12
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14127 |
Adenosine A1 receptor activator T62
|
Adenosine Receptor | GPCR/G Protein; Neuroscience |
Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂,有镇痛作用。 | |||
TP1559L |
Ziconotide Acetate (107452-89-1 free base)
醋酸齐考诺肽,Prialt,Ziconotide Acetate |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂,已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用,因此通过有效的镇痛作用减少突触传递。 | |||
T41005 |
PA-8
|
PACAP | GPCR/G Protein |
PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂,有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化,但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。 | |||
T1787 |
Levobupivacaine
|
Sodium Channel | Membrane transporter/Ion channel |
Levobupivacaine 是一种氨基酰胺类局麻药,属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。 | |||
T3614 |
Inosine pranobex
Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun |
IL Receptor; HIV Protease | Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Inosine pranobex (Delimmun) 是一种免疫增强剂,它是一种广谱抗病毒剂,用于 HIV 感染。 | |||
T71356 |
Lanperisone HCl
|
||
Lanperisone, also known as NK433, is a muscle relaxant. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spina... | |||
T68592 |
Mafosfamide sodium
|
||
Mafosfamide sodium is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide sodium alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, Mafosfamide sodium, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, Mafosfamide sodium is potentially useful in the intrathecal treatment of neoplastic meningitis. | |||
T68434 |
Mafosfamide
|
||
Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, mafosfamide, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, mafosfamide is potentially useful in the intrathecal treatment of neoplastic meningitis. | |||
T37127 |
L-AP4 monohydrate
L-AP4 monohydrate |
||
L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio... | |||
T83739 |
Myr-Tat-CBD3 TFA
Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3 |
||
Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下,该化合物能够约81%地抑制Cav2.2-CRMP2相互作用,并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入(IC50约为2.8 µM)。在20 µM的浓度下,Myr-Tat-CBD3能抑制钙电流,但不影响钠电流,在初级DRG神经元中表现出这种特性。经过脊髓内给药,myr-Tat-CBD3(20 µg/5 µl)能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外,Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。 | |||
T83674 |
K 41498 TFA
|
||
K 41498 是一种针对皮质酮释放因子受体2α(CRF2α)和CRF2β的肽拮抗剂,其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性,与CRF1相比(在表达人类受体的HEK293细胞中Ki值为425 nM)。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药,K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。 | |||
T83731 |
Tat-CBD3 TFA
|
||
Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中,Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%,并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流,并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S0581 |
Sec-O-Glucosylhamaudol
亥茅酚苷,Hamaudol 3-glucoside |
Others; Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others |
Sec-O-Glucosylhamaudol (Hamaudol 3-glucoside) 是从滨海前胡中分离得到的一种天然产物,能够降低 μ 阿片受体的蛋白水平,可用于缓解疼痛的研究。它通过调节脂多糖刺激的 RAW264.7 细胞系中的 p38 丝裂原活化蛋白激酶具有抗炎作用。 |