YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models.

CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.

PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP).

4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM).

JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.

YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models.

PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis.

Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be used for essential and renovascular hypertension research.

Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer.

Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.

A68930, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.

Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM in HEK 293 cells, and Kds of 0.9 nM and 1.2 nM, respectively. Alniditan dihydrochloride has migraine-preventive effects.

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.

TCS 2510 is a selective EP4 agonist. TCS 2510 can be used for the research of metabolic diseases.

Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo

Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.

CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects.

Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia.

Capromorelin Tartrate (CP 424391-18), a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki of 7 nM for hGHS-R1a and EC50 of 3 nM for rat pituicyte.

Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.

[Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity.

Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.

FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.

SKF83959 is a potent and selective dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors, respectively). SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.

Lisuride is an orally active dopamine D2 receptors agonist. Lisuride as an ergot derivative can be used for the research of Parkinson's disease, migraine, and high prolactin levels.

RC-3095 TFA is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist. RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice.

Synephrine (Oxedrine) hemitartrate, an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine hemitartrate is a sympathomimetic compound and can be used for weight loss.

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.