Arcaine sulfate

CAS# 14923-17-2

Arcaine sulfate

Catalog No. BCC6631----Order now to get a substantial discount!

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Chemical structure

Arcaine sulfate

3D structure

Chemical Properties of Arcaine sulfate

Cas No. 14923-17-2 SDF Download SDF
PubChem ID 119020 Appearance Powder
Formula C6H18N6O4S M.Wt 270.31
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 25 mM in water
Chemical Name 2-[4-(diaminomethylideneamino)butyl]guanidine;sulfuric acid
SMILES C(CCN=C(N)N)CN=C(N)N.OS(=O)(=O)O
Standard InChIKey RWTGFMPOODRXIM-UHFFFAOYSA-N
Standard InChI InChI=1S/C6H16N6.H2O4S/c7-5(8)11-3-1-2-4-12-6(9)10;1-5(2,3)4/h1-4H2,(H4,7,8,11)(H4,9,10,12);(H2,1,2,3,4)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Arcaine sulfate

DescriptionNO synthase inhibitor. An NMDA antagonist acting as a competitive inhibitor at the polyamine site.

Arcaine sulfate Dilution Calculator

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Arcaine sulfate Molarity Calculator

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Preparing Stock Solutions of Arcaine sulfate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.6995 mL 18.4973 mL 36.9946 mL 73.9891 mL 92.4864 mL
5 mM 0.7399 mL 3.6995 mL 7.3989 mL 14.7978 mL 18.4973 mL
10 mM 0.3699 mL 1.8497 mL 3.6995 mL 7.3989 mL 9.2486 mL
50 mM 0.074 mL 0.3699 mL 0.7399 mL 1.4798 mL 1.8497 mL
100 mM 0.037 mL 0.185 mL 0.3699 mL 0.7399 mL 0.9249 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Arcaine sulfate

Histamine facilitates in vivo thalamocortical long-term potentiation in the mature visual cortex of anesthetized rats.[Pubmed:18371073]

Eur J Neurosci. 2008 Apr;27(7):1731-8.

Recent evidence indicates that the mature central visual system retains a higher degree of plasticity than traditionally assumed. However, little is known regarding the neuromodulatory factors that influence plasticity in the adult primary visual cortex (V1). We investigated the role of histamine, one of the neuromodulators that densely innervate all neocortical fields, in modulating plasticity of V1 by examining thalamocortical long-term potentiation (LTP). Theta-burst stimulation of the lateral geniculate nucleus of urethane-anesthetized rats resulted in potentiation of the field postsynaptic potential recorded in the superficial layers of V1. Histamine (0.01-10 mM), applied locally in V1 by reverse microdialysis, produced a clear, dose-dependent enhancement of LTP. In addition, histamine also allowed a weak theta-burst induction protocol, that by itself failed to induce significant synaptic potentiation, to produce stable LTP. The effect of histamine to facilitate LTP was largely resistant to blockade of H(1)[chlorpheniramine, 5 and 10 mg/kg, intraperitoneal (i.p.)] or H(2) receptors (cimetidine, 10 mg/kg, zolantidine, 5 mg/kg, i.p.). However, Arcaine sulfate salt (10 mg/kg, i.p.), a blocker of the polyamine binding site of the N-methyl-D-aspartate (NMDA) receptor, completely antagonized the LTP amplification induced by histamine, suggesting that it acts via a direct modulation of NMDA receptors, rather than histaminergic receptor activation. The present experiments provide the first demonstration of a histaminergic influence on neocortical synaptic plasticity in vivo and show that cortical histaminergic activation acts to lower the induction threshold and increase the degree of plasticity in the mature thalamocortical visual system.

Investigation of the actions and antagonist activity of some polyamine analogues in vivo.[Pubmed:9641557]

Br J Pharmacol. 1998 May;124(2):386-90.

1. The ability of three putative polyamine antagonists to antagonize behavioural changes induced by spermine was assessed. 2. Injection of an excitotoxic dose of spermine (100 microg, i.c.v.) in mice results in the development of a characteristic behavioural profile, which has two temporally distinct phases. The early events include clonic convulsions, and the later, more general excitation, includes tremor and culminates in the development of a fatal tonic convulsion. 3. Co-administration of arcaine (25 microg, i.c.v.) potentiated the early phase effects after spermine injection, but antagonized the development of spermine-induced tonic convulsions. A larger dose of arcaine (50 microg, i.c.v.) given alone resulted in the development of spermine-like body tremor and convulsions. It therefore appears that arcaine is not a pure polyamine antagonist in vivo, but may be a partial agonist. 4. Similarly, 1,10-diaminodecane appeared to act as a partial agonist in vivo, although it was less potent than arcaine. 5. In contrast, diethylenetriamine (DET) effectively inhibited the development of the early effects of spermine, but was ineffective against the spermine-induced CNS excitation and tonic convulsions. 6. It is concluded that none of the putative polyamine antagonists tested behaved as effective polyamine antagonists in vivo, although each produced some antagonism.

Structure-activity relationships of arginine analogues on nitric oxide synthase activity in the rat brain.[Pubmed:7532812]

Neuropharmacology. 1994 Nov;33(11):1261-5.

Nitric oxide (NO) is synthesized by nitric oxide synthase (NOS) from L-arginine (Arg) which has a guanidino group in its molecule. We examined the effect of 23 different Arg analogues on NOS activity in the rat brain. Though homoarginine, epsilon-guanidinocaproic acid and canavanine act as substrates of NOS, production of NO from them was lower than that from Arg. alpha-Guanidinoglutaric acid (2-GGA) and arcaine inhibited NOS activity at levels equal to NG-monomethyl-L-arginine (MeArg), a well known NOS inhibitor. Though almost all previously reported NOS inhibitors were synthesized by substituting the guanidino nitrogen of Arg, the guanidino nitrogens of arcaine and 2-GGA were not substituted. Furthermore, 2-GGA is a known endogenous convulsant in mammals, and arcaine, which was isolated from a marine mollusc, is also a convulsive substance. Hence, 2-GGA and arcaine will be excellent drugs to investigate not only the chemical nature of NOS but also the physiologic function of NO.

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