cytosolic receptor

Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger, which is synthesized from NAD + by ADP-ribosyl cyclase. Cyclic ADP-ribose mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release

Fluticasone propionate (CCI-187881) 是一种选择性糖皮质激素受体激动剂，是一种局部抗炎激素，亲和力KD 为 0.5 nM。具有抗病毒活性。

Bicalutamide (ICI-176334) 是一种具有口服活性的非甾体雄激素受体拮抗剂，可研究前列腺癌。

Taltirelin acetate (TA-0910 acetate) 是促甲状腺激素释放激素受体(TRH-R)超激动剂(IC50:910 nM)，能够刺激细胞溶质Ca2+浓度增加 (Ca2+释放) ，其EC50值为 36 nM。

Pimecrolimus (SDZ-ASM 981) 是一种免疫亲和素配体，能与胞质受体特异性的结合。

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw. At concentrations as high as 30 μM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.

5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a powerful calcium mobilization second messenger synthesized from NAD+ by an ADP-ribosyl cyclase. It primarily raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum, while also facilitating extracellular influx through the opening of TRPM2 channels [1][2][3].

Bourgeonal is an agonist of human testicular olfactory receptor hOR17-4. It increases cytosolic calcium levels in human spermatozoa, acts as a chemoattractant, and increases swimming speed in sperm chemotaxis assays in a concentration-dependent manner.

Taltirelin (TA-0910) 是促甲状腺激素释放激素受体(TRH-R)超激动剂(IC50:910 nM)，能够刺激细胞溶质 Ca2+浓度增加 (Ca2+释放) (EC50:36 nM)。

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。

Taltirelin-13C-d3 是 Taltirelin 的 13C 和氘代化合物。Taltirelin 的 CAS 号为 103300-74-9。Taltirelin 是促甲状腺激素释放激素受体(TRH-R)超激动剂(IC50:910 nM)，能够刺激细胞溶质Ca2+浓度增加 (Ca2+释放) (EC50:36 nM)。

Variabilin, a novel inhibitor of human platelet aggregation, it is a potent RGD (Arg-Gly-Asp)-containing antagonist of the fibrinogen receptor glycoprotein IIb-IIIa (GPIIb-IIIa; αIIbβ3) and the vitronectin receptor αvβ3.Variabilin is also an antimicrobial furanosesterterpene. Variabilin is an inhibitor of human secretory and cytosolic phospholipase A2 (PLA2) activities that controls eicosanoid production in vitro and in vivo, inhibits neutrophil degranulation and superoxide generation in vitro and shows anti-inflammatory activity after topical or p.o. administration to mice.