AChR

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Anisodine is an inhibitor of muscarinic acetylcholine receptors (mAChR) with neuroprotective activity, used in research on multiple myeloma and metastatic breast cancer.

Xanomeline tartrate (LY 246708 tartrate) is an M1 and M4 mAChR agonist with antipsychotic-like activity that improves cognition and can be used in studies of schizophrenia and Alzheimer's disease.

beta-Amyrone (β-Amyron) has antifungal activity against Chikungunya virus replication with an EC50 of 86 uM. beta-Amyrone has anti-inflammatory activity through inhibiting the expression of COX-2. beta-Amyrone exhibits anti-α-glucosidase inhibitory activity and moderate AChE activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity.

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist that binds to DREADD receptor subtypes [hM3Dq] and [hM4Di] with Ki values of 6.3 nM and 4.2 nM, respectively.

Tematropium (CDDD3602) possesses anticholinergic effects and can be used in neurological studies.

Pilocarpine Hydrochloride (NSC 5746 HCl) is an M3-type muscarinic acetylcholine receptor agonist. Pilocarpine Hydrochloride was used to make an experimental model of epilepsy.

Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

LY2033298, a positive allosteric modulator of muscarine M4 receptor, enhances the inhibitory effect of oximoline on light-induced phase shift in circadian activity in hamsters and can be used in neurosystem-related diseases.

ICL-CCIC-0019, an inhibitor of choline kinase alpha (ChoKα), induces G1 arrest, endoplasmic reticulum stress, and apoptosis in cancer cell lines.

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

Clozapine N-oxide dihydrochloride, a derivative of Clozapine and an agonist of human muscarinic design receptors (DREADDs), crosses the blood-brain barrier and activates DREADD receptors hM3Dq and hM4Di.

PF-4348235 HCl (β2AR/M-receptor agonist-2 HCl) is a muscarinic M3 receptor antagonist (Ki: 0.73 nM) and β2 adrenergic receptor agonist (MABA, EC50: 3.7 nM). PF-4348235 HCl is also a bronchial BM213 acetate is a bronchodilator used to study cardiovascular and respiratory diseases such as chronic obstructive pulmonary disease (COPD).

α-Conotoxin GI acetate is a competitive antagonist of the muscle-type nicotinic acetylcholine receptors (nAChR).

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) shows human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity, with IC50 values of 0.83 +/- 0.04 microM and 4.20 +/- 0.19 microM, respectively.

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

Spinosad is a naturally-occurring insecticide found in the the soil bacterium S. spinosa. It is a mixture of the macrocyclic lactones spinosyn A and spinosyn D, which act as agonists of insect nicotinic acetylcholinesterase receptors (nAChRs).

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

(R,S)-Anatabine is a minor tobacco alkaloid found in the Solanaceae family of plants, and serves as a specific marker for detecting tobacco use.

Sulfoxaflor (GF 2032) is an agonist of nAChR1 and nAChR2 subtypes and a systemic insecticide that acts on the insect central nervous system. Sulfoxaflor was found to have some effects on peripheral blood lymphocytes and is used to control sap-feeding insects such as brown planthopper, whitefly, peach aphid, and cotton aphid.