vasoconstriction

Aprikalim (RP 52891) is an adenosine triphosphate potassium channel (KATP) opener that protects against nerve damage in a rabbit model of spinal cord ischemia.Aprikalim inhibits vasoconstriction and inhibits the elevation of [Ca2+]i during myocardial paralysis, and can be used to study cardiovascular disease.

Clazosentan (Ro 61-1790) is a selective antagonist of the endothelin A receptor (ETAreceptor) that inhibits ET-1-mediated vasoconstriction, preventing cerebral vasospasm and vasospasm-associated cerebral infarction.

Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

Perindopril erbumine (S9490-3) is the tert-butylamine salt of perindopril, the ethyl ester of a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, Perindopril erbumine (S9490-3) is converted to its active form perindoprilat, inhibiting ACE and the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue.

Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction as a result of overdose with certain 5-HT2A agonist drugs.

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist (IC50: 0.26 nM). Upon hydrolysis to candesartan during gastrointestinal absorption, it selectively competes with angiotensin II for binding to the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation.

Danshensu sodium salt (Sodium Danshensu) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstriction in Ca2+-free medium.

Neocuproine is a copper(I) chelator that enhances the purinergic component of vasoconstriction induced by electric field stimulation, and is often used as a ligand reagent and copper ion detector.Neocuproine forms stable complexes with copper ions and can play a catalytic role in certain chemical reactions and analytical methods.Neocuproine acts as a redox-active on the iron and cobalt ligand platform for protection against oxidative damage in NSC34 cells.

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

Naphazoline hydrochloride (Naphazoline HCl) is an adrenergic vasoconstrictor agent used as a decongestant.

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

Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.

Nadolol is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities. Nadolol competitively blocks beta-1 adrenergic receptors located in the heart and vascular smooth muscle, inhibiting the activities of the catechola

Terlipressin Acetate, a highly selective vasopressin V1 receptor agonist, on oxygen and glucose deprivation re-oxygenation (OGD R)-induced damage in intestinal epithelial cells (IEC-6).Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

Amastatin HCl is an inhibitor of aminopeptidase. It also induces vasoconstriction.

Almotriptan (LAS 31416) is a 5-HT1B 1D-receptor agonist used to treat migraine.Almotriptan is a triptan drug for treatment of migraine headaches.Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels.

Naphazoline (Naphcon-a) is a sympathomimetic compound with marked alpha adrenergic activity. Naphazoline can be used as a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane.

Angiotensin I/II (2-7) is a peptide that contains the amino acids 2-7 and is converted from Angiotensin I/II peptide. Angiotensin is a peptide hormone that causes vasoconstriction and a subsequent increase in blood pressure. Angiotensin also stimulates th

PD 142893 is a functional endothelin-stimulated vasoconstriction antagonist.

Forasartan is a non - peptide angiotensin II receptor antagonist with antihypertensive activity. Forasartan and angiotensin II compete to bind AT1 receptor subtypes in vascular smooth muscle, thereby blocking angiotensin II-mediated vasoconstriction, lead

Thromboxane A2, as an unstable intermediate between the prostaglandin endoperoxides and thromboxane B2, is a potent inducer of platelet aggregation and causes vasoconstriction.

Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)

5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50 = 0.54 μM), and Cav3.3 and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5(6)-EET is provided as a mixture of the free acid and lactone.