hypertensive

Anti-hypertensive sulfonanilide 1 is an antihypertensive compound.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker. The mechanism of action of irbesartan is as an Angiotensin 2 Receptor Antagonist.

LY 272015 hydrochloride is an orally active and selective 5-HT2B receptor antagonist that displays antihypertensive effects in DOCA-salt hypertensive rats.LY 272015 hydrochloride inhibits 5-HT- or BW723C86-induced ERK2 phosphorylation and attenuates MVIC and Tissue downstream cellular effects of 5HT signaling and can be used to study hepatocellular carcinoma.

Liensinine Diperchlorate is an isoquinoline alkaloid extracted from the embryonic seeds of the sacred lotus. It inhibits late autophagy by blocking autophagosome-lysosome fusion and exhibits biological activities such as anti-arrhythmic, anti-hypertensive, anti-pulmonary fibrosis, and vascular smooth muscle relaxation.

Antihypertensive sulfonanilide XVII is an orally available antihypertensive sulfonanilide small molecule compound for the study of hypertension.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist that shows antihypertensive and antiplatelet aggregation activity in hypertensive rats.

Alamandine TFA , a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine TFA targets to protect the kidney and heart through anti-hypertensive actions[1][2].

Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting hypotensive action was observed in various experimental hypertensive models.

ME-3221 is an angiotensin AT1 receptor antagonist that prevents hypertensive complications in aged stroke-prone hypertensive rats.

BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.

Antihypertensive agent 3 (compound 4a), an angiotensin II receptor 1 antagonist, demonstrates antihypertensive activity in spontaneously hypertensive rats (SHRs) [1].

Antihypertensive agent 2 (Compound 4g) exhibits effective antagonistic activities against angiotensin II receptor 1 and reduces blood pressure with equal or greater potency than Losartan [1].

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

1. Vitexin has antinociceptive and antispasmodic activities. 2. Vitexin exhibits a prominent first-pass effect. 3. Vitexin has antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. 4. Vitexin can either inhibit or induce activities of

Neuromedin U-25 (porcine) is a peptide known for its uterotonic and hypertensive properties [1].

3alpha-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats.

L-159282 is an orally active and nonpeptide angiotensin II receptor antagonist. It also has anti-hypertensive activity.

Endogenous melanocortin MC3 receptor agonist (pKi = 7.46) that displays ~ 40-fold selectivity over MC4. Increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. Exhibits hypertensive, tachycardic and

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

O-Des[2-aminoethyl]-O-carboxymethyl dehydroamlodipine is a major metabolite of the calcium channel inhibitor amlodipine .1 1.Taguchi, R., Naito, T., Sato, H., et al.Validated LC-MS/MS method for the simultaneous determination of amlodipine and its major metabolites in human plasma of hypertensive patientsTher. Drug Monit.39(6)625-631(2017)

Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.

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.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

BIBS-222, a nonpeptide angiotensin II (Ang II) receptor antagonist, appears to be an effective antihypertensive in the model of the renal hypertensive rat.

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.

Isoproterenol-d7 is intended for use as an internal standard for the quantification of isoproterenol by GC- or LC-MS. Isoproterenol is an agonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 224 and 458 nM, respectively). It is selective for β1- and β2-ARs over β3-ARs (Ki = 1,570 nM). Isoproterenol inhibits contractions in isolated field-stimulated rat vas deferens (EC50 = 45.6 nM). In vivo, isoproterenol (0.33 mg/kg) decreases blood pressure and increases water intake in nephrectomized rats. It reduces blood pressure and increases heart rate in renal hypertensive rabbits. Isoproterenol inhibits histamine-induced bronchospasms in anesthetized dogs. Formulations containing isoproterenol have been used in the treatment of bradydysrhythmias and to improve breathing during anesthesia.

AD011 is a dual cACE/NEP inhibitor. AD011 was synthesized via the previously reported C-domain selective ACE inhibitor lenopril-tryptophan. AD011 shows potential to provide potent anti-hypertensive and cardioprotective effects.

BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor. With Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 shows hypertensive effects[1].

Guanadrel is an antihypertensive agent.

Hydroflumethiazide is a thiazide diuretic. It has also shown the activity of anti-hypertensive.

AE0047 Hydrochloride is a blocker of calcium, and used in the research of the hypertensive disease.

BAY-747 (BAY 1165747) is an orally administered, brain-penetrant compound that stimulates soluble guanylate cyclase (sGC). It effectively counteracts memory impairments induced by L-NAME and improves cognitive performance in rats during the object location task (OLT). Additionally, BAY-747 reduces blood pressure in conscious normotensive and spontaneously hypertensive rats (SHR) and enhances skeletal muscle function in the mdx/mTRG2 mouse model of Duchenne muscular dystrophy (DMD) [1] [2] [3].

Endothelin-1 (1-31) (Human) acetate, a potent vasoconstrictor and hypertensive agent, is produced through the selective hydrolysis of big ET-1 by chymase [1].

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

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)

Hexamethonium Bromide (Hexamethonium Dibromide), a specific antagonist of neuronal-type nicotinic AChR in ganglia, is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier.

High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc

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.

Tritylolmesartan medoxomil is an intermediate in the synthesis of olmesartan medoxomil , a prodrug form of the angiotensin II receptor 1 (AT1) antagonist olmesartan .1 1.Hanumantha Rao, B., Subramanyeswara Rao, I.V., Ravi Kanth, V., et al.A competent and commercially viable process for the synthesis of the anti-hypertensive drug olmesartan medoxomilSci. Pharm.83(3)465-478(2015)

Methoxamine hydrochloride (Methoxamine HCl) is an alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.

6-(γ,γ-Dimethylallylamino)purine (Triacanthine), which is a plant growth substance, shows hypertensive and antitumor activity, also cardiotonic, antispasmodic and a respiratory analeptic.

Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.Hirsutine has anticancer, cardioprotective, anti-hypertensive and anti-arrhythmic activities, it also has vasodilatation activity, the mechanism is related to blockade of Ca2+ influx through L-type Ca2+ channels and inhibition of intracellular Ca2+ release may have no relationship with K+ channels.

Potent and selective bradykinin B1 receptor antagonist (ID50 values are 2.8 and > 600 nM at B1 and B2 receptors respectively). Exhibits no intrinsic agonist activity and is resistant to aminopeptidase and kininase II (ACE) cleavage. Displays hypertensive

Endothelin-1 (1-31) (Human) TFA, a potent vasoconstrictor and hypertensive agent, originates from the chymase-mediated selective hydrolysis of big ET-1 [1].

Ecadotril is a neutral endopeptidase (NEP) inhibitor, which plays an anti hypertensive role.

Diazoxide (Proglycem) is a benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.

(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..

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.