spontaneously. hypertensive

Hexamethonium Bromide (Hexamethonium Dibromide) 是神经节中神经元型烟碱型 AChR 的特异性拮抗剂。在自发性高血压动物模型中，它能降低其交感神经活动和血压。

BMY 7378 dihydrochloride (BMY7378 HCl) 是选择性 α1D 肾上腺素受体拮抗剂，也是5-HT1A 受体部分激动剂。它同表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM)  是同克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 的100 以上。

CGP48369 是一种有效的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂，具有降血压作用，可增强自发性高血压大鼠冠状动脉的内皮依赖性松弛。

N,N'-Dicyclohexylurea (AURORA KA-3582) 是一种可溶性环氧化物水解酶 (sEH) 抑制剂。

Tempone 是一种氨基氧烷，具有自由基清除剂的作用，会与活性氧（ROS）发生反应。静脉注射 Tempone 可降低自发性高血压大鼠的平均动脉。

AVE3085 是内皮一氧化氮合酶的增强剂，可恢复自发性高血压大鼠的内皮功能并降低血压，可用于研究心血管疾病。

Phenidone (1-phenyl-3-pyrazolidinone) 是可口服发环氧化酶和脂氧合酶双重抑制剂，可改善实验性自身免疫性脑脊髓炎大鼠的瘫痪，降低自发性高血压大鼠的血压，可用作照片显像剂。

KRH-594 is a potent, specific and insurmountable AT1 receptor antagonist. KRH-594 ameliorates hyperlipidaemia and nephropathy in diabetic spontaneously hypertensive rats. KRH-594 prevents end-organ damage in stroke-prone spontaneously hypertensive Izm ra

Milfasartan is a potent, selective antagonist of AT1 receptor with oral activity. It markedly lowers the blood-pressure in conscious renal and spontaneously hypertensive rats.

Methylspinazarin is a naphthoquinone bacterial metabolite that has been found in Streptomyces and is an inhibitor of catechol O-methyltransferase (COMT; IC50 = 0.8 μg ml).1 It is selective for COMT over tyrosine hydroxylase, DOPA decarboxylase, and dopamine-β-hydroxylase at 100 μg ml. Methylspinazarin decreases blood pressure in spontaneously hypertensive rats when administered at a dose of 50 mg kg. |1. Chimura, H., Sawa, T., Takita, T., et al. Methylspinazarin and dihydromethylspinazarin, gatechol-O-methyl transerfase inhibitors produced by Streptomyces. J. Antibiot. 26(2), 112-114 (1973).

Adrenomedullin (13-52) is a truncated form of adrenomedullin (1-52) . It induces nitric oxide-dependent relaxation of and inhibits release of angiotensin II and endothelin-1 from isolated rat aorta. In vivo, adrenomedullin (13-52) decreases mean arterial pressure (MAP) in spontaneously and renal hypertensive rats in a dose-dependent manner. Adrenomedullin (13-52) (10-3,000 ng per animal) reverses increases in lobar arterial pressure induced by U-46619 in a dose-dependent manner in cats but has no effect on basal lobar arterial pressure or systemic arterial pressure. It also potentiates inflammatory edema and neutrophil accumulation in rats.

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)

Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods.

(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC 50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..

Trandolapril 是 Trandolaprilat 的前体药物。Trandolapril 是一种口服血管紧张素转换酶抑制剂，在高血压和充血性心力衰竭及心肌梗死领域有研究价值。

EP3 antagonist 3是一种有效和选择性的EP3拮抗剂，具有口服活性的优点，在自发性高血压大鼠（SHR）中显著抑制了GR63799或乙酸诱导的膀胱容量降低和PGE2诱导的过度活跃膀胱模型。

HS56 是一种 ATP 竞争性 Pim DAPK3双重抑制剂，对 DAPK3、Pim-3、Pim-1和 Pim-2 的 Ki 值分别为 0.26、0.208、2.94 和 ＞100 μM。 HS56 抑制 LC20 磷酸化和平滑肌收缩。HS56 降低自发性高血压小鼠的血压。HS56可用于高血压研究。

Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg kg per day) reduces blood pressure in spontaneously hypertensive rats.1 It also reduces infarct volume in a rat model of focal cerebral ischemia when used at a concentration of 0.01 mg kg.

Quinapril-d5 is intended for use as an internal standard for the quantification of quinapril by GC- or LC-MS. Quinapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor quinaprilat. In vivo, quinapril reduces mean arterial pressure in renal hypertensive and spontaneously hypertensive rats. It inhibits angiotensin I-induced pressor responses in normotensive rats and dogs. Quinapril prevents left ventricular heart failure in CHF 14.6 cardiomyopathic hamsters. Formulations containing quinapril have been used in the treatment of hypertension, heart failure, and diabetic nephropathy.

Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium. It inhibits decreases in renal cortex SIRT1 activity and increases in NADPH oxidase-dependent reactive oxygen species (ROS) production, as well as reduces kidney hypertrophy and albuminuria in a spontaneously hypertensive rat model of streptozotocin-induced diabetes when administered at a dose of 5 mg kg per day.3 Theobromine is toxic to dogs with an LD50 value of 250 to 500 mg kg.

BAY-747 (BAY 1165747) 为一种通过口服生效且具有脑渗透性的sGC刺激剂。它能可逆地逆转L-NAME所诱导的记忆障碍并在大鼠中增强认知功能。BAY-747还可在有意识状态下降低正常血压及自发性高血压大鼠(SHR)的血压。此外，BAY-747在mdx mTRG2小鼠模型中改善了与Duchenne肌营养不良症(DMD)相关的骨骼肌功能。

Antihypertensive agent 3 (compound 4a) 是一种针对血管紧张素 II 受体 1(AT1) 的拮抗剂，其在自发性高血压大鼠(SHRs)的模型中表现出显著的降压效果。

R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。

Urocortin II, a neuropeptide hormone within the corticotropin-releasing factor (CRF) family—which comprises mammalian CRF, urocortin I, urocortin III, frog sauvagine, and piscine urotensin I—displays 34, 43, and 37-40% sequence homology with rat and human CRF, human urocortin I, and human urocortin III, respectively. This compound enhances rabbit ventricular myocyte shortening and relaxation in both a time- and concentration-dependent manner. In vivo studies reveal that urocortin II lowers arterial blood pressure in both normotensive and spontaneously hypertensive rats through peripheral CRF2 receptor agonism, inducing dose-dependent tachycardia and hypotension at doses of 3 and 30 pmol/kg. Additionally, it mitigates the visceral pain response to colorectal distension at 10 and 20 μg/kg in conscious rats and delays gastric emptying in mice.