Drug results: 100
| rilonacept | an anti-arthritis agent derived from IL-1R and IL-1RAcP | |
| naltrexone | Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. |
|
| rupatadine | Rupatadine is a second-generation antihistamine, long-acting histamine antagonist with selective peripheral H1-receptor and platelet activating factor (PAF) antagonistic activities. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug, maintaining activity for up to 24 hours. |
|
| perampanel | a non-competitive AMPA glutamate receptor antagonist indicated as adjunctive therapy for the treatment of seizures |
|
| loratadine | A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness. |
|
| pranlukast | SRS-A antagonist; leukotriene D4 receptor antagonist |
|
| rolapitant | An orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. |
|
| tirofiban | a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation, when administered intravenously inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner |
|
| flibanserin | a serotonin receptor modulator with high affinity for the following serotonin (5-hydroxytryptamine or 5-T) receptors: agonist activity at 5-HT1A and antagonist activity at 5-HT2A. Flibanserin also has moderate antagonist activities at the 5-HT2B, 5-HT2C, and dopamine D4 receptors, used in the treatment of premenopausal women with hypoactive sexual desire disorder |
|
| aripiprazole | A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression. |
|
| losartan | An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II. |
|
| relugolix | Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone. |
|
| macitentan | an endothelin receptor antagonist that prevents the binding of ET-1 to both ETA and ETB receptors, macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells |
|
| candesartan cilexetil | a nonpeptide angiotensin II receptor antagonist |
|
| maropitant | Neurokinin-1 receptor antagonist for treatment and prevention of emesis |
|
| avacopan | Avacopan is a complement 5a receptor (C5aR) antagonist that inhibits the interaction between C5aR and the anaphylatoxin C5a. Avacopan blocks C5a-mediated neutrophil activation and migration. The precise mechanism by which avacopan exerts a therapeutic effect in patients with ANCA-associated vasculitis has not been definitively established. |
|
| ebrotidine | an H2-receptor antagonist and gastric mucosa protector |
|
| alprenolol | One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. |
|
| fimasartan | an angiotensin II receptor antagonist |
|
| atogepant | Atogepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. |
|
| revefenacin | Revefenacin is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo models, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of revefenacin is predominantly a site-specific effect. |
|
| bupranolol | An adrenergic-beta-2 antagonist that has been used for cardiac arrhythmia, angina pectoris, hypertension, glaucoma, and as an antithrombotic. |
|
| tasosartan | angiotensin II antagonist; structure given in first source |
|
| grapiprant | A potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties |
|
| cyproheptadine | A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. |
|
| famotidine | A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. Computer-aided, structure-based, virtual screening of libraries of compounds against SARS-CoV-2 proteins suggested potential for famotidine to interact with viral proteases in-volved in coronavirus replication. HOWEVER, there is no clinical trial evidence supporting efficacy or safety for treatment of COVID-19. |
|
| nizatidine | A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. |
|
| sonidegib | specific Smoothened/Smo antagonist |
|
| tolvaptan | A benzazepine derivative and selective VASOPRESSIN V2 RECEPTOR antagonist that is used to treat euvolemic and hypervolemic HYPONATREMIA. It is also used in the treatment of rapidly progressing AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE to slow the rate of cyst development and renal insufficiency. |
|
| ambrisentan | an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor |
|
| seratrodast | has thromboxane A2 & prostaglandin H2 receptor antagonistic action |
|
| naloxone | A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. |
|
| naldemedine | Naldemedine is an opioid antagonist with binding affinities for mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids. |
|
| lifitegrast | a lymphocyte function-associated antigen-1 ( LFA-1) antagonist, blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1), LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues |
|
| anakinra | A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA. As IL-1 levels are elevated in patients with COVID-19, anakinra is currently being investigated for its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19. | |
| irbesartan | A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease. |
|
| darifenacin | a competitive muscarinic receptor antagonist with greater affinity for the M3 receptor than for the other known muscarinic receptors, M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function |
|
| rimonabant | A pyrazole and piperidine derivative that acts as a selective cannabinoid type-1 receptor (CB1 RECEPTOR) antagonist. It inhibits the proliferation and maturation of ADIPOCYTES, improves lipid and glucose metabolism, and regulates food intake and energy balance. It is used in the management of OBESITY. |
|
| ketanserin | A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients. |
|
| rimegepant | Rimegepant is a calcitonin gene-related peptide receptor antagonist |
|
| azasetron | a selective 5-HT3 receptor antagonist; structure given in first source |
|
| atosiban | Atosiban is a synthetic peptide which is a competitive antagonist of human oxytocin at receptor level. In human pre-term labour, atosiban at the recommended dosage antagonises uterine contractions and induces uterine quiescence. |
|
| pimavanserin | an atypical antipsychotic, mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson's disease psychosis is unknown. however, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors |
|
| timolol | A beta-adrenergic antagonist that is similar in action to PROPRANOLOL; the levo-isomer is more active. Timolol has been proposed as an anti-hypertensive, anti-arrhythmic, anti-angina, and anti-glaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor. |
|
| methylnaltrexone | a selective antagonist of opioid binding at the mu-opioid receptor with restricted ability to cross the blood-brain barrier, function as a peripherally-acting mu‑opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system |
|
| metipranolol | A beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent. |
|
| elacestrant | Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERalfa). In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17beta-estradiol mediated cell proliferation at concentrations inducing degradation of ERalfa protein mediated through proteasomal pathway. Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations. |
|
| carotegrast methyl | Carotegrast methyl is a small-molecule alpha4 integrin antagonist which received its first approval in Japan for the treatment of moderate ulcerative colitis in patients who had inadequate response to 5-aminosalicylic acid. The active metabolite of carotegrast methyl exerts an anti-inflammatory effect by blocking the interaction of alpha4beta1 or alpha4beta7 integrins and their ligands, VCAM-1 and MAd-CAM-1, thereby inhibiting the adhesion of inflammatory cells, including T cells, to vascular endothelial cells and extravasation into inflammatory sites. |
|
| zavegepant | Zavegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. |
|
| acebutolol | A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action. |
|
| aprepitant | Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. |
|
| azelastine | Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine Hydrochloride is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity. |
|
| bosentan | a specific and competitive antagonist at endothelin receptor types ETA and ETB, has a slightly higher affinity for ETA receptors than for ETB receptors, indicated for the treatment of pulmonary arterial hypertension |
|
| eprosartan | angiotensin II receptor antagonist; structure given in first source |
|
| bevantolol | a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension |
|
| nebivolol | A cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial L-arginine/ NITRIC OXIDE system. It is used to manage HYPERTENSION and chronic HEART FAILURE in elderly patients. |
|
| gefapixant | Gefapixant is a selective, non-narcotic P2X3 receptor antagonist being approved for the treatment of refractory chronic cough or unexplained chronic cough. |
|
| dolasetron | Dolasetron mesylate is an antinauseant and antiemetic agent. Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. |
|
| telmisartan | A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION. |
|
| dexloxiglumide | a CCK receptor antagonist; structure given in first source |
|
| palonosetron | an antiemetic and antinauseant agent, it is a serotonin subtype 3 (5-HT3) receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors |
|
| eplerenone | A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. |
|
| solifenacin | A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE. |
|
| linzagolix | Linzagolix is a selective, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist that inhibits endogenous GnRH signalling by binding competitively to GnRH receptors in the pituitary gland, thereby modulating the hypothalamic-pituitary-gonadal axis. |
|
| mifepristone | A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. |
|
| fosnetupitant | Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 (NK-1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses. |
|
| betaxolol | A cardioselective beta-1-adrenergic antagonist with no partial agonist activity. |
|
| diprenorphine | A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered specific antagonist to etorphine |
|
| propranolol | A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs. |
|
| loxiglumide | cholecystokinin receptor antagonist; RN refers to (+-)-isomer |
|
| practolol | A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS. |
|
| pentazocine | The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97) |
|
| elagolix | Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of ORILISSA results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones, estradiol and progesterone. |
|
| suvorexant | a highly selective antagonist for orexin receptors OX1R and OX2R, the orexin neuropeptide signaling system is a central promoter of wakefulness, blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive |
|
| alizapride | a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting. Its effect is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS), this action prevents nausea and vomiting triggered by most stimuli. |
|
| esaxerenone | Esaxerenone is an oral, selective nonsteroidal mineralocorticoid receptor antagonist used for the treatment of hypertension and diabetic nephropathies. |
|
| celiprolol | A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION. |
|
| fulvestrant | An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. |
|
| maraviroc | Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc. |
|
| lafutidine | histamine H(2)-receptor antagonist used as an antiulcer drug |
|
| paliperidone palmitate | A benzisoxazole derivative and active metabolite of RISPERIDONE that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST and SEROTONIN 5-HT2 RECEPTOR ANTAGONIST. It is an ANTIPSYCHOTIC AGENT used in the treatment of SCHIZOPHRENIA. |
|
| vorapaxar | Vorapaxar is a reversible antagonist of the protease-activated receptor-1 (PAR-1) expressed on platelets, but its long half-life makes it effectively irreversible. Vorapaxar inhibits thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation in vitro studies. Vorapaxar does not inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen or a thromboxane mimetic and does not affect coagulation parameters ex vivo. PAR-1 receptors are also expressed in a wide variety of cell types, including endothelial cells, neurons, and smooth muscle cells, but the pharmacodynamic effects of vorapaxar in these cell types have not been assessed. |
|
| zafirlukast | a leukotriene D4 receptor antagonist |
|
| oxprenolol | A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. |
|
| ramatroban | thromboxane A2 receptor antagonist; BAY u 3405 & 3406 are enantiomers of each other |
|
| netupitant | Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 (NK-1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses. |
|
| tropisetron | An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting. |
|
| sitaxentan | endothelin A receptor antagonist |
|
| laropiprant | a potent orally active human prostaglandin D(2) receptor 1 antagonist |
|
| alcaftadine | Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated. |
|
| icatibant | a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer |
|
| carteolol | A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. |
|
| nadolol | A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor. |
|
| talinolol | Talinolol is a beta1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity. By blocking beta1-adrenergic receptors, talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity. |
|
| nalorphine | A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete. |
|
| fezolinetant | Fezolinetant is a neurokinin 3 (NK3) receptor antagonist that blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate neuronal activity in the thermoregulatory center. Fezolinetant has high affinity for the NK3 receptor (Ki value of 19.9 to 22.1 nmol/L), which is more than 450-fold higher than binding affinity to NK1 or NK2 receptors. |
|
| lumateperone | The mechanism of action of lumateperone in the treatment of schizophrenia is unknown. However, the efficacy of lumateperone could be mediated through a combination of antagonist activity at central serotonin 5-HT2A receptors and postsynaptic antagonist activity at central dopamine D2 receptors. |
|
| ubrogepant | Ubrogepant is a calcitonin gene-related peptide receptor antagonist. |
|
| pindolol | A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638) |
|
| ondansetron | A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. |
|
