antagonistic

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

Dalcotidine (KU 1257) is a novel histamine H2 receptor antagonist with histamine H9 receptor antagonistic activity and antisecretory effects.The Ki value for binding to guinea pig cerebral cortex was 0.040 The KB value for antagonism of histamine-induced positive chronotropic responses in the right atrium of isolate guinea pigs was 0.041.Dalcotidine improves the quality of ulcer healing, and may contribute to a reduction in ulcer recurrence and relapse rates.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

Tefludazine, a novel neuroleptic with a benzindone structure, is a compound with good oral activity and antagonistic effects on dopamine and 5-hydroxytryptamine receptors. Tefludazine has shown potent dopamine (DA) antagonistic activity in in vitro and in vivo test models in mice, rats and dogs. Tefludazine is a therapeutic agent used to treat psychiatric disorders.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

Pipoxizine has an antagonistic effect on histamine-induced bronchoconstriction and may be used in the study of asthma disease.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

Clemastine fumarate (Meclastine (fumarate)) is a synthetic ethanolamine with anticholinergic, sedative, and histamine H1 antagonistic properties.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

Lanthanum trichloride can be used as an analytical reagent and can be used as a raw material for extracting metal lanthanum and as a petroleum cracking catalyst. Lanthanum chloride also has a certain role in the field of medicine. For example, studies have shown that the antagonistic effect of lanthanum chloride on endotoxin (LPS) in vivo effects has a certain impact on the search for new effective endotoxin antagonists, providing experimental evidence for the prevention and treatment of endotoxemia.

Xanthotoxol (Psoralen) is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.

Sonepiprazole (PNU-101387G) is a chemical compound known for its selective antagonistic properties toward D4 dopamine receptors, exhibiting dissociation constants (Kis) of 3.6 nM and 10.1 nM for rat D4 (rD4) and human D4.2 (hD4.2) dopamine receptors, respectively; it shows significantly less affinity for rat D2 (rD2) dopamine and Histamine-H1 receptors, with Kis of 5147 nM and 7430 nM, respectively.

Lin28-let-7a antagonist 1, with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction,and shows a clear antagonistic effect against the Lin28-let-7a interaction.

BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively.

Estetrol(Donesta) is an orally available, selective modulator of the estrogen receptor, a naturally occurring estrogen synthesized by the human fetal liver during pregnancy.Estetrol has effects on the endometrium or central nervous system, but is antagonistic to the breast.Estetrol may help to reduce thrombosis at low concentrations. Estetrol may be used to relieve menopausal symptoms.

Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).

LBG20304 (compound 2s) serves as a ligand for the homologous GluK5 receptor, demonstrating an IC50 of 432 nM and exhibiting over 40-fold selectivity against the GluK1-3 isoforms. At concentrations below 10 μM, LBG20304 shows neither agonistic nor antagonistic effects on heterologous GluK2 5 receptors. However, at concentrations above 10 μM, it displays minimal agonist activity in neuronal slices (rat).

Anti-osteoporosis agent-10 is an inhibitor of osteoporosis that suppresses the formation of osteoclasts with an IC50 of 0.042 μM. It also exhibits antagonistic activity towards PPARγ, with an EC50 value of 0.75 μM.

S18327 demonstrates significant antagonistic effects on both α1 and α2 adrenergic receptors, positioning it as a potential antipsychotic compound.

Trioxifene (LY133314) is a selective estrogen receptor modulator (SERM) that competitively binds to estrogen receptor alpha (ERalpha) and exhibits antagonistic effects on ERalpha-mediated gene expression.

TAS-108 (also known as SR-16234) is a selective estrogen receptor modulator (SERM) reported to exhibit antagonistic activity towards estrogen receptor (ER) α, while demonstrating high affinity and weak partial agonistic activity for the ERβ receptor.

BD1018 is a novel sigma receptor ligand with antagonistic activity.