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Acetylcholine Receptors (Muscarinic) / Related Products
You are here: Product Lines > Signal Transduction > Receptors > G-Protein Coupled Receptors & Ligands / Related Products > Acetylcholine Receptors (Muscarinic) / Related Products
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ALX-550-101 Revised 16-Apr-05
AIDA
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SYNONYMS (±)-1-Aminoindane-1,5-dicarboxylic acid
UPF 523
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-101-M005   5 mg 35.00 USD Add To Cart
ALX-550-101-M025   25 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C11H11NO4
MW: 221.2
CAS NUMBER: 168560-79-0
PURITY: ≥96%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent and selective ligand for group I mGluRs. Shows no effect on group II or group III mGluRs. Has no effect on ionotropic glutamate receptors.
Product Specific Literature References
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors: R. Pellicciari, et al.; J. Med. Chem. 38, 3717 (1995) Abstract
mGluR modulation of post-traumatic neuronal death: role of NMDA receptors: A.G. Mukhin, et al.; Neuroreport 8, 2561 (1997) Abstract
Class I mGlu receptor antagonist 1-aminoindan-1,5-dicarboxylic acid blocks contextual but not cue conditioning in rats: K.S. Nielsen, et al.; Eur. J. Pharmacol. 326, 105 (1997) Abstract
Pharmacological characterization of 1-aminoindan-1,5-dicarboxylic acid, a potent mGluR1 antagonist: F. Moroni, et al.; J. Pharmacol. Exp. Ther. 281, 721 (1997) Abstract
Induction of LTD by activation of group l mGluR in the denate gyrus in vitro: N. Camodeca, et al.; Neuropharmacology 38, 1597 (1999) Abstract
Metabotropic G-protein-coupled glutamate receptors as therapeutic targets: R. Pellicciari & G. Costantino; Curr. Opin. Chem. Biol. 3, 433 (1999), (Review) Abstract
1-Aminoindan-1,5-dicarboxylic acid and (S)-(+)-2-(3'- carboxybicyclo[1.1.1] pentyl)-glycine, two mGlu1 receptor-preferring antagonists, reduce neuronal death in in vitro and in vivo models of cerebral ischaemia: D.E. Pellegrini-Giampietro, et al.; Eur. J. Neurosci. 11, 3637 (1999) Abstract
Evaluation of agonists and antagonists acting at Group I metabotropic glutamate receptors in the thalamus in vivo: T.E. Salt, et al.; Neuropharmacology 38, 1505 (1999) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
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Acetylcholine Receptors (Muscarinic) / Related Products
 
 
ALX-550-143 Revised 19-Aug-02
Benztropine . mesylate
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Acetylcholine Receptors (Muscarinic) / Related Products
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ALX-550-143-G001   1 g 20.00 USD Add To Cart
Product Specification
FORMULA: C21H25NO . CH3SO3H
MW: 307.4 . 96.1
CAS NUMBER: 132-17-2
MERCK INDEX: 14: 1121
PURITY: ≥99%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.

Product Description
Muscarinic acetylcholine receptor antagonist. Inhibits the dopamine transporter.
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Dopaminergics & Dopamine Receptors / Related Products
 
 
ALX-550-046 Revised 14-May-03
4-DAMP methiodide
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SYNONYMS 4-Diphenylacetoxy-N-methylpiperidine methiodide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Acetylcholine Receptors (Muscarinic) / Related Products
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ALX-550-046-M005   5 mg 20.00 USD Add To Cart
ALX-550-046-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C21H26NO2I
MW: 451.4
CAS NUMBER: 1952-15-4
PURITY: ≥99.5%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.

Product Description
M3 muscarinic receptor antagonist.
Product Specific Literature References
A further search for selective antagonists at M2-muscarinic receptors: R.B. Barlow & M.K. Shepherd; Br. J. Pharmacol. 89, 837 (1986) Abstract
 
 
ALX-550-099 Revised 25-Feb-08
S-(+)-Dexetimide . hydrochloride
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SYNONYMS R16 470
(S)-(+)-3-Phenyl-1'-(phenylmethyl)-[3,4'-bipiperidine]-2,6-dione . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cholinergics / Related Products
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ALX-550-099-M005   5 mg 20.00 USD Add To Cart
Product Specification
FORMULA: C23H26N2O2 . HCl
MW: 362.5 . 36.5
CAS NUMBER: 21888-98-2
MERCK INDEX: 14: 2945
PURITY: ≥99%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO, methanol, water or DMF.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reference compound for research involving the anticholinergic or muscarinic action of drugs. Binds to the muscarinic receptor with a 1000-fold higher affinity than its optical isomer, R(-)-levetimide . HCl.
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Acetylcholine Receptors (Muscarinic) / Related Products
 
 
ALX-550-400 Revised 16-Jan-06
Dimethyl-W84 dibromide
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SYNONYMS N,N’-Bis[3-(1,3-dihydro-5-methyl-1,3-dioxo-2H-isoindol-2-yl)propyl]-N,N,N’,N’-tetramethyl-1,6-hexanediamminium dibromide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Acetylcholine Receptors (Muscarinic) / Related Products
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ALX-550-400-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C34H48Br2N4O4
MW: 736.6
CAS NUMBER: 402475-33-6
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, water or aqueous buffer.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Avoid freeze/thaw cycles.

Product Description
Very potent allosteric modulator of muscarinic receptors, selective for M2-receptors. Retards the dissociation of the antagonist N-methylscopolamine. Affinity for the free receptor is about 10-fold higher than with W84 (Prod. No. ALX-550-399). pKA=7.08, p(αKA)=6.75, pEC50,diss=6.77.
Product Specific Literature References
Identification of a [3H]Ligand for the common allosteric site of muscarinic acetylcholine M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 54, 139 (1998) Abstract; Full Text
Using a radioalloster to test predictions of the cooperativity model for gallamine binding to the allosteric site of muscarinic acetylcholine M(2) receptors: C. Trankle, et al.; Mol. Pharmacol. 56, 962 (1999) Abstract; Full Text
Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties: R. Li, et al.; Arch. Pharm. 334, 121 (2001) Abstract
Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators: A. Raasch, et al.; J. Med. Chem. 45, 3809 (2002) Abstract
Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 64, 180 (2003) Abstract; Full Text
Allosteric site on muscarinic acetylcholine receptors: identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupie: U. Voigtlander, et al.; Mol. Pharmacol. 64, 21 (2003) Abstract; Full Text
Contribution of lateral substituents in symmetrical and non-symmetrical heptane-bisammonio compounds to the allosteric stabilization of N-methylscopolamine binding to muscarinic M2 receptors: M. Staudt, et al.; Arch. Pharm. (Weinheim) 336, 385 (2003) Abstract
Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors: C. Trankle, et al.; Mol. Pharmacol. 68, 1597 (2005) Abstract
General Literature References
G protein-coupled receptor allosterism and complexing: A. Christopoulos and T. Kenakin; Pharmacol. Rev. 54, 323 (2002) Abstract
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Parkinson's Disease Other Products
 
 
ALX-350-216 Revised 23-Nov-07
(-)-Eburnamonine
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SYNONYMS (3α,16α)-Eburnamenin-14(15H)-one
Vincamone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-350-216-M100   100 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C19H22N2O
MW: 294.4
CAS NUMBER: 4880-88-0
MERCK INDEX: 14: 3487
PURITY: ≥99%
APPEARANCE: White powder.
SOLUBILITY: Soluble in chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Cerebral metabolic stimulant; shows antihypoxic effects. Vasodilator.
Product Specific Literature References
Experimental approach of activity and mechanism(s) of action of drugs used in cerebral metabolic insufficiency. Application to 1-eburnamonine: P. Linee, et al.; Eur. Neurol. 20, 253 (1981) Abstract
’Cerebroactive’ drugs. Clinical pharmacology and therapeutic role in cerebrovascular disorders: A. Spagnoli & G. Tognoni; Drugs 26, 44 (1983), Review Abstract
Experimental clinical studies on the effect of eburnamonine in cerebrovascular disorders: W. Jansen, et al.; Pharmacopsychiatry 19, 389 (1986) Abstract
Asymmetric synthesis of (-)-eburnamonine and (+)-epi-eburnamonine from (4S)-4-ethyl-4-[2-(hydroxycarbonyl)ethyl]-2-butyrolactone: A.G. Wee & Q. Yu; J. Org. Chem. 66, 8935 (2001) Abstract
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Acetylcholine Receptors (Muscarinic) / Related Products
 
 
ALX-550-061 Revised 18-Mar-08
(+)-Himbacine
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SYNONYMS (3S,3aR,4R,4aS,8aR,9aS)-4-[(1E)-2-[(2R,6S)-1,6-Dimethyl-2-piperdinyl]ethenyl]decahydro-3-methyl-naphtho[2,3-c]furan-1(3H)-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-550-061-M001   1 mg 40.00 USD Add To Cart
ALX-550-061-M005   5 mg 160.00 USD Add To Cart
ALX-550-061-M025   25 mg 520.00 USD Add To Cart
Product Specification
FORMULA: C22H35NO2
MW: 345.5
CAS NUMBER: 6879-74-9
RTECS: QL0843500
SOURCE/HOST: Isolated from the Australian pine Galbulimima baccata.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol, 100% ethanol or methylene chloride; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Hygroscopic.

Product Description
Potent muscarinic antagonist that displays selectivity for the M2 or M4 receptors.
Product Specific Literature References
Binding and functional selectivity of himbacine for cloned and neuronal muscarinic receptors: J.H. Miller, et al.; Pharmacol. Exp. Ther. 263, 663 (1992) Abstract
Structural basis of the subtype selectivity of muscarinic antagonists: a study with chimeric m2/m5 muscarinic receptors: J. Wess, et al.; Mol. Pharmacol. 41, 369 (1992) Abstract
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptors: M.J. Malaska, et al.; Bioorg. Med. Chem. Lett. 3, 1247 (1993)
Chemical modification of ring C of himbacine: discovery of a pharmacophoric element for M2-selectivity: M.J. Malaska, et al.; Bioorg. Med. Chem. Lett. 5, 61 (1995)
Total Syntheses of (+)-Himbacine and (+)-Himbeline: D.J. Hart, et al.; JACS 117, 9369 (1995)
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists: D. Doller, et al.; Bioorg. Med. Chem. Lett. 9, 901 (1999) Abstract
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations: S. Chackalamannil, et al.; Bioorg. Med. Chem. Lett. 14, 3967 (2004) Abstract
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Acetylcholine Receptors (Muscarinic) / Related ProductsAlkaloids
 
 
ALX-550-241 Revised 28-Jan-05
5-Methylfurmethide
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SYNONYMS 5-Methylfurtrethonium iodide
N,N,N,5-Tetramethyl-2-furanmethanaminium iodide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cholinergics / Related Products
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ALX-550-241-M010   10 mg 60.00 USD Add To Cart
ALX-550-241-M050   50 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C9H16INO
MW: 281.1
CAS NUMBER: 1197-60-0
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent muscarinic agonist.
Product Specific Literature References
Pharmacological differences between two muscarinic responses of the rat superior ganglion in vitro: N.R. Newberry & T. Priestly; Br. J. Pharmacol. 92, 817 (1987) Abstract
A pharmacological study of the responses induced by muscarinic agonists on the isolated superior cervical ganglion of the guinea-pig: K.E. Roberts & N.R. Newberry; Eur. J. Pharmacol. 186, 257 (1990) Abstract
Pharmacological analysis of agonist-antagonist interactions at acetylcholine muscarinic receptors in a new urinary bladder assay: Durant, et al.; Br. J. Pharmacol. 104, 145 (1991) Abstract
Interaction of the neuromuscular blocking drug atracurium with muscarinic acetylcholine receptors: J. Musilkova, et al.; Physiol. Res. 40, 293 (1991) Abstract
Characterization of muscarinic receptors in rat kidney: W.M. Blankesteijn, et al.; Eur. J. Pharmacol. 244, 21 (1993) Abstract
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Acetylcholine Receptors (Muscarinic) / Related Products
 
 
ALX-550-401 Revised 16-Jan-06
Naphmethonium dibromide
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SYNONYMS N-[3-(1,3-Dihydro-1,3-dioxo-2H-isoindol-2-yl)propyl]-N’-[3-(1,3-dioxo-1H-benz[d,e]isoquinolin-2(3H)-yl)-2,2-dimethylpropyl]-N,N,N’,N’-tetramethyl-1,6-hexanediamminium dibromide
2-{3-[1-(6-{1,1-Dimethyl-1-[3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)propyl]ammonium}hexyl)-1,1-dimethylammonio]-2,2-dimethylpropyl}benzo[d,e]isoquinoline-1,3-dione dibromide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Acetylcholine Receptors (Muscarinic) / Related Products
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ALX-550-401-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C38H50Br2N4O4
MW: 786.6
CAS NUMBER: 505059-27-8
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, water or aqueous buffer.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: After reconstitution, prepare aliquots and store at -20°C.

Product Description
Very potent allosteric modulator of muscarinic receptors, selective for M2-receptors. Retards the dissociation of the antagonist N-methylscopolamine and exhibits positive cooperativity, i.e. shows higher affinity for occupied receptors compared to free receptors. Affinity for the free receptor is about 100-fold higher than with W84 (Prod. No. ALX-550-399). pKA=8.29, p(αKA)=8.66, pEC50,diss=8.36.
Product Specific Literature References
Systematic development of high affinity bis(ammonio)alkane-type allosteric enhancers of muscarinic ligand binding: M. Muth, et al.; J. Med. Chem. 46, 1031 (2003) Abstract
Design, Synthesis, and Action of Oxotremorine-Related Hybrid-Type Allosteric Modulators of Muscarinic Acetylcholine Receptors: T. Disingrini, et al.; J. Med. Chem. 49, 366 (2006) Abstract
General Literature References
G protein-coupled receptor allosterism and complexing: A. Christopoulos and T. Kenakin; Pharmacol. Rev. 54, 323 (2002) Abstract
Further Categories Containing This Product:
Parkinson's Disease Other Products
 
 
ALX-350-264 Revised 17-Dec-07
Sceptrin . dihydrochloride
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products with Antibiotic Activity
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ALX-350-264-M001   1 mg 98.00 USD Add To Cart
Product Specification
FORMULA: C22H24Br2N10O2 . 2HCl
MW: 620.3 . 73.0
CAS NUMBER: 79703-25-6
SOURCE/HOST: Isolated from the sponge Agelas nakamurai.
PURITY: ≥97% (HPLC)
APPEARANCE: Amorphous powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibits the growth of several Gram-positive and Gram-negative bacteria. Competitively inhibits muscarinic acetylcholine receptors.
Product Specific Literature References
Anti-muscarinic activity of a family of C11N5 compounds isolated from Agelas sponges: R. Rosa, et al.; Experientia 48, 885 (1992) Abstract
A study on the mechanism of action of sceptrin, an antimicrobial agent isolated from the South Pacific sponge Agelas mauritiana: V.S. Bernan, et al.; J. Antimicrob. Chemother. 32, 539 (1993) Abstract
New bromopyrrole alkaloids from the Indopacific sponge Agelas nakamurai: C. Eder, et al.; J. Nat. Prod. 62, 1295 (1999) Abstract
Cyclic heptapeptides from the Jamaican sponge Stylissa caribica: R. Mohammed, et al.; J. Nat. Prod. 69, 1739 (2006) Abstract
Total synthesis of dimeric pyrrole-imidazole alkaloids: sceptrin, ageliferin, nagelamide e, oxysceptrin, nakamuric acid, and the axinellamine carbon skeleton: D.P. O’Malley, et al.; J. Am. Chem. Soc. 129, 4762 (2007) Abstract