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.

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.

GW406381 is a highly selective inhibitor of cyclooxygenase-2 (COX-2). GW406381 also attenuates spontaneous ectopic discharge in the sural nerves of rats following chronic constriction injury.

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).

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.

Daurinoline is a non-competitive antagonist, it exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism, it would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.

CGP 33304 is a dual leukotriene receptor antagonist and phospholipase A2 inhibitor. It prevents hypoxia secondary to bronchial constriction induced by leukotriene in a shocking state.

CGP 45715A (irukostat) is a potent peptide-leukotriene antagonist used to treat respiratory diseases by antagonizing the bronchial constriction, mucus secretion, and inflammatory effects of these leukotrienes.

Argiprestocin (Arginine vasotocin) , also called antidiuretic hormone that plays a key role in maintaining osmolality. It is a neurohypophysial hormone found in most mammals. Drugs used to cause constriction of the blood vessels.

N-acetyl Leukotriene E4 is an endogenous metabolite of Leukotriene E4, which is excreted mainly through bile, and is one to three orders of magnitude less active than Leukotriene E4, causing constriction of the airways.

(S)-4CPG ((S)-4-Carboxyphenylglycine) is a competitive mGlu1 receptor antagonist that attenuates nociceptive hypersensitivity and nociceptive abnormalities associated with sciatic nerve constriction injuries in rats, and may be used in the study of neurological disorders.

Pranlukast hemihydrate (ONO-1078 hemihydrate) is a selective and potent leukotriene (LT) antagonist with anti-asthmatic activity that inhibits [3H]LTD4 and [3H]LTE4 binding to lung membranes and antagonizes LTC4-induced constriction of guinea-pig airways.Pranlukast hemihydrate is used in the study of asthma. Pranlukast hemihydrate is used in the study of asthma.

KB-R7785 is a novel ADAM12 and MMP inhibitor, ameliorating cardiac function in a transverse aortic constriction (TAC) model by inhibiting the proteolytic activation of HB-EGF signaling, exerting its antidiabetic effect by ameliorating insulin sensitivity through the inhibition of TNF-alpha production.

SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.

Fremanezumab (TEV-48125) is a humanised monoclonal antibody targeting CGRP, capable of neutralising human (IC50=7.94 nM), mouse (IC50=19.6 nM) and rat CGRP, and is indicated for the prevention of migraine. Fremanezumab inhibits CGRP's vasodilatory effects in the basilar artery constriction segment and suppresses activation of A-δ and high-threshold (HT) neurons in the meningeal nociceptive system triggered by cortical spreading depression (CSD) in rats. In vitro, Fremanezumab counteracts CGRP's immunosuppressive effects on microglia and lymphocytes.