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141879 (−)-Lobeline hydrochloride 98%  
N1019   (−)-Nicotine hemisulfate salt ≥95% (TLC), ~35 % (w/v) in H2O (based on free base) Prototype nicotinic acetylcholine receptor agonist; naturally occurring isomer.
SML1236 (−)-Nicotine hydrogen tartrate salt ≥98% (HPLC) Nicotine hydrogen tartrate (NHT) is a biodegradable polymer of chitosan. NHT is considered to be more stable than nicotine. Nicotine is highly addictive drug and is indirectly but strongly associated with tobacco related diseases. It helps to discontinue smoking. Nicotine might serve as a therapeutic agent in treating Alzheimer’s disease, Parkinson’s disease and ulcerative colitis.
Prototype nicotinic acetylcholine receptor agonist; naturally occurring isomer.
N3876 (−)-Nicotine ≥99% (GC), liquid Nicotine binds to nicotinic acetylcholine receptors and exhibit both neuroprotective and neurotoxic effects on the developing brain. It is associated with lung cancer development and reduces the efficiency of chemotherapeutic agents. In addition, nicotine has an ability to impair phagocytic host defense and also increase reactive oxygen species (ROS) associated injury. It also stops Akt/ protein kinase B (PKB) deactivation and decreases spontaneous death of neutrophils. Nicotine is used to treat Alzheimer′s and Parkinson′s disease.
Prototype nicotinic acetylcholine receptor agonist; naturally occurring isomer.
E1145 (±)-Epibatidine dihydrochloride hydrate ≥98% (HPLC), powder The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.
M104 (±)-Muscarine chloride hydrate ≥98% (HPLC) Muscarinic acetylcholine receptor agonist; originally isolated from Amanita muscaria.
N0267 (±)-Nicotine ≥99% (TLC), liquid (±)-Nicotine is a tertiary amine compound that is predominantly present in tobacco. It binds to the nicotinic cholinergic receptors of the brain, autonomic ganglia and neuromuscular junction. Nicotine allosterically regulates a number of biological events such as production of growth hormone, dopamine, adrenocorticotropic hormone and prolactin. Nicotine absorption across biological membranes is pH sensitive, which alters its ionization state. Absorption of nicotine is shown to be higher at alkaline pH, when it remains unionized. Nicotine metabolism occurs extensively in the liver and it can cross placenta.
N3018 (±)-Nornicotine ≥98% (TLC), liquid Nicotinic acetylcholine receptor agonist; active metabolite of nicotine; tobacco alkaloid.
M6532 (+)-Muscarine chloride ~95% (TLC), powder Prototype muscarinic acetylcholine receptor agonist; active enantiomer.
5.05227 (-)-Cytisine - CAS 485-35-8 - Calbiochem Primary Target
Reversible: yes
Target Ki: 2, 5890, 480, 329, and 492 nM at &alpha
481975 (--)-Nicotine, Ditartrate - CAS 65-31-6 - Calbiochem Potent agonist of the nicotinic acetylcholine receptor. Cell permeable: no
Primary Target
Nicotinic acetylcholine receptor
Product does not compete with ATP.
Reversible: no
5.05412 1,1-Dimethyl-4-phenylpiperazinium iodide - CAS 54-77-3 - Calbiochem Primary Target
D5891 1,1-Dimethyl-4-phenylpiperazinium iodide ≥98% (TLC or titration), powder Nicotinic acetylcholine receptor agonist.
SML1167 4BP-TQS ≥98% (HPLC) 4BP-TQS is an atypical agonist of a7-nAChR that binds to the receptor in an intrasubunit cavity, and activates the channel via a mechanism that is distinct from conventional agonists. Maximal activation of a7-nAChR by 4BP-TQS is eight fold greater than activation by a maximum dose of acetylcholine (Ach), and 4BP-TQS can poteniate an EC10 concentration of ACh to invoke a response that is 540-fold higher than the maximal dose of ACh alone.
5.05413 5-Iodo-A-85380 dihydrochloride hydrate - CAS 213550-82-4 - Calbiochem Primary Target
α4β2 nAChR
SML0023 5-Iodo-A-85380 dihydrochloride hydrate ≥98% (HPLC) 5-Iodo-A-85380 increases the influx of extracellular Ca+2 in rat cortical neurons and exhibits protective effects against glutamate-induced neurotoxicity. Studies reveal that it also activates α6β2 nicotinic acetylcholine receptors.
5-Iodo-A-85380 is a highly selective α4β2 nicotinic receptor agonist. The Ki values for binding to the human and rat receptors are 12 and 10 pM, respectively.
SML1487 ABT-089 dihydrochloride ≥98% (HPLC) ABT-089 (Pozanicline) is a subtype-selective neuronal nicotinic receptor partial agonist binding primarily to the α4β2 and also α6β2 subtypes. It has been investigated for alleviating symptoms of nicotine withdrawal including cognitive deficits and anxiety.
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
SML0787   AC 42 ≥98% (HPLC) AC-42 is a specific agonist of the muscarininc M1 receptor (pEC50 = 6.54) with little or no activity against other muscarinic receptor family members. AC-42 binds to an allosteric site adjacent to the adjacent to the orthosteric, acetylcholine binding site.
5.05821 AF-DX 116 - CAS 102394-31-0 - Calbiochem Primary Target
SML0180 Aceclidine hydrochloride ≥98% (HPLC) Aceclidine at a concentration of 5 and 50 μg is capable of enhancing the outflow facility, following ciliary muscle disinsertion.
Aceclidine hydrochloride is a parasympathomimetic drug with weak anticholinesterase activity. It acts on cholinergic nerve-endings, lowers intraocular pressure and potent therapeutic agent for open-angle glaucoma.
Aceclidine is a non-selective muscarinic acetylcholine receptor partial agonist that is effective in reducing intraocular pressure.
A2251 Acetyl-β-methylcholine chloride ≥98% (TLC), powder Metabolically stable analog of acetylcholine; muscarinic agonist. Its ability to constrict airway smooth muscle is used to assess bronchial reactivity in the laboratory and clinically.
A6500 Acetylcholine bromide ≥99% Endogenous neurotransmitter at cholinergic synapses; amplifies action potential of the sarcolemma thereby inducing muscle contractions.
A6625 Acetylcholine chloride ≥99% (TLC) Acetylcholine chloride, injected at 20 mg/kg body weight, reduces mortality and plasma proinflammatory cytokines in mice with experimentally-induced sepsis . The cholinergic anti-inflammatory mechanism is probably mediated by interaction of acetylcholine with α7n cholinoreceptor on monocytes, macrophages, and neutrophils, which decreases the levels of proinflammatory cytokines such as TNF-α, IL-1β, and IL-6.
A7000 Acetylcholine iodide ≥97% Endogenous neurotransmitter at cholinergic synapses; amplifies action potential of the sarcolemma thereby inducing muscle contractions.
A2394   Acetylcholine perchlorate  
A5626 Acetylthiocholine chloride ≥99% (TLC), powder Acetylcholinesterase (AChE) enzyme plays an important physiological role in the neurotransmission process.
Acetylcholinesterase substrate and nicotinic acetylcholine receptor agonist.
A5751 Acetylthiocholine iodide ≥98% (TLC), powder or crystals  
A140 Arecaidine propargyl ester hydrobromide solid Potent muscarinic acetylcholine receptor agonist exhibiting slight selectivity for M2 receptors; inactive at nicotinic receptors.
5.05773 Bethanechol Chloride - CAS 590-63-6 - Calbiochem  
212385-M Carbachol - CAS 51-83-2 - Calbiochem An unsubstituted carbamoyl ester that acts as an agonist for nicotinic and muscarinic acetylcholine receptors. Primary Target
Agonist for nicotinic and muscarinic acetylcholine receptors
C4382 Carbamoylcholine chloride ≥98% (titration), crystalline Carbachol elicits tear fluid secretion by interacting with muscarinic receptors. It is an analog of acetylcholine and an antiglaucoma drug. In ciliary processes, carbachol along with nitric oxide (NO) regulates Na+ and K+-ATPase activity. It stimulates insulin vesicles transport to the secretory site to increase insulin secretion.
Non-selective cholinergic agonist that is resistant to the action of cholinesterases; inhibits apoptotic death of cultured neurons, and may induce apoptosis in thymocytes.
C5259 Carbamyl-β-methylcholine chloride ≥99% (TLC), crystalline Carbamyl-β-methylcholine has a selective action on urinary bladder and intestine. It induces smooth muscle tension in the bladder. Its main function is to induce detrusor muscle action, mediated by postganglionic parasympathetic effector cells. Nausea, flushing, sweating, abdominal cramps are some of the side effect caused by carbamyl-β-methylcholine.
SML0007 Cevimeline hydrochloride hemihydrate ≥95% (HPLC, NMR) Cevimeline is a muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and is used to treat the symptoms of dry mouth.
Cevimeline stimulates the peripheral muscarinic acetylcholine receptors of salivary glands and increases the concentration of Ca+2 in parotic acini and duct cells of rats. It thus acts as therapeutic agent for xerostomia.
C4740 Cisapride monohydrate ≥98% (HPLC), solid 5-HT4 serotonin receptor agonist.
C2899 Cytisine ≥99%, powder Potent agonist at α3β4 and α7 nicotinic acetylcholine receptors and partial agonist at α4β2 nicotinic acetylcholine receptors.
D7938 DBO-83 solid Novel nicotinic acetylcholine receptor agonist, structurally related to epibatidine, with antinociceptive properties in rodents.
D1260 Decamethonium bromide crystalline Decamethonium serves as a muscle relaxant and is also a neuromuscular blocking agent. It has a molecular weight of 258.4.
Nicotinic acetylcholine receptor partial agonist and neuromuscular blocking agent; depolarizes striated muscles and blocks their activity.
E152 Epiboxidine hydrochloride Potent nicotinic acetylcholine receptor agonist; analog of epibatidine
SML0326 GTS-21 ≥97% (HPLC) GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.
SML0790   Iperoxo ≥98% (HPLC) Iperoxo forms an important building block for the class of G protein-coupled receptors modulators. Iperoxo specifically binds to the orthosteric site of the muscarinic acetylcholine receptor. It has a higher efficacy than the endogenous agonist acetylcholine.
Iperoxo is a muscarinic acetylcholine receptor superagonist. The pEC50 values for G-protein activation by acetylcholine and iperoxo in CHO cells expressing recombinant human M2 receptors are 7.6 and 10.1, respectively.
K4269 KAB-18 hydrochloride ≥98% (HPLC), powder KAB-18 is a negative allosteric modulator (NAM) at Hα2 β4 nChR nicotinic cholinergic receptors.
SML0870   LY 2087101 ≥98% (HPLC) LY 2087101 is a selective positive allosteric potentiator of α7 and α4β2 nicotinic acetylcholine receptors (nAChRs). LY 2087101 was shown to not enhance the activity of α3β4 subtype nAChRs.
SML0243 ML169 ≥98% (HPLC) ML169 is a positive allosteric modulator (PAM) of the muscurinic acetycholine receptor M1 (CHRM1). ML169 does not cross react with other muscarinic receptors and is able to penetrate the blood brain barrier.
C7041 McN-A-343 ≥98% (TLC) M1 muscarinic acetylcholine receptor agonist.
5.05983 NS1738 - CAS 501684-93-1 - Calbiochem Primary Target
α7 AChR
A6706 O-Acetyl-L-carnitine hydrochloride ≥99% (titration), powder Endogenous mitochondrial metabolite that transports acetyl groups across the mitochondrial membrane. Exogenous acetylcarnitine enhances mitochondrial function in aged rats. As an acetate donor to coenzyme A, it increases the central and peripheral acetylcholine synthesis and function. Acetylcarnitine has antinociceptive activity that may be mediated by enhanced activity of muscarinic cholinergic receptors or mGlu2 glutamate receptors.
O100 Oxotremorine M solid Nonselective muscarinic acetylcholine receptor agonist.
O9126 Oxotremorine sesquifumarate salt ≥98% (HPLC), solid Oxotremorine sesquifumarate salt is a muscarinic acetylcholine receptor agonist with preference for the M2 receptor.
PZ0323 PF-06767832 ≥98% (HPLC) PF-06767832 is a cell permeable, potent and selective M1 muscarinic acetylcholine receptor Positive Allosteric Modulator (PAM). Studies have shown that PF-06767832 potentiates the activity of acetylcholine (Ach) in vitro.
PZ0359 PF-06827443 ≥98% (HPLC) PF-06827443 is a otent, low clearance, orally bioavailable, and CNS penetrant muscarinic M1-selectivepositive allosteric modulator (PAM) with minimal agonist activity.
5.05316 PHA-543,613 - CAS 478149-53-0 - Calbiochem Primary Target
α7 nAChR
PZ0135 PHA-543613 ≥98% (HPLC) PHA-543613 is a potent selective α7 nAChR agonist. Nicotinic acetylcholine receptors are ligand-gated ion channels activated by nicotine, expressed in multiple tissues, with high functional expression in brain. The homomeric subtype α7 is a potential therapeutic target for cognitive deficits in schizophrenia and Alzheimer′s disease. PHA-543613 is active in both in vitro (binding, calcium flux, patch-clamp) and in vivo (auditory gating, novel object recognition) assays.
5.05278 PNU 282987 - CAS 123464-89-1 - Calbiochem Primary Target
α7 nAChRs
Reversible: yes
P6499 PNU-282987 hydrate solid, ≥98% (HPLC) Decreased expression of a homomeric alpha7 nicotinic acetylcholine receptor (nAChR) is connected with inability to process sensory information in schizophrenia. PNU-282987 is a novel selective agonist of the alpha7 nAChR that evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity. The alpha7 nAChR agonist PNU-282987 improves auditory gating and enhances hippocampal oscillatory activity. These results provide further support for the concept that drugs that selectively activate alpha7 nAChRs may offer a novel, potential pharmacotherapy in treatment of schizophrenia.
PNU-282987 is an agonist of nicotinic α-7 acetylcholine receptor (nAChRα7). It helps to decrease acute lung injury (ALI), stimulated by lipopolysaccharide (LPS). PNU-282987 can increase GABAergic synaptic activity in brain slices and helps to bring back auditory gating deficits in anesthetized rats.
SML1587 Perlapine ≥98% (HPLC) Perlapine is a potent and selective agonist of hM3Dq DREADD (Designer Receptors Exclusively Activated by Designer Drugs), which does not activate the native human M3 receptor. Perlapine is a neuroleptic agent that exhibits sedative and sleep-promoting properties.
P6503 Pilocarpine hydrochloride ≥98% (titration), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
Pilocarpine is alkaloid isolated from the shrub Pilocarpus species. It comprises imidazole ring and γ- lactone rings in its structure. It has cholinergic potential and it stimulates the parasympathetic system. Pilocarpine is also effective for treating glaucoma. It stimulates ciliary muscle contraction by binding to muscarinic M3 receptors. It is effective in treating corneal dryness in Sjogren′s syndrome. It is a secretagogue, which improves salivary secretions in Xerostomia or a dry mouth condition in Sjogren′s syndrome patients and in radiotherapy patients with head and neck carcinoma.
P6628 Pilocarpine nitrate salt ≥98% (HPLC) Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
Pilocarpine is a cholinergic muscarinic agonist, useful in inducing epilepsy in animal models. It is specially used to study the pathogenesis of epileptogenesis and pharmacoresistant epilepsy. Pilocarpine application is more popular among the rat and mice models.
5.05228 S 24795 - CAS 304679-75-2 - Calbiochem Primary Target
→7 nAChRs
SML1111 S 24795 ≥98% (HPLC) S 24795 is a selective partial agonist for the α7-subtype of nicotinic acetylcholine receptor (nAChR). S 24795 was shown to be effective at improving learning and memory in various animal models relevant to Alzheimer’s disease and age-related memory loss, and is used in investigating the roles of α7 nAChRs in aging, learning, memory, and cognition.
V5015 VU0152100 ≥98% (HPLC) Positive allosteric modulator of muscarinic choline receptor M4. Potentiates activation by acetylcholine, but posesses no intrinsic agonist activity alone.
PZ0004 Varenicline tartrate ≥98% (HPLC) Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
X2754 Xanomeline L-tartrate hydrate ≥98% (HPLC) Xanomeline L-tartate is a M1 muscarinic receptor agonist.
5.05816 Xanomeline Oxalate - CAS 141064-23-5 - Calbiochem