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ET-A and ET-B antagonist
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. -
5HT3-receptor antagonist
Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. -
CXCR4 antagonist
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. -
Endothelin antagonist receptor
Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer. -
H3 receptor antagonist
Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
H3 receptor antagonist
Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
D3/D2 Dopamine Receptor Antagonist
Cariprazine hydrochloride is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors. -
H1-receptor antagonist
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. -
H1 histamine receptor antagonist
Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. -
H2-receptor antagonist
Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. -
5-HT3 antagonist
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. -
μ-opioid antagonist
Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation. -
Dopamine Receptor antagonist
Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic. -
mGlu5 antagonist
MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively. -
OX Receptor Antagonist
SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. -
NK3 receptor antagonist
Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. -
5HT1A antagonist
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT. -
5-HT/dopamine receptor antagonist
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. -
5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. -
5-HT Receptor antagonist
Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist. -
Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
Dopamine Receptor antagonist
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. -
Histamine Receptor antagonis
Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine. -
Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. -
PAFR antagonist
Ginkgolide B (BN 52021) is a PAFR antagonist with IC50 of 3.6 μM. -
5-HT3 receptor antagonist
Granisetron HCl is a serotonin 5-HT3 receptor antagonist -
AT1 antagonist
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. -
5-HT2A serotonin receptor antagonist
Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. -
5-HT2/5-HT1 antagonist
Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant. -
5-HT1A and α1-adrenergic receptor antagonist
Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. -
5-HT Receptors/D2 dopamine receptor antagonist
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. -
5-HT Receptors antagonist
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy. -
α1-adrenoceptor antagonist
Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers).

