MAR2011

Cayman offers a select group of research tools (inhibitors and substrates as well as receptor agonists and antagonists) pertinent to Neuroscience research areas such as Alzheimer’s disease and pain management as well as more general factors related to excitatory and inhibitory signal transduction.

Neuroscience Products: Inhibitors, Substrates, Agonists, and Antagonists

Item No. Product Name Notes

78050 (-)-(α)-Kainic Acid Developed as the prototype neuroexcitatory amino acid for the induction of seizures in

experimental animals

13644 Aspalatone Generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in

rat hippocampus

10008346 Gabapentin A GABA analog

13623 Topiramate A sugar sulfamate that exhibits potent anticonvulsant activity

13667 Muscimol A full GABAA agonist and partial GABAC agonist

10032 N-(α-Linolenoyl) Tyrosine A simple a-amide conjugate prepared as a method for CNS dopamine content by

facilitated transport of the tyrosine precursor across the blood-brain barrier

13248 L-DOPA A metabolic precursor of dopamine that is capable of crossing the blood-brain barrier

13205 Halopemide A potent inhibitor of phospholipase D and dopamine receptors

10488 Bupropion (hydrochloride) An inhibitor of dopamine and norepinephrine reuptake and an antagonist of neuronal

acetylcholine nicotinic receptors

13358 CAY10608 A potent, selective, and non-competitive antagonist of the NR2B subunit of NMDA receptors

10010743 Capsaicin (technical grade) The primary active component of the heat and pain-eliciting lipid-soluble fraction of the

Capsicum pepper

92350 Capsaicin The primary active component of the heat and pain-eliciting lipid-soluble fraction of the

Capsicum pepper

92355 Dihydrocapsaicin A major impurity found in natural hot pepper extracts

90052 Arvanil A structural analog of capsaicin

90262 Olvanil A structural analog of capsaicin

10005633 CAY10448 A potent capsaicin receptor antagonist

10007518 Capsazepine A competitive antagonist of TRPV1

10009501 20-hydroxy

N-Arachidonoyl Taurine

A potential CYP450 metabolite of N-arachidonoyl taurine that may activate

members of the TRP family of calcium channels

10012565 CAY10568 A physically smaller, less hydrophobic version of QX314 designed to be more permeable

to TRPV1 ion channel

10137 Icilin A synthetic CMR1/TRPM8 super agonist that serves as a reference cold nociceptive

agonist for TRP-type ion channels

70090 BW 723C86 A 5-HT receptor agonist with 10-fold selectivity for the HT2B receptor

13203 Agomelatine A metabolically stable analog of melatonin a competitive antagonist of 5-HT2C and

5-HT2B receptors

10011546 AL 34662 A potent 5-HT2 receptor agonist with ocular hypotensive activity

10096 SB 242084 (hydrochloride) An antagonist of the 5-HT2C receptor

10005254 AFMK A melatonin metabolite that has antioxidant and free radical scavenging activities

90377 13-Docosenamide The amide of docosenoic acid identified in the CSF of sleep-deprived cats

10012588 A-803467 A sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8

sodium channels

10009312 SKF-96365 (hydrochloride) Inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels

10010109 8-DY547-cGMP A fluorescently-labeled cyclic nucleotide used to study CNGA2 channel activation

10011135 BAY-60-7550 A potent type 2 cyclic nucleotide phosphodiesterases (PDE2) inhibitor

10011126 Clobenpropit (hydrobromide) A selective histamine H3 receptor antagonist that crosses the blood-brain barrier

10011127 Thioperamide Maleate A selective histamine H3 receptor antagonist that crosses the blood-brain barrier

9000849 Phenazepam A benzodiazepine agonist of the GABAA-benzodiazepine receptor chloride channel complex

To view Cayman’s entire line

of Neuroscience products,

request a copy of the

Neuroscience catalog

For full information on these products and more, visit caymanchem.com

MAR2011 Cayman Chemical Ann Arbor, MI (800) 364-9897 caymanchem.com

Additional Compounds

Alzheimer’s DiseaseInsoluble deposits of β-amyloid peptide (Aβ) and hyperphosphorylation of the microtubule-associated tau protein leads to the aggregation and formation of amyloid plaques and neurofibrillary tangles, both hallmarks of Alzheimer’s disease. In an effort to support the necessary research to prevent and treat the symptoms of this degenerative disease, Cayman offers a collection of tools that target the inhibition of β-amyloid peptide production and aggregation, as well as the prevention of tau protein phosphorylation and modification. Additional compounds purport to stave off dementia and improve cognitive function by targeting other various signaling pathways.

β-Amyloid (1-8, A2V) Peptide 10229Aβ, Aβ 1-8 mutant, β-amyloid (1-8) dominant negativeβ-Amyloid peptide (1-42) aggregation results in the formation of neurotoxic fibrils or globular oligomers. The amyloid precursor protein (APP) mutation Ala673 → Val673 results in disease for homozygous carriers but not for heterozygous carriers. The mutation generates β-amyloid peptide with valine at amino acid position two. Biochemical analysis of Aβ (1-42) aggregation suggests this small peptide may be a useful guide for developing β-amyloid peptide aggregation inhibitors.

• Also Available: β-Amyloid (1-8) Peptide (10241)

BACE (human recombinant) 10227ASP-2, BACE-1, Memapsin, Membrane-bound Aspartic Protease, β-SecretasePurity: ≥95% Summary: Source: human recombinant C-terminal His-tag protein purified from E. coli • Mr: 48 kDa

BACE Inhibitor Screening Assay Kit 600070BACE, the major β-secretase, initiates the first step in β-amyloid peptide production. Inhibition of BACE activity could potentially block the entire cascade of Alzheimer’s disease pathogenesis. Cayman’s BACE Inhibitor Screening Assay Kit provides a convenient method for screening human BACE inhibitors. The assay utilizes a synthetic Swedish mutant APP peptide (EVNLDAEF) that has been linked to a fluorophore (EDANS) at one end and to a quenching agent (Dabcyl) at the other. After cleavage by BACE, the product (peptide-EDANS) is brightly fluorescent and can be easily analyzed using a fluorescence plate reader or a fluorometer with excitation wavelengths of 335-345 nm and emission wavelengths of 485-510 nm.

Methyltransferase ActivityMethylation of key biological molecules and proteins play important roles in numerous biological systems. S-adenosylmethionine (SAM) dependent methyltransferases use SAM, also known as AdoMet, to donate a methyl group that is required for the modification of proteins and DNA. Aberrant levels of SAM have been linked to many abnormalities, including Alzheimer’s disease, depression, Parkinson’s disease, multiple sclerosis, liver failure, and cancer.

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Methyltransferase Fluorometric Assay Kit 700150Cayman’s Methyltransferase Fluorometric Assay Kit is an enzyme-coupled assay that can continuously monitor SAM-dependent methyltransferases. The removal of the methyl group from SAM generates S-adenosylhomocysteine (AdoHcy), which is rapidly converted to S-ribosylhomocysteine and adenine by AdoHcy nucleosidase. This rapid conversion prevents the buildup of AdoHcy and its feedback inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine, by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2). The reaction between H2O2 and ADHP (10-acetyl-3,7,-dihydroxyphenoxazine) produces the highly fluorescent compound resorufin. Resorufin fluorescence can be easily analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.

Methyltransferase Colorometric Assay Kit 700140Cayman’s Methyltransferase Colorimetric Assay Kit operates on a similar principle as the above fluorometric kit except the rate of production of H2O2 is measured with the colorimetric reagent, 3,5-dichloro-2-hydroxybenzenesulfonic acid, by an increase in absorbance at 500-520 nm.

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Methionine SulfoxideProtein methionine sulfoxide (MetO) is a reversible oxidative modification that occurs by exposure of protein(s) methionine residues to reactive oxygen species (ROS). Methionine oxidation can alter the function(s) of the modified proteins and if not reversed by MetO reductases can be further oxidized to methionine sulfone, an irreversible modification. The overabundance of methionine sulfoxidation is implicated in age-related diseases.

Methionine Sulfoxide Immunoblotting Kit 600160Cayman’s MetO Immunoblotting Kit contains reagents needed for the immunochemical detection of proteins containing MetO residues by western blotting. MetO-containing samples of interest include those from cell or tissue lysates as well as semi-pure or purified proteins. Samples may be prepared with reducing or non-reducing sample buffer prior to SDS-PAGE and tested alongside one SDS-PAGE well designated for the provided positive control. The MetO Polyclonal Antibody was isolated from rabbit serum generated after immunization with a oxidized corn protein (MetO-DZS18) rich in methionine. This polyclonal antibody is specific for protein methionine sulfoxide and can detect IgG-containing MetO from sera of Alzheimer’s patients but not from normal control sera.

β-AmyloidThe β-amyloid peptide is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Initial cleavage by β-secretase (BACE), a membrane anchored aspartic protease, generates a soluble N-terminal fragment and a membrane-associated C-terminal fragment. The C-terminal fragment then undergoes proteolysis by γ-secretase to give the Aβ peptide.

Item No. Product Name Notes

13332 (S)-Glycyl-H-1152 (hydrochloride) A selective, potent Rho kinase IV inhibitor derived from HA-1077 (Fasudil)

70240 Tacrine (hydrochloride) A derivative of aminoacridine which functions as an inhibitor of both AChE and butyrylcholinesterase

10005836 bis(7)-Tacrine An AChE inhibitor that is 1,000 times more potent than tacrine

13245 Donepezil A reversible AChE inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine

13662 Arecoline (hydrobromide) An agonist of the muscarinic acetylcholine receptors M1, M2, and M3

10230 (+)-Muscarine (iodide salt) The biologically active stereoisomer of muscarine

9000556 DimebolinA non-selective antihistamine that also inhibits the neurotoxic action of β-amyloid and blocking L-type calcium channels, inhibits NMDA-type glutamate receptors, and prevents mitochondrial leakage

10011349 Dimebolin (hydrochloride) The hydrochloride form of Dimebolin soluble in both aqueous and organic solvents

13197 DAPT An inhibitor of γ-secretase; blocks production of total Aβ in human primary neuronal cultures

10007963 E-64 A natural, potent, and irreversible inhibitor of cysteine proteases

10009021 AVE-1625 A highly potent, selective antagonist for the CB1 receptor; significantly improves the performance of rodents in working memory tasks

13033 Valproic Acid (sodium salt)An inhibitor of histone deacetylases and GSK3 that depletes cellular inositol-1,4,5-trisphosphate; shows promise in combination therapy for cancer and in treating Alzheimer’s disease