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α2-receptor agonist
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal. -
CCK antagonist
Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist. -
sigma-2 (σ2) receptor ligand
Glycerol phenylbutyrate is a sigma-2 (ς2) receptor ligand, with a pKi of 8.02. -
Histamine H1 antagonist
Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. -
alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. - Sodium deoxycholate is a bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.
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β2-adrenergic receptor agonist
Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist. -
Somatostatin Receptor agonist
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). - Bromperidol, also known as Impromen and R-11333, is used as a means of long-term maintenance treatment of schizophrenia. Bromperidol is a close structural analogue of haloperidol. C3435T polymorphism is associated with some therapeutic response to bromperidol in schizophrenic patients, possibly by different drug concentration in the brain.
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5-HT receptor /dopamine receptors antagonist
Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors. -
β-adrenergic receptor antagonist
Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity. - Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic drug. Levomepromazine is used for the treatment of psychosis, particularly those of schizophrenia, and manic phases of bipolar disorder.
- Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
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dopamine D2 receptor antagonist
Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic. -
selective IP receptor agonist
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist. -
α2 adrenoceptor antagonist
Piperoxan hydrochloride is an α2 adrenoceptor antagonist. -
5-HT1A receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone. -
ligand-linker conjugate
CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker. -
CRTH2 antagonist
ACT-129968 is a potent and selective CRTH2 antagonist. -
mGlu2 receptor modulator
CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM -
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
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EP2 Agonist
C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM. -
Serotonin2A Receptor Inverse Agonist
Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease. -
sGC activator?€?
BAY 41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator. -
5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
prostaglandin EP4 receptor antagonist
Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. -
Opioid antagonist
Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
CysLT1 receptor antagonist
MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. -
CCK-2 receptor antagonist
Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
β2-adrenergic receptor agonist
Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD). - cAMPS-Sp, triethylammonium salt is a cell-permeable cAMP analog that activates cAMP receptor proteins such as PKA and cAMP-regulated guanine nucleotide exchange factor.
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dopaminergic stabilizer
ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission.

