Procaine HCl (Novocaine)

Alias: Novocaine HCl; Procaine Hydrochloride; Procaine HCl; Novocaine hydrochloride; Gerovital H3; Aminocaine
Cat No.:V1666 Purity: ≥98%
Procaine HCl(also known as Novocaine; Gerovital H3; Aminocaine), the HCl salt of Procaine, is alocal anesthetic that acts as an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM.
Procaine HCl (Novocaine) Chemical Structure CAS No.: 51-05-8
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
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Other Forms of Procaine HCl (Novocaine):

  • Procaine (Novocaine)
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Procaine HCl (also known as Novocaine; Gerovital H3; Aminocaine), the HCl salt of Procaine, is a local anesthetic that acts as an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM. Procaine is also an inhibitor of 5-HT3 with KD of 1.7 μM. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Procaine hydrochloride (0.01-100 microM) reduced the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. Procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM[1]. is a DNA-demethylating chemical that produces a 40% reduction in 5-methylcytosine DNA concentration as assessed by high-performance capillary electrophoresis or total DNA enzyme digestion. Procaine can also demethylate heavily hypermethylated CpG islands. Procaine also exhibits growth-inhibitory actions in malignant cancer cells, producing mitotic arrest[2]. Procaine serves as an excitant of limbic system cells, and that procaine changes synaptic transmission in some, but not all, output pathways from the amygdale[3].
ln Vivo
Procaine is an excitant of limbic system cells. 15 mg/kg Procaine increases cellular activity in amygdala ventral hippocampus, nucleus accumbens, temporal neocortex and ventromedial hypothalamus of awaken cat. Procaine facilitates transmission of evoked excitatory activity from the amygdala to the ventromedial hypothalamus. Procaine influences frequency and amplitude of reticularly elicited hippocampal rhythmical slow activity. Procaine (0.5 μL, 20% wt/vol) injected at points in the ascending system anterior to the supramamillary nucleus, in the region of the medial forebrain bundle or in the medial septum, reduces the amplitude of reticularly elicited rhythmical slow activity (RSA) but has no effect on its frequency. Procaine injected at points in the ascending system from just anterior to the reticular formation stimulation site, up to, and including the supramamillary nucleus, reduces both the frequency and amplitude of reticularly elicited RSA. Procaine (80mg/kg) increases the duration and propagation of epileptiform afterdischarges (ADs) produced by electrical stimulation of the amygdala in rats. Porcaine also increases the rate of seizure development (kindling) produced by repeated stimulation of the amygdala. Procaine would itself act as convulsants in well kindled subjects. Procaine produces a weak but significant increase in the amplitude of the transcallosal evoked potential. Procaine influences generation of auditory brain stem responses (ABRs). Procaine (30 μL of 1% solution) injection into the trapezoid body of guinea pig affects many of the components of the scalp-derived ABR: N2 is delayed making P2 broader in duration, P3 and N3 are lost, P4 is shortened in latency, broadened in duration but unaffected in amplitude, and N4 is considerably attenuated. Only P1 and N1 are unaffected by the procaine injection. Procaine increases the therapeutic index of cisplatin by improving antitumor activity of cisplatin and reducing its nephrotoxicity. Simultaneous administration of cisplatin and Procaine (40 mg/kg) to BDF1 mice produces 50% lethal dose (LD50) and 90% lethal dose (LD90) values approximately two times higher than those observed with cisplatin alone. Simultaneous administration produces a higher cure rates compared with cisplatin alone (50% vs 9%). The increased blood urea nitrogen (BUN) levels observed 4-7 days following a single administration of cisplatin, as well as the tubular degenerative changes detected by light microscopy, are not observed when the same doses of cisplatin are given simultaneously with Procaine.
Animal Protocol


References
[1]. Fan, P. and F.F. Weight, Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons. Neuropharmacology, 1994. 33(12): p. 1573-9.
[2]. Villar-Garea, A., et al., Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res, 2003. 63(16): p. 4984-9.
[3]. Adamec, R.E. and C. Stark-Adamec, The effects of procaine HCl on population cellular and evoked response activity within the limbic system of the cat. Evidence for differential excitatory action of procaine in a variety of limbic circuits. Prog Neuropsychopharmacol Biol Psychiatry, 1987. 11(4): p. 345-64.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H20N2O2.HCL
Molecular Weight
272.77
CAS #
51-05-8
Related CAS #
Procaine;59-46-1;Procaine-d4 hydrochloride
SMILES
O(C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])[H])=O)C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H]
Synonyms
Novocaine HCl; Procaine Hydrochloride; Procaine HCl; Novocaine hydrochloride; Gerovital H3; Aminocaine
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:55 mg/mL (201.6 mM)
Water:55 mg/mL (201.6 mM)
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 130 mg/mL (476.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6661 mL 18.3305 mL 36.6609 mL
5 mM 0.7332 mL 3.6661 mL 7.3322 mL
10 mM 0.3666 mL 1.8330 mL 3.6661 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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