hypotensive

Losulazine is a peripheral sympathetic antihypertensive compound that can be taken orally. Losulazine causes relatively modest, transient depletion of dopamine and norepinephrine in brain regions protected by the blood-brain barrier.

Gamibetal (4-Amino-3-hydroxybutyric Acid) is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues. Also used in the preparation of HIV-1 inhibitors derived from Betulinic Acid (B330250).

Lysergol has been used as a hypotensive, psychotropic analgesic, and uterus- and intestine-stimulating drug. Lysergol is a clavinet alkaloid isolated from seeds of Ipomoea muricata and is a bioenhancer for the drugs and nutrients and has antibacterial act

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].

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

Acebutolol hydrochloride (Acebutolol HCl) acts as a cardioselective beta-adrenergic antagonist with little effect on bronchial receptors and has intrinsic sympathomimetic properties. Acebutolol hydrochloride is the hydrochloride salt form of acebutolol, a synthetic butyranilide derivative with hypotensive and antiarrhythmic activity. Having stabilizing and quinidine-like effects on cardiac rhythm, Acebutolol hydrochloride is used in ventricular arrhythmias. Other indications include hypertension, alone or in combinations with other agents.

Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

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.

Bunazosin Hydrochloride (E 1015) is an alpha(1)-adrenoceptor antagonist used as a systemic antihypertensive and an ocular hypotensive drug.

Lys-[Des-Arg9]Bradykinin,TFA is Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Theodrenaline is a cardiac stimulant and acts as an anti-hypotensive agent in conjunction with cafedrine.

1. Dihydrolycorine-HCL(DL) shows hypotensive effects, it can block alpha 1-adrenoceptors. 2. Dihydrolycorine is an inhibitors of protein synthesis in eukarytic cells, it halts protein synthesis in eukaryotic cells by inhibiting the peptide bone formation

Solasodine (Purapuridine)(Purapuridine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine showed selective cytotoxicity against cervical cancer cell line (HeLa) and human myeloid leukemia cell line (U937).

14-Deoxy-11,12-didehydroandrographolide (AP10) has hypotensive, anti-inflammatory, anti-asthma, and anti-cancer actions. It can inhibit NF-κB activation.

Guanabenz hydrochloride (NE56490) is an orally active α2-adrenoceptor agonist with hypotensive effects.

(+)-pinoresinol-β-D-glucoside; (+)-pinor is the major active furanoid lignan in Lianxian. It shows antioxidant, hypotensive and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory activities.

CUDA is an effective soluble cyclohydrolase inhibitor with IC50 of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases the activity of peroxisome proliferator-activated receptor (PPAR) alpha. CUDA may be valuable for the study of cardiovascular diseases.

1. Delsoline (Belsoline) has hypotensive effects.2. Delsoline is not only effective in preventing ventricular fibrillation and arrythmia, but can raise the intebsity of the threthold of electrical shocks to cause ventricular fibrillation in rabbits, the antiarrythmic effect of it may be mainly attributed to itsganglionic blocking and negative cardiac inotropic effect.

Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell (Ac-Pro-Tyr-Asn-Ser-Ser-Pro-Arg-Pro-Glu-Gln-His-Lys-Ser-Tyr-Lys-Cys) is a peptide that inhibits the function of NOSs as a result it blocks the production of NO. Because of the invol

Flesinoxan, a hypotensive agent, is an effective, high-affinity, and selective 5-hydroxytryptamine1A receptor agonist (EC50: 24 nM).

17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma, with unsubstituted or meta-substituted aromatic derivatives being the most potent FP receptor agonists. 17-trifluoromethylphenyl trinor PGF2α, which contains an aromatic ring reminiscent of the trifluoromethyl-phenoxy ring in travoprost ((+)-fluprostenol isopropyl ester), is expected to act similarly to the free acid form of travoprost as an ocular hypotensive agent. Additionally, 17-phenyl trinor PGF2α is a potent luteolytic and abortifacient with a potency equal to or greater than that of fluprostenol and cloprostenol.

A 62198 is a potent and selective renin inhibitor with potential as a hypotensive agent.

Bimatoprost is the Allergan trade name for 17-phenyl trinor prostaglandin F2α ethyl amide (17-phenyl trinor PGF2α ethyl amide), an F-series PG analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group produces 15-keto-17-phenyl trinor PGF2α ethyl amide. 15-keto-17-phenyl trinor PGF2α ethyl amide is a potential metabolite of 17-phenyl trinor PGF2α ethyl amide when 17-phenyl trinor PGF2α ethyl amide is administered to intact animals. No pharmacological studies on 15-keto-17-phenyl trinor PGF2α ethyl amide have been reported.

Foslevcromakalim (QLS-101), an ATP-sensitive potassium channel opener, serves as a proagent for ocular hypotensive effects [1] [2].

Piperilate, also known as Pipethanate, is a hetrazepine derivative PAF antagonist and anticholinergic mixture, commonly utilized in bronchial asthma research. This compound exhibits hypotensive properties and has been found to effectively counteract the toxic effects of organophosphates in mice [1] [2] [3].

AL 8810 is an 11β-fluoro analog of prostaglandin F2α (PGF2α) which acts as a potent and selective antagonist at the FP receptor. AL 8810 ethyl amide is an analog of AL 8810 in which the C-1 carboxyl group has been modified to an N-ethyl amide. This modification is analogous to the PG N-ethyl amides, as typified by Bimatoprost, that have been introduced as alternative PG ocular hypotensive prodrugs. In contrast to AL 8810 which contracted the cat iris, AL 8810 ethyl amide showed no contraction activity at concentrations up to 10-4 M and did not antagonize the activity of PGF2α-ethanolamide in this system.

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

Ketanserinol is the metabolite of ketanserin. Ketanserin is a hypotensive drug with 5-HT2 receptor antagonism, used to reverse pulmonary hypertension caused by protamine.

KUL-7211 is an β2 and β3 adrenergic receptor agonist. KUL-7211 is a potent ureteral relaxant with a relatively small hypotensive effect.

Bimatoprost isopropyl ester is an F-series prostaglandin analog, which has been approved as a hypotensive drug.

Potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

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

Adrenomedullin (ADM) is a 52-aa hypotensive peptide. Adrenomedullin (ADM) has structural similarity with amylin.

BNP-45 (rat) TFA is a circulating form of rat brain natriuretic peptide isolated from rat heart with potent hypotensive and natriuretic potency.

Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a peptide known for its strong hypotensive effects and inhibition of catecholamine release from chromaffin cells. It effectively suppresses catecholamine secretion in PC12 pheochromocytoma cells with an IC50 of 350 nM and prevents the desensitization of nicotinic cholinergic agonist-induced catecholamine release and nicotinic signal transduction, with an EC50 of approximately 270 nM for desensitization blockade, as evidenced by inhibited 22 Na+ uptake [1].

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Catharanthine tartrate (Catharanthine hemitartrate) is an alkaloid from periwinkle that inhibits voltage-gated L-type calcium channels and has antitumor and hypotensive activities.

Visnagin has acute hypotensive, anti-inflammatory, and neuroprotective effects, it protects against doxorubicin-induced cardiomyopathy through modulation of mitochondrial malate dehydrogenase.

A 39355 may specifically overcome multidrug resistance without the serious hypotensive effects associated with calcium antagonists.

N-Desethyl Bimatoprost (17-phenyl trinor PGF2α amide) is an F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative PG hypotensive prodrugs. Although it has been claimed that PG amides are not converted to the free acids in vivo, studies have shown that bovine and human corneal tissue converts the amides of various PGs to the free acids with a conversion efficiency of about 10-20% relative to the hydrolysis of isopropyl esters. 17-phenyl trinor PGF2α amide would be expected to show the typical intraocular effects of latanoprost, but with the much slower hydrolysis pharmacokinetics of the PG N-amides.

Bimatoprost is an F-series prostaglandin (PG) analog approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group and amide hydrolysis of Bimatoprost produces 15-keto-17-phenyl trinor PGF2α, a potential metabolite when administered to animals. 15-keto PG analogs can be minor impurities in commercial preparations of corresponding bulk drug compounds. Although much less potent than the parent compound, 15-keto PGs can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure of normal cynomolgus monkeys at a dose of 1 μg eye. 15-keto Latanoprost (15-keto-17-phenyl-13,14-dihydro trinor PGF2α isopropyl ester) acts as a miotic in normal cat eyes, causing an 8 mm reduction in pupillary diameter at 5 μg eye. This is less potent compared to many other F-type PGs; for example, PGF2α induces similar miosis at less than 1 μg eye.

Fluprostenol is an F-series prostaglandin analog which has been approved for many years as a luteolytic in veterinary animals. The isopropyl ester of fluprostenol (travoprost) is an effective ocular hypotensive drug. CAY10532 is a methyl ester analog of fluprostenol.

17-phenyl trinor Prostaglandin F2α N-ethyl amide (17-phenyl trinor PGF2α) is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name 17-phenyl trinor PGF2α ethyl amide. Investigations in our lab have shown that 17-phenyl trinor PGF2α ethyl amide is converted by an amidase enzymatic activity in the human cornea to yield the corresponding free acid, with a conversion rate of about 25 μg/cornea/24 hours. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist. 15(R)-17-phenyl trinor PGF2α is the 15-epi, or unnatural isomer of this active free acid metabolite. It has much diminished FP receptor-mediated activity

A number of 17-phenyl trinor prostaglandin F2α(17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma.1,2,3Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.417-trifluoromethylphenyl-13,14-dihydro trinor PGF2αbears an aromatic ring which is reminiscent of the trifluoromethyl-phenoxy ring of travoprost ((+)-fluprostenol isopropyl ester). As an ocular hypotensive agent, it would be expected that 17-trifluoromethylphenyl-13,14-dihydro trinor PGF2αwould act very much like the free acid of latanoprost.

Amiquinsin is a drug with hypotensive effect.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group without isopropyl ester hydrolysis produces 15-keto latanoprost. 15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type PGs; for example, PGF2α will produce this degree of miosis at a dose of less than 1 μg/eye. Products of β-oxidation account for most of the metabolites of latanoprost recovered in plasma and urine. However, 15-keto latanoprost is a minor metabolite, and one which could be enhanced in situations where β-oxidation is reduced.

17-phenyl trinor Prostaglandin F2α (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and is a potent agonist for the FP receptor, binding with a relative potency of 756% compared to that of PGF2α. The ethyl amide of 17-phenyl trinor PGF2α bimatoprost has been approved for use as an ocular hypotensive drug. 17-phenyl trinor PGF2α methyl amide is an analog of bimatoprost. Its biological and toxicological properties have not been evaluated.

(15R)-Bimatoprost (15(R)-17-phenyl trinor PGF2α ethyl amide), an isomer of Bimatoprost characterized by an inverted (β) hydroxyl group on C-15 [1], is a prostaglandin analog employed in the treatment of glaucoma and ocular hypertension.

Bimatoprost (AGN 192024) is a cloprostenol-derived amide that is used as an antihypertensive agent in the treatment of open-angle glaucoma and ocular hypertension.