outflow

BAY 73-1449 是前列环素受体选择性拮抗剂，在人 HEL 细胞和大鼠 DRG 的 cAMP 分析中具有很高的效价，IC50小于 0.1 nM。BAY 73-1449在降血压方面有研究的价值。

Verosudil (AR-12286) 是一种高效的 Rho 激酶 (ROCK) 抑制剂，对 ROCK1 和 ROCK2 的 Ki 分别为 2 和 2 nM。AR-12286 可逆转类固醇诱导的小鼠眼内压，可通过增加眼房水通过小梁网流出来减缓眼压。

Trazium esilate is an adrenergic receptor antagonist. Trazium esilate is a weak displacer on a1-, a2- and D2-receptors, however, it induced a2-receptor desenzitization after repeated treatment. It had no influence on rat brain cortical noradrenaline and s

δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a 40 mg/ml suspension is administered subconjunctivally. Formulations containing triamcinolone acetonide are used in the treatment of diabetic macular edema.

(E)-Guanabenz ((E)-Wy-8678) 是一种具有口服活性的中枢α2-肾上腺素受体 (α2-adrenoceptor)激动剂。(E)-Guanabenz 具有抗高血压活性，通过刺激中枢 α2- 肾上腺素受体，并减少交感神经向外周的净流出而起作用。(E)-Guanabenz z 也直接结合并抑制 GADD34，具有神经保护活性。(E)-Guanabenz 可用于研究高血压和帕金森病。

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and​/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg/kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

P-gb-IN-1 是一种有效的 P-糖蛋白 (P-gp) 抑制剂，通过抑制 P-gp 外流展现出逆转活性。P-gb-IN-1 通过与残基 Asn 721 和 Met 986 形成氢键相互作用从而显示出对 P-gp 的抑制作用。P-gb-IN-1 在 MCF-7/ADR 细胞中显示出低毒性。

Neuropeptide W-30 (human) 作为中枢神经系统的一种关键应激介质，它参与调节下丘脑-垂体-肾上腺 (HPA) 轴和交感系统的输出。作为两种孤儿G蛋白偶联受体 (GPCRs) GPR7和GPR8的内源性配体，Neuropeptide W-30 (human) 可在类似的有效浓度下激活并与GPR7和GPR8结合。

Neuropeptide W-30 (rat) 是一种重要的中枢神经系统应激介质，调节下丘脑-垂体-肾上腺 (HPA) 轴和交感输出。作为内源性配体，它与两种结构相关的孤儿 G 蛋白偶联受体 (GPCRs) GPR7 和 GPR8 结合并激活。