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5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. -
PAF receptor antagonist
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor. -
Adrenoceptors antagonist
BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration. -
Adrenergic α1 Receptor Antagonist
HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes. -
5-HT1A receptor antagonist
NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. -
α2-adrenergic receptor antagonist
Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM). -
Adrenoceptors antagonist
S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker. -
Adrenoceptors antagonist
(S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR. -
Adrenoceptors antagonist
SR 59230A hydrochloride is a β3-adrenoceptor antagonist. -
Histamine H4 receptor antagonist
A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). -
Adenosine A2A receptor antagonist
Preladenant is a potent and selective antagonist at the adenosine A2A receptor. -
adrenergic receptor antagonist
Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro. -
5HT2A antagonist
Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors. -
CCK-2 receptor antagonist
Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
CCK antagonist
Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini. -
adenosine A2B receptors antagonist
CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. -
dual antagonist of TP/DP2
BAY-u 3405 is an approved human medication for the treatment of allergic rhinitis that has documented activity as an antagonist of the thromboxane receptor (TP receptor). -
Oxytocin antagonist
PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM. -
mGluR antagonist
SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype. -
5-HT4 Receptor Antagonist
SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist. -
5-HT3 receptor antagonist
Tropanserin acts as a potent and selective 5-HT3 receptor antagonist. -
ETA antagonist
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA). -
α2 adrenergic receptor antagonist
Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant. -
A2A receptor antagonist
Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease. -
5-HT6 serotonin receptor antagonist
SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes. -
CRF-1 antagonist
Emicerfont, also known as GW876008, is a CRF-1 antagonist. Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release. -
5-HT6 antagonist
SB 399885 hydrochloride is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
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OX2 receptor antagonist
JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R). -
CRF1 receptor antagonist
Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor. -
angiotensin II receptor antagonist
BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor. -
LPA1 Receptor antagonist
AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively

