Membrane Transporters/Ion Channels
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TRPV1 antagonist
NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
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TRPV1 拮抗剂
SB-705498是有效,选择性和口服生物利用的TRPV1拮抗剂,抑制TRPV1的Capsaicin,酸和热激活,IC50分别为3 nM, 0.1 nM和6 nM,该作用具有一定的电压依赖性,作用于TRPV1比作用于TRPM8选择性高100倍以上。
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TRPV1 拮抗剂
AMG 517是有效的选择性TRPV1拮抗剂。
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- Jun Hai, .et al. Intragastric administration of AMG517, a TRPV1 antagonist, enhanced activity-dependent energy metabolism via capsaicin-sensitive sensory nerves in mice, Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Hai J, .et al. Differences in the effects of TRPV1 antagonists on energy metabolism in mice, Biomed Res, 2018, 39(6):279-286 PMID: 30531157
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TRPV1 receptor 拮抗剂
A-889425是选择性TRPV1受体拮抗剂。A-889425阻断TRPV1通道,IC50为335 nM(大鼠)和34 nM(人)。
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TRPV1 拮抗剂
Mavatrep是生物利用的TRPV1拮抗剂(Ki = 6.5 nM),对CYP亚型3A4、1A2和2D6的酶活性(IC50> 25μM)影响很小。
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TRPV1 receptor 拮抗剂
SB-366791是新颖,有效且选择性的肉桂酰胺TRPV1拮抗剂。
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TRPV1 antagonist
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
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TRPM8 拮抗剂
RQ-00203078是一种高度选择性,有效且可口服的TRPM8拮抗剂(大鼠和人类通道的IC50值分别为5.3和8.3 nM),对TRPM8的选择性是TRPV4,TRPV1和TRPA1的> 350倍。
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TRPM8 拮抗剂
AMG-333是有效的选择性TRPM8拮抗剂,IC50为13 nM。
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TRPM8 antagonist
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
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AMPA and Kainate 拮抗剂
GYKI-52466 dihydrochloride是选择性非竞争性AMPA受体拮抗剂(对于AMPA、红藻氨酸和AMPA诱导的反应,IC50值分别为10-20、~ 450和> > 50 μM)。
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AMPA Receptor 拮抗剂
NBQX是一种有效,选择性和竞争性的AMPA受体拮抗剂。
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NMDA receptor 拮抗剂
DNQX是一种非N-甲基-D-天冬氨酸(非NMDA)受体复合物拮抗剂。
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AMPA/kainate 拮抗剂
CNQX是一种竞争性的非NMDA谷氨酸受体拮抗剂(AMPA和海藻酸酯受体的IC50分别为0.3和1.5 uM,而NMDA受体的IC50 = 25 uM)。
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AMPA/kainate 拮抗剂
CNQX disodium salt,AMPA/海藻酸酯拮抗剂CNQX(GLXC-11053)的水溶性形式。
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AMPA 拮抗剂
GYKI53655 Hydrochloride是一种非竞争性AMPA和海藻酸酯受体拮抗剂。
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non-competitive AMPAR antagonist
CFM-2 is a selective non-competitive AMPAR antagonist.
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AMPA antagonist
Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
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AMPA 拮抗剂
Tezampanel是AMPA和离子型谷氨酸受体的海藻酸盐家族的拮抗剂,对海藻酸盐受体的GluR5亚型具有选择性。
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AMPA 拮抗剂
YM90K hydrochloride是一种选择性AMPA受体拮抗剂,在局部缺血后给药后,可延迟整体缺血模型中的神经元死亡和局部缺血模型中的脑梗塞。
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AMPA/kainate receptor 拮抗剂
Talampanel是AMPA受体的非竞争性拮抗剂,具有抗癫痫活性。
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AMPA 拮抗剂
CP 465022 hydrochloride是一种选择性的非竞争性AMPA拮抗剂,在大鼠皮质神经元中的IC50为25 nM,显示出有效的抗惊厥活性。
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AMPA receptor antagonist
SYM 2206 is a novel, potent, non-competitive AMPA receptor antagonist.
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AMPA/kainate antagonist
Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
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CP-AMPA receptors antagonist
Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
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AMPA/kainate antagonist
Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
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AMPAR antagonist
Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
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AMPA (CP-AMPA) receptors antagonist
Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
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KATP channel 拮抗剂
Mitiglinide calcium是一种降血糖药物,通过关闭胰腺β细胞中的ATP敏感K+通道来刺激胰岛素分泌。
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NMDA receptor 拮抗剂
Orphenadrine柠檬酸盐是NMDA受体拮抗剂,Ki为6.0μM,还是HERG钾离子通道阻断剂。
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Voltage-gated sodium channels 拮抗剂
Proparacaine HCl是一种电压门控钠通道拮抗剂,ED50为3.4 mM。
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Calcium channel antagonist
Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
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L-type calcium antagonist
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
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T-type Ca2+ channel antagonist
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
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T-type Ca2+ channel antagonist
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
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ATPase 拮抗剂
PF 3716556是H+,K+-ATPase酶抑制剂(在人类重组离子渗漏试验中PIC50 = 6)。
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