constriction

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

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

Methacholine Chloride (Acetyl-β-methylcholine chloride) is a quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma.

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

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

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.

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.

Ablukast (Ro 23-3544) is a leukotriene receptor antagonist that functions as an anti-asthmatic.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Benzamil is an epithelial sodium channel (ENaC) blocker that inhibits sodium transport from (IC50 = 4 nM) and binds to (Kd = 5 nM) bovine kidney cortex membrane vesicles.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

Palmitoyl glutamic acid (N-Palmitoyl-L-glutamic acid) is an acyl amino acid that inhibits aortic constriction and counteracts haloperidol-induced oral motility disorders.

Laprafylline is a xanthine compound with inhibitory effects on bronchoconstriction in vivo and antitumor activity.Laprafylline acts as a competitive serotonergic antagonist at low concentrations, and inhibits constriction induced by hist at high difficulties.

ZD-2138 is a potent and selective specific inhibitor of 5-lipoxygenase (5-LOX) that inhibits allergen-induced pulmonary bronchoconstriction and reduces neurally-induced fast-acting kallikrein-ergic constriction of isolated airways in guinea pigs.ZD-2138 can be used for the treatment of asthma disease.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

Norepinephrine bitartrate acts directly on the α- and β-adrenergic receptors. Norepinephrine Bitartrate is a bitartrate salt of norepinephrine, a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine. Clinically, norepinephrine is used as a peripheral vasoconstrictor that causes constriction of arterial and venous beds via its alpha-adrenergic action. It is also used as a potent inotropic and chronotropic stimulator of the heart mediated through its beta-1 adrenergic action.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

Tetrahydrozoline (Tetryzoline), an alpha agonist, have an effect on the constriction of conjunctival blood vessels. This contributes to relieve the redness of the eye resulted from minor ocular irritants.

GW-406381 is a highly selective COX-2 inhibitor acting peripherally and centrally, reducing spontaneous ectopic discharges in rat sural nerves following chronic compressive injury. It is suitable for studying central sensitisation and inflammatory pain.

Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2/7.3 channels (KV7.2/7.3 channel/KCNQ2/3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg/kg and 9.63 mg/kg, respectively.

ASP8477 is a potent and selective FAAH inhibitor. It increases anandamide levels in the brain when administered orally. In rat models of neuropathic and osteoarthritic pain, ASP8477 demonstrates significant efficacy without causing motor coordination issues. A single oral dose of ASP8477 improves thermal hyperalgesia and cold allodynia in rats with chronic constriction nerve injury. Moreover, ASP8477 restores the decreased muscle pressure threshold in a myalgia model induced by reserpine. Research indicates that ASP8477 possesses analgesic effects effective for alleviating neuropathic and functional pain, making its pharmacological properties suitable for chronic pain treatment.

PLC-β-IN-1 (Compound 8a) is an inhibitor of PLCβ that exhibits anti-airway constriction activity by suppressing PLCβ and its downstream signaling pathways. It also enhances the bronchorelaxant effects of β-agonists. This compound can be utilized in asthma research.