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.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

Emraclidine (CVL-231) is a novel, highly selective allosteric modulator of the muscarinic M4 receptor positive receptor for the study of neurological diseases.

Harmalol (Harmidol) is a bioactive beta-carboline and a member of the harmala alkaloids

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.

Asoxime dichloride (Tert-Butyl2-(2-hydroxyethyl)-1-pyrrolidinecarboxylate) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system. Asoxime dichloride involves in modulating immunity response.

Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

3-Bromocytisine ((-)-3-Bromocytisine) is an effective agonist of nAChR (IC50s: 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7).

GTS-21 dihydrochloride (DMBX-anabaseine) is a nAChRs agonist. nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter ACh.

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

Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR TLR4 associations and downstream pathologies.

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).

Mivacurium dichloride (Mivacurium chloride) is a non-depolarising, rapid neuromuscular blocker of short duration, used therefore as anesthetic, to provide skeletal muscle relaxation in minor surgical operations, in emergency surgical procedures of short to intermediate duration and during intubation of the trachea.

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

V-11-0711 HCl is a selective and highly effective choline kinase α (ChoKα) inhibitor that inhibits the catalytic activity of Chk.

Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder.

Methyllycaconitine citrate (MLA) is an α7 neuronal nicotinic acetylcholine receptor (α7nAChR) antagonist that crosses the blood-brain barrier.

SCH-900271 is a potent nicotinic acid receptor for the treatment of dyslipidaemia and is commonly used in the study of mixed hyperlipidaemia and primary hypercholesterolaemia.

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.

GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.

α-Conotoxin Vc1.1 TFA is a peptide isolated from Conus victoriae and a selective nAChR antagonist that inhibits α3α5β2, α3β2 and α3β4, reversing mechanical allodynia in neuropathic pain models and can be used to study neuropathic chronic pain. α-Conotoxin Vc1.1 TFA inhibits human dorsal root ganglion nerve excitability and mouse colon nociception via GABA(B) receptors.

Simpinicline (OC-02) (OC-02) is a highly selective nicotinic acetylcholine receptor (nAChR) agonist that activates the trigeminal parasympathetic pathway and can be used to treat dry eye.

Adenine (6-Aminopurine), a purine derivative, is a nucleobase essential in biochemistry, participating in cellular respiration through ATP, NAD, and FAD, and in protein synthesis as a component of DNA and RNA.

Afacifenacin (SMP-986) fumarate is an M3 muscarinic receptor-selective antagonist used in the study of ischemic heart disease, urinary incontinence and cystitis and other disorders.

CP-810123 is a new alpha 7 nAChR agonist for the treatment of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a acetylcholine transport inhibitor.

Cotinine (NIH-10498) is an alkaloid found in tobacco and is also the predominant metabolite of nicotine.

(Rac)-ABT-202 dihydrochloride is a racemate of ABT-202, a nicotinic acetylcholine receptor (nAChRs) agonist used as an analgesic.

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

Agaricic acid is an adenine nucleotide translocase antagonist.It is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid (Agaricinic Acid) induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.

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.

Anabasine ((S)-Anabasine) is an alkaloid extracted from tobacco, acting as a full agonist of nicotinic acetylcholine receptors (nAChRs) with insecticidal activity. It depolarizes TE671 cells that endogenously express human myotypic nAChRs.

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

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

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

Loganin (Loganoside), an iridoid glucoside, has been reported to be an inhibitor of Cox-1 and also noted to suppress TNF-α formation. This compound also has displayed potent free-radical-scavenging activity and inhibitory effects on melanogenesis.

SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) , the adenosine analogue 9-(Tetrahydro-2-furyl)adenine, inhibited adenylate cyclase activity of crude membrane preparations from catfish (Ictalurus melas) and rat isolated hepatocytes in a non-competitive manner.

9-Cyclopentyladenine (NSC-19486) is an adenylate cyclase inhibitor that blocks cellular morphological differentiation and phosphorylation of specific signaling molecules.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.