Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo.

Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia.

Sabcomeline (hydrochloride) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition.

Milameline is a muscarinic receptor agonist that improves cognition.

MK-6884-11C is a positron emission tomography (PET) imaging agent for the study of M4 muscarinic receptor positive allosteric modulators (PAMs) in neurodegenerative diseases.

Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to treat asthma.

Ecnoglutide is a glucagon-like peptide 1 (GLP-1) receptor agonist.

Utreglutide is a potent glucagon-like peptide 1 (GLP-1) receptor agonit.

Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. Raclopride binds to D2 and D3 receptors with dissociation constants of between 1.8 nM and 3.5 nM, but has a very low affinity for D4 receptors.

Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness.

Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.

HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute treatment of migraine.

Vicasinabin is the potent agonist of cannabinoid receptor 2 (CB2). Vicasinabin has the potential for the research of human diseases including chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and other related diseases (extracted from patent US20130116236A1).

Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family.

Mopivabil is the antagonist of angiotensin II receptor.

Mepixetil is a potent antagonist of angiotensin II receptor.

Azilsartan mopivabil is the potent antagonist of angiotensin II receptor.

Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A).

KUC-7322, a selective β3 -adrenoceptor agonist, is the active form of ritobegron. Ritobegron decreases intravesical pressure with minimal effects on the cardiovascular system.

Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.

ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.

Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.

Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

DC260126, a small-molecule antagonist of GPR40.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity.

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]