dual antagonist

BMS-813160 is the first dual CCR2 CCR5 antagonist to enter Clinical development for cardiovascular.

Cyclodrine hydrochloride is a dual cholinergic muscarinic receptor (mAChR) and nicotinic receptor (nAChR) antagonist that can be used in the study of neurologically related diseases.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

RO0270608, the active metabolite of R411, is an orally active dual α4β1 α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

5-HT6 7 antagonist 1 is a dual 5-HT6 7 2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

β2AR M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2 iNOS expression.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob ob mice.

Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.

SCH-37370 is an effective and orally active dual antagonist of platelet-activating factor and histamine. Sch 37370 blocks the binding of [3H]pyrilamine to histamine-H1 receptors in rat brain membranes. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets (IC50 : 0.6 mM) and also competes with PAF binding to specific sites in membrane preparations from human lungs (IC50 : 1.2 mM).

TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2 3 nM for OX2 1 receptors).

KSK67 is a selective dual antagonist of sigma-2 and histamine H3 receptors with inhibitory effects on H3 receptors, sigma-1, and sigma-2 receptors, with Ki values of 3.2, 1531, and 101 nM, respectively.KSK67 can be used to study injury pain and neuropathic pain.

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

Cenicriviroc Mesylate is a dual CCR2 CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

CMI-392 is a dual inhibitor of 5-lipoxygenase and a receptor antagonist for platelet-activating factor (PAF) with IC50 values of 100 nM and 10 nM, respectively.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

Ziprasidone, an antipsychotic agent, functions as a dual antagonist of 5-HT (serotonin) and dopamine receptors. Keto Ziprasidone represents an impurity found within Ziprasidone.

KP496 is a selective, dual antagonist for the Thromboxane A2 receptor (TP) and the Leukotriene D4 receptor (cysLT1).