced neuronal activation in the rat CA3 region of the dorsal hippocampus in vivo .
|
-
- HY-P5770
-
|
Sodium Channel
|
Neurological Disease
|
Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC50 of 604.2 nM) .
|
-
- HY-P3071
-
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
|
-
- HY-P10358
-
|
Calcium Channel
|
Neurological Disease
|
TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
|
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- HY-P3162
-
-
- HY-P3162A
-
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