Antagonists

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S7882 (−)-Scopolamine N-butyl bromide ≥98% (TLC), powder Scopolamine is an anti-muscarinic and cholinolytic alkaloid that inhibits parasympathetic-cholinergic system.5 The central effects include hallucinations, disorientation, restlessness and euphoria.6 Scopolamine disturb the stimulus detection performance in rats by interfering with the reticular cholinergic pathways.7
S1875 (−)-Scopolamine hydrobromide trihydrate ≥98% (HPLC), powder Competitive nonselective muscarinic acetylcholine antagonist. Scopolamine-induced amnesia in laboratory animals is a commonly-used model of memory deficit.
S1013 (−)-Scopolamine hydrochloride ≥90% (HPLC), powder Competitive nonselective muscarinic acetylcholine antagonist. Scopolamine-induced amnesia in laboratory animals is a commonly-used model of memory deficit.
S8502 (−)-Scopolamine methyl bromide ≥98% (HPLC), powder Scopolamine is an anti-muscarinic and cholinolytic alkaloid that inhibits parasympathetic-cholinergic system.7 The central effects include hallucinations, disorientation, restlessness and euphoria.8 Scopolamine disturb the stimulus detection performance in rats by interfering with the reticular cholinergic pathways.9
C002 (±)-Quinuclidinyl benzilate powder Nonselective muscarinic acetylcholine receptor antagonist.
C003 (R)-(−)-3-Quinuclidinyl benzilate Nonselective muscarinic acetylcholine receptor antagonist. More potent enantiomer of QNB.
SML0255 4-DAMP ≥98% (HPLC) 4-DAMP is a M3 preferring cholinergic receptor antagonist.
T1516 DL-Trihexyphenidyl hydrochloride solid DL-trihexyphenidyl hydrochloride (Benzhexol hydrochloride) is known to function as an antimuscarinic agent and a centrally acting anticholinergic. It can be used for controlling the symptoms of all Parkinsonism types, such as the idiopathic, and postencephalitic arteriosclerotic forms. Benzhexol hydrochloride exerts inhibitory functions on the parasympathetic nervous system.
H9002 L-Hyoscyamine ≥98% (TLC), powder Competitive antagonist at post-ganglionic synapses and on smooth muscle
SML0457 AE9C90CB ≥98% (HPLC) AE9C90CB is a muscarinic acetylcholine receptor antagonist with 20-fold selectivity for M3 receptor subtypes compared to M2. In an in vivo assay, AE9C90CB was approximately 5 times more selective for inhibiting carbachol-induced urinary bladder contraction, compared to saliva production.
SML0435 AF-DX 116 ≥98% (HPLC) AF-DX 116 is a selective M2 muscarinic acetylcholine receptor antagonist.
SML0620   AF-DX 384 Free Base ≥98% (HPLC) AF-DX 384 Free Base is a potent muscarinic M2/M4 receptor selective antagonist (pKi values are 8.22, 8.00, 7.51, 7.18 and 6.27 at human M2, M4, M1, M3 and M5 receptors respectively).
SML0252 Anisodamine ≥98% (HPLC) Anisodamine is a muscarinic receptor antagonist. Anisodamine is a naturally occurring atropine derivative isolated from Scopolia Tangutica Maxim plant indigenous to Tibet.
A0257 Atropine sulfate salt monohydrate ≥97% (TLC), crystalline Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
A0132 Atropine ≥99% (TLC), powder Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
SML0847 Benztropine mesylate ≥98% (HPLC) Benztropine mesylate is a centrally acting muscarinic acetylcholine receptor antagonist and dopamine transporter (DAT) inhibitor (IC50 = 118 nM). Benztropine mesylate has been used to treat the symptoms of Parkinson′s disease and is currently in clincial trials for chronic back pain.
SML0319 Caramiphen hydrochloride ≥98% (HPLC) Caramiphen is an anti-muscarinic similar to atropine; muscarinic acetylcholine receptor antagonist. Caramiphen is commonly used as a cough suppresant, but is also administered for the treatment of Parkinson′s disease. The compound has also been shown to have anti-depressant properties that may involve inhibition of G protein-coupled inwardly rectifying potassium channel GIRK.
C2108 Condelphine ≥95%, solid Nicotinic acetylcholine receptor antagonist.
SML0845 DAU-5884 ≥98% (HPLC) DAU-5884 is a M3-selective muscarinic receptor antagonist. The compound DAU-5884 blocks cobrotoxin-induced transient A-type K(+) currents in dorsal root ganglion neurons.
SML1102 Darifenacin hydrobromide ≥98% (HPLC) Darifenacin hydrobromide is an antispasmodic muscarinic antagonist, selective for blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. Darifenacin hydrobromide has 9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4. Darifenacin is used clinically to treat urinary incontinence and overactive bladder syndrome.
D7909 Dicyclomine hydrochloride ≥99% (TLC), powder Competitive muscarinic acetylcholine receptor antagonist.
D7689   Diquine ≥98%, solid A nicotinic cholinoreceptor antagonist at the neuromuscular junction; curare-like ganglioblocker.
F6301 Fluorocurarine chloride ≥97% (TLC), from Vinca erecta, solid Short-acting selective sympathetic ganglioblocker with weak antagonist activity on the nicotinic receptor at the neuromuscular junction; hypotensive.
371780 GP Antagonist-2A - Calbiochem The GP Antagonist-2A controls the biological activity of GP. This small molecule/inhibitor is primarily used for Neuroscience applications.  
G8134 Gallamine triethiodide ≥98% (TLC), powder, muscarinic receptor antagonist Muscle relaxant; allosteric muscarinic receptor antagonist with an order of potency of M2 > M1 = M4 > M3 = M5. Ligand for the peripheral anionic binding site of acetylcholinesterase.
SML0029 Glycopyrrolate ≥98% (HPLC) Glycopyrrolate is long-acting muscarinic antagonist (LAMA). It is kinetically selective muscarinic M3 receptor antagonist.
H0879 Hexamethonium bromide Preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier only at high doses.
H2138 Hexamethonium chloride solid (hygroscopic) Preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier only at high doses.
SML1821 Imidafenacin hydrochloride ≥95% (HPLC) New Imidafenacin is a potent antimuscarinic agent that exhibits selectivity toward muscarinic M3 receptors with Kb of 0.317 nM. Imidafenacin is used for treating overactive bladder.
I1637 Ipratropium bromide monohydrate ≥98% (TLC), powder Nonselective muscarinic acetylcholine receptor antagonist; bronchodilator.
SML1861 J104129 fumarate ≥98% (HPLC) J104129 is a muscarinic M3 receptor antagonist greater than 100-fold selectivity for M3 over M2 receptors. Its Ki for M3 receptors = 4.2 nM compared to a Ki of 490 nM for M2 receptors. J-104129 showed potent bronchodilator activity in animal studies.
L9919 LY2033298 ≥98% (HPLC) LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.
SML0130 Loxiglumide ≥97% (HPLC) Loxiglumide is a small-molecule antagonist of the cholecystokinin receptor CCKA. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.
M3184 MG 624 ≥98% Nicotinic acetylcholine receptor antagonist; selectively inhibits neuronal nicotinic α-bungarotoxin sensitive receptors that contain the α7 subunit.
M9020 Mecamylamine hydrochloride Noncompetitive nicotinic acetylcholine receptor antagonist; preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier.
M105 Methoctramine hydrate ≥97% (NMR), solid Methoctramine is a selective M2 muscarinic receptor antagonist at nM concentrations. At mM concentrations, methoctramine directly inhibits the high affinity GTPase activity of G proteins. The increase in calcium and arachidonic acid release were attenuated by the M2 receptor antagonist methoctramine, but not by the M3 receptor antagonist p-fluoro-hexahydro siladifenidol.
Methoctramine is a selective M2 muscarinic receptor antagonist at nM concentrations. At mM concentrations, methoctramine directly inhibits the high affinity GTPase activity of G proteins. In oesophageal muscle, acetylcholine-mediated increase in calcium and arachidonic acid release were reduced by the M2 receptor antagonist, methoctramine. Methoctramine infused bilaterally in the dorsolateral striatum, considerably enhanced memory in cognitively impaired aged rats. Methoctramine plays a vital role in muscarinic receptor classification.
5.05208 Methyllycaconitine Citrate - CAS 21019-30-7 - Calbiochem  
M168 Methyllycaconitine citrate salt from Delphinium brownii seeds, ≥96% (HPLC) Potent and specific nicotinic receptor antagonist that binds to neuronal α-bungarotoxin sites.
N5537 NDNI hydriodide solid, (The product is pure based on CHN, NMR, MS) Highly selective α4β2 nicotinic receptor antagonist
75517 Orphenadrine hydrochloride ≥98.0% (AT) Muscarinic receptor antagonist; H1 histamine receptor antagonist; muscle relaxant. Orphenadrine has also been reported to inhibit the noradrenergic transporter and to block the NMDA receptor ion channel.
SML1454 Otilonium bromide ≥98% (HPLC) Otilonium Bromide is a muscarinic receptor antagonist (antimuscarinic). Otilonium Bromide is a quaternary ammonium salt that exerts spasmolytic action selective on the distal gastrointestinal tract. It is used world-wide for the treatment of irritable bowel syndrome (IBS).
O2881 Oxybutynin chloride ≥98% (TLC), powder Muscarinic acetylcholine receptor antagonist; inhibits proliferation of bladder smooth muscle cells, perhaps by downregulation of growth promoting genes.
SML1848 PCS1055 dihydrochloride ≥98% (HPLC) PCS1055 is a potent and selective muscarinic M4 acetylcholine receptor competitive antagonist that exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 was originally described as a potent electric eel AChE inhibitor (IC50 = 22 nM) and less potent at human AChE (IC50 = 120 nM).
5.05226 Pancuronium Dibromide - CAS 15500-66-0 - Calbiochem  
P1918 Pancuronium bromide Aminosteroidal neuromuscular blocking agent; skeletal muscle relaxant
SML1636   Pipecuronium bromide ≥98% (HPLC) Pipecuronium is a bisquaternary aminosteroid muscle relaxant which acts at the nicotinic acetylcholine receptor of the neuromuscular junction. Pipecuronium is a non-depolarizing neuromuscular blocking agent.
P7412 Pirenzepine dihydrochloride ≥98% (TLC), powder Selective M1 muscarinic acetylcholine receptor antagonist.
P3794 Procyclidine hydrochloride Atropine-like antispasmodic
P8891 Propantheline bromide ≥97% (TLC), powder Inhibits action of acetylcholine at post-ganglionic synapses; muscarinic acetylcholine receptor antagonist; antispasmodic; reduces gastric acid secretion.
SML0602   Propiverine hydrochloride ≥98% (HPLC) Propiverine is an antimuscarinic drug used for the treatment of overactive blaqdder and urinary incontinence. Propiverine and/or its metabolites also have calcium channel blocking properties in addition to antimuscarinic activity, which may contribute to the clinical activity.
Q0255 Quirestine ≥98% (TLC), powder Nicotinic acetylcholine receptor antagonist. Potent short-acting ganglioblocker.
Q108 R(−)-Quinuclidinyl benzilate methiodide crystalline Nonselective muscarinic acetylcholine receptor antagonist.
R5155 Rocuronium bromide ≥98% (perchloric acid titration) Aminosteroid; neuromuscular blocker for anaesthesia
Rocuronium Bromide is a fumarate, non-depolarizing, neuromuscular blocking agent. It is rapid-acting, relaxes the skeletal muscle and decreases oxygen consumption during surgery. It competes with acetylcholine and bind to cholinergic receptors at neuromuscular junctions.
S8251 Succinylcholine chloride dihydrate 98.0-102.0%, solid Cholinergic antagonist which induces a long-lasting depolarization of the acetylcholine neuron membrane; neuromuscular blocking agent.
Succinylcholine is a cholinergic antagonist and a neuromuscular blocking agent. It induces depolarization of acetylcholine receptors on the muscle membrane and efflux of potassium from the muscle that leads to hypokalemia in individuals with upregulated expression of acetylcholine receptors.3
T5576 TMPH hydrochloride solid, (Product is pure based on CHN, NMR and MS results) 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH) is a potent inhibitor of neuronal nicotinic receptors. Evaluation of nicotinic acetylcholine receptor (nAChR) subunits expressed in Xenopus laevis oocytes indicated that TMPH can produce a potent and long-lasting inhibition of neuronal nAChR formed by the pairwise combination of the most abundant neuronal alpha (i.e., alpha3 and alpha4) and beta subunits (beta2 and beta4), with relatively little effect, because of rapid reversibility of inhibition, on muscle-type (alpha1beta1gammadelta) or alpha7 receptors. However, the inhibition of neuronal beta subunit-containing receptors was also decreased if any of the nonessential subunits alpha5, alpha6, or beta3 were coexpressed. This decrease in inhibition is shown to be associated with a single amino acid present in the second transmembrane domain of these subunits. TMPH abilitty to relate the diverse central nervous system effects to specific nAChR subtypes makes it a useful tool for studying the functional roles of nAChR.
T122 Telenzepine dihydrochloride hydrate solid, ≥98% (HPLC) Telenzepine is an analog of pirenzepine and inhibits the secretion of gastric acid. It is an antagonist to M1-receptor and targets the oxyntic gastric glands and the salivary glands.
T4819 Tempoxime hydrochloride ≥98% (TLC) Neuronal nicotinic AChR antagonist and potent ganglioblocker.
PZ0009 Tolterodine L-tartrate ≥98% (HPLC) Tolterodine L-tartrate is a bladder-specific muscarinic antagonist.
T9778 Tropicamide solid M4 muscarinic acetylcholine receptor antagonist.
T2379 Tubocurarine hydrochloride pentahydrate ≥97% Muscle relaxant; nicotinic acetylcholine receptor antagonist; can induce neuromuscular paralysis.
V3765 VU0255035 hydrate ≥98% (HPLC) VU0255035 is the first highly selective antagonist at the orthosteric site of the M1 receptor (75-fold selective for M1 relative to other muscarininc subtypes and devoid of activity at other GPCRs, ion channels, transporters and kinases). There are no highly selective M1 muscarinic receptor antagonists. The existing non-selective drugs do not permit direct evaluation of the role of M1 receptors in CNS fucntions and do not premit therapeutic targeting of M1 receptors in various disease states in which M1 receptors are implicated (epilepsy, Parkinson′s disease, attention and cognitive disorders, dystonia, etc).
SML0182 bPiDl hydrate ≥98% (HPLC) bPiDI is an α6β2-specific antagonist that inhibits nicotine-evoked and endogenous dopamine release from rat striatal slices (IC50 = 150 nM, Imax = 55%). bPiDI treatment decreases nicotine self-administration, and nicotine-induced locomotor activity in rats.
H127 p-Fluorohexahydro-sila-difenidol hydrochloride powder, ≥98% (HPLC) High affinity M3 muscarinic acetylcholine receptor antagonist.