vasodilation

LDN-27219 is a potent hTGase inhibitor with IC50 of 0.6 uM.

Dilazep dihydrochloride is an adenosine uptake inhibitor. It also inhibits ischemic damage, membrane transport of nucleosides, and platelet aggregation. It has cerebral and coronary vasodilating action through the enhancement of the effect of adenosine.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

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.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is the sodium salt form of bromfenac, a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory properties. Upon ophthalmic administration, bromfenac binds to and inhibits cyclooxygenase II (COX II), an enzyme that converts arachidonic acid to cyclic endoperoxides, which are prostaglandin (PG) precursors. By inhibiting PG formation, bromfenac prevents PG-induced inflammation, vasodilation, leukocytosis, disruption of the blood-aqueous humor barrier, increased vascular permeability, and elevated intraocular pressure (IOP).

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

2-Ethylpyrazine is present in roasted coffee beans and is a volatile compound .2-Ethylpyrazine induces vasodilation through the activity of endothelium-derived relaxing factors.2-Ethylpyrazine activates NO synthesis through the action of endothelial endothelial NO synthase.2-Ethylpyrazine induces vasodilation by inducing NO release and increasing peripheral blood flow to induce vasodilation.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

Methyl nicotinate (methyl pyridine-3-carboxylate) is the methyl ester of that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation.

1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside), isolated from the Caribbean sponge [Tectitethya crypta], is a methoxyadenosine derivative with anti-inflammatory activity, analgesic, and vasodilation properties.

Tertatolol is a highly active antagonist of beta-adrenoceptors and 5-HT receptors, and possesses the pharmacological effect of vasodilation.

Ilepatril TFA is a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), exhibiting physiological effects such as enhanced natriuresis and vasodilation. In animal studies and early clinical trials, Ilepatril TFA has demonstrated the ability to improve insulin sensitivity and metabolic abnormalities, suggesting its potential value in the treatment of cardiovascular and metabolic diseases.

Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.

trans-Ned 19 is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist and two-pore channel (TPC) blocker. It binds with high affinity to the NAADP receptor to inhibit NAADP-dependent lysosomal/endolysosomal calcium release without affecting IP3 or cADPR-mediated calcium signaling pathways. Functionally, trans-Ned 19 inhibits glucose-induced calcium oscillations in pancreatic islets and low histamine concentration-induced endothelium-dependent vasodilation, and reduces Ebola virus infection of host cells. In immunomodulation, NAADP signaling blockade by trans-Ned 19 promotes the conversion of mouse Th17 cells to regulatory T cells (Tregs) and shows protective effects in intestinal inflammation models.

Iloprost (Ciloprost) is a stabilized synthetic analog of prostaglandin I2, an inhibitor of platelet aggregation and vasodilation, used in the study of cardiovascular disease.

Naminidil (BMS-234303) is an ATP-sensitive potassium channel opener with vasodilatory activity that was developed as a topical medication candidate for the treatment of androgenic alopecia. Naminidil is used in research to investigate potassium channel–mediated vasodilation, hair follicle biology, and localized drug delivery strategies.