antihypertensive effect

Urapidil hydrochloride (Urapidil HCl) is 5-HT1A receptor agonist and an α1-adrenoceptor antagonist.

Dixyrazine (UCB 3412)has a transient antihypertensive effect, prevents cerebral edema induced by injections of ichthyosperm sulfate, and may be used in the study of neurologically related disorders.

N,N'-Dicyclohexylurea (AURORA KA-3582) is a soluble epoxide hydrolase (sEH) inhibitor.

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

Alacepril (DU-1219) is a relatively novel angiotensin-converting enzyme inhibitor, used as an antihypertensive

Nanofin (Lupetidine) is a neuropathic blocker, with antihypertensive effect.

(R)-SCH 42495, the less active enantiomer of SCH 42495, is an orally active inhibitor of neutral metalloendopeptidase (NEP) with antihypertensive effects.

SCH 42495 racemate is the racemate of SCH 42495, an orally active neutral inhibitor of metalloendopeptidase (NEP) with antihypertensive effects.

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent. It exhibits inhibitory effects on angiotensin II receptors with IC50 values of 9.2 nM in rat adrenocortical membranes and 3.9 nM in human adrenocortical membranes.

A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8

Fenquizone (M.G. 13054), a thiazide-like diuretic, exhibits chronic antihypertensive effect. Fenquizone can be used for the research of oedema and hypertension.

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.

Trichlormethiazide sodium is an orally active thiazide diuretic with antihypertensive effects. In an acute renal failure rats model, it increases urine volume (UV), Na and K excretion, and tends to improve creatinine clearance (CCRE).

Azilsartan medoxomil potassium (QR-01019K), an angiotensin II receptor antagonist, exhibits a potent and sustained antihypertensive effect, along with a more pronounced and enduring reduction in heart rate, and a high safety profile. It shows promise for investigation in the management of hypertension, chronic heart failure, and diabetic nephropathy[1].

Isomartynoside has inhibition against the angiotensin converting enzyme (ACE) activities, the IC 50 value is 505±26.7μg ml, it may have antihypertensive effect. Isomartynoside also shows obvious anti-fatigue activity.

Serpentinine may have antihypertensive effect.