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.

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.

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.

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.

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.

Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

Gymnestrogenin has a dual LXRα±/α2 antagonistic profile.

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.

[Pmp1,Tyr(OEt)2] AVP, a linear analog of the cyclic arginine vasopressin (AVP) antagonist, retains the antagonistic properties of its parent compound while featuring modified phenylalanine (Pmp) and diethyltyrosine (Tyr(OEt)2) components.

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.

WAY-649123 is an active molecule that exhibits (in vitro) antagonistic properties against (alpha-1A adrenergic receptors), with a (pKi) of 8.9. It also demonstrates a 70-fold selectivity over (alpha-1B) and 100-fold selectivity over (alpha-1D) subtypes. This compound has been shown to cross the blood-brain barrier (BBB) effectively in preclinical trials. Furthermore, WAY-649123 exhibits a high level of oral bioavailability and a favorable pharmacokinetic profile, making it a potential candidate for clinical development targeting conditions associated with (alpha-1A) receptors.

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.

Belrestotug (EOS-448), an antagonistic anti-TIGIT (VSIG9, VSTM3) antibody of the human immunoglobulin G1 kappa (hIgG1 kappa) class, exhibits antineoplastic activity [1].

TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2].

Pregomisin shows platelet-activating factor (PAF) antagonistic activity and the IC 50 value is 4.8x10(-5) M.

Inactive analog of m-3M3FBS (PLC activator)

2-Hydroxy-3-methoxybenzoic acid glucose ester shows a potent antagonistic activity against platelet activating factor (PAF), it can prevent the mice from the PAF-induced death at a dose of 300 micrograms/mouse.

Kadsulignan L shows in vitro antiviral effects on hepatitis B virus. It also shows moderate platelet-activating factor (PAF) antagonistic activities with the IC50 value of 2.6 x 10(-5) M.

L-Albizziin (2-Methoxyidazoxan monohydrochloride) is a highly potent selective antagonist of the alpha 2r adrenergic receptor, with little or no antagonistic effect on imidazoline. It has a significantly higher affinity for the alpha 2D adrenergic receptor (pKd9.7) in guinea pigs than for the alpha 2A adrenergic receptor (pKd8.2) in rabbits.

Topiramate lithium (McN 4853) is a wide-ranging antiepileptic compound with GluR5 receptor antagonistic properties. Its mechanism of action involves enhancing GABAergic activity, inhibiting kainate/AMPA receptors, voltage-sensitive sodium and calcium channels, and increasing potassium conductance. Additionally, this compound inhibits carbonic anhydrase. [1][2][3]

Atrosab, a humanized IgG1 anti-TNFR1 antibody, exhibits antagonistic properties by inhibiting TNF-induced apoptosis and reducing the production of IL-6 and IL-8. It is utilized for research on inflammatory diseases [1].

20681-S has narcotic antagonistic properties and antinociceptive.

Imlunestrant tosylate (LY-3484356) is a potent, orally active selective estrogen receptor degrader (SERD) exhibiting purely antagonistic properties. It effectively maintains inhibition of estrogen receptor (ER)-dependent gene transcription and inhibits cell growth. This compound is applicable in research on ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) [1] [2].

Psycholeine is isolated from the tropical plant Psychotria oleoides; exhibits somatostatin antagonistic activity on growth hormone secretion.

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).

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

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.

Bimatoprost acid (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compared to PGF2α for binding to the FP receptor on ovine luteal cells.

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

1. Rhynchophylline (Mitrinermine) can protect against ischemic damage, probably via regulating the Akt/mTOR pathway. 2. Rhynchophylline can protect against glutamate-induced neuronal death, can inhibit MA impairment in cultured neurons in vitro. 3. Rhynchophylline and isorhynchophylline have a non-competitive antagonistic effect on the NMDA-type ionotropic glutamate receptors, suggest that these alkaloids exert their protective action against ischemia-induced neuronal damage by preventing NMDA, muscarinic M1, and 5-HT2 receptors-mediated neurotoxicity during ischemia.

Cyclo(Tyr-Pro) shows antibacterial activity towards several marine bacterial species, it also shows weak antagonistic activity against VEGFR2 -CD. Cyclo(Tyr-Pro) and cyclo(Pro-Val) are toxic to both suspension cells and seedlings of Pinus thunbergii, whic

Benzoylmesaconine (Mesaconine 14-benzoate) is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesconine has analgesic activity. Benzoylmesconine may improve the resistance of T6S-mice (or thermally injured mice) to the infection of HSV-1, through the induction of antagonistic CD4+ T cells against burn-associated type-2 T cells.

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

Muscarinic toxin 7 (MT7) is a peptide exhibiting selective, noncompetitive antagonistic activity at the muscarinic M1 receptor [1].

Oxycinchophen is a quinoline-like organic, anti-rheumatic compound. It has been used to study P- selectin antagonistic activity, DHOD inhibitory activity, and the effects of anti-inflammatory drugs on vascular smooth muscle.

Antagonist G TFA is a potent antagonist of vasopressin, with additional, weaker antagonistic effects on GRP and Bradykinin. This compound also promotes AP-1 transcription and enhances cellular sensitivity to chemotherapy [1] [2].

AUNP-12 TFA (NP-12 TFA) is a polypeptide antagonist in the pd-1 signaling pathway, which has the same antagonistic effect on pd-l1 and pd-l2, and can protect the proliferation and effector function of lymphocytes.

Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner......

Cyclo(Phe-Gly) shows weak antagonistic activity against VEGFR2 -CD, it also shows strong inhibitory activity against human cancer cells(KB,KBv200) with LD50 at 6.5 and 11.2 umol/L,respectively.

Microgrewiapine A is a selective cytotoxic agent for colon cancer cells over normal colon cells and to exhibit nicotinic receptor antagonistic activity for both the hα3β4 and hα4β2 receptor subtypes.

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.

(-)-(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.

Isopimaric acid is active against MDR and MRSA strains of S. aureus which are becoming increasingly resistant to antibiotics, the minimum inhibitory concentrations (MIC) are 32-64 microg/mL . Isopimaric acid is also possible that an antagonistic interacti

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

Nifedipine HCl is a potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.

GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].

DS69910557, a potent, selective, and orally active antagonist of the human parathyroid hormone receptor 1 (hPTHR1), exhibits antagonistic activity with an IC50 value of 0.08 μM. It is useful in researching hyperparathyroidism, hypercalcemia of malignancy, and osteoporosis.