在全细胞膜片钳记录中，5-HT3 钳传导的内向电流被普鲁卡因 (0.01-100 μM) 抑制。普鲁卡因的 KD 为 1.7 μM，似乎对 5-HT3 产生互补抑制作用 [1]。普鲁卡因是一种 DNA 甲基化剂，利用毛细管快速或高效酶消化整个 DNA，将 5-甲基胞嘧啶 DNA 的量减少 40%。此外，重甲基化的 CpG 岛可以被普鲁卡因去甲基化。这些杏仁同样会受到丙帕辛的生长抑制作用，导致有丝分裂曼哈顿分裂 [2]。普鲁卡因改变杏仁核输出的一部分的突触传递并兴奋边缘系统中的细胞[3]。

Absorption, Distribution and Excretion
With normal kidney function, the drug is excreted rapidly by tubular excretion.
/PARA-AMINOBENZOIC ACID/ ... IS EXCRETED IN URINE TO EXTENT OF ABOUT 80%, EITHER UNCHANGED OR IN CONJUGATED FORM. ONLY 30% OF DIETHYLAMINOETHANOL CAN BE RECOVERED IN URINE; REMAINDER UNDERGOES METABOLIC DEGRADATION.
... IT HAS BEEN SHOWN THAT, FOLLOWING INTRODUCTION OF PROCAINE INTO EPIDURAL SPACE IN USUAL ANESTHETIC DOSE, SIGNIFICANT CONCN IS ACHIEVED IN SPINAL FLUID.
RATE OF ENZYMATIC HYDROLYSIS OF LOCAL ANESTHETIC AGENTS BY SPINAL FLUID IS SLOW. ... DURATION OF ANESTHESIA DEPENDS UPON RATE AT WHICH DRUG IS REMOVED FROM CSF & FROM NERVE ROOTS WHERE IT EXERTS ITS ACTION. /LOCAL ANESTHETICS/
ABSORPTION DOES NOT TAKE PLACE FROM STOMACH, ESOPHAGUS, OR BLADDER IF MUCOSA INTACT. /LOCAL ANESTHETICS/
For more Absorption, Distribution and Excretion (Complete) data for PROCAINE (7 total), please visit the HSDB record page.

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Metabolism / Metabolites
Hydrolysis by plasma esterases to PABA
REDUCED RATE OF PROCAINE HYDROLYSIS IN SERUM FROM UREMIC PT IS DUE TO DECR ENZYME ACTIVITY RATHER THAN COMPETITIVE INHIBITION OF ENDOGENOUS SUBSTANCE IN SERUM.
... /Procaine/ is hydrolyzed in vivo to produce paraaminobenzoic acid ...
YIELDS 2-DIETHYLAMINOETHYL P-ACETAMIDOBENZOATE IN GUINEA PIG; BILLIAR, RB, & EIK-NES, KB, ARCHS BIOCHEM BIOPHYS, 115, 318 (1966). /FROM TABLE/
Hydrolysis by plasma esterases to PABA
Route of Elimination: With normal kidney function, the drug is excreted rapidly by tubular excretion.
Half Life: 7.7 minutes

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Biological Half-Life
7.7 minutes
SERUM T/2 VALUES FOR PROCAINE WERE LONGER FOR PT WITH LIVER DISEASE (2.3 MIN), PT WITH RENAL FAILURE (1.4 MIN), & NEW-BORN INFANTS (1.4 MIN) THAN FOR HEALTHY ADULTS (0.66 MIN).
INFUSION OF 2% PROCAINE-HCL ADMIN TO 12 WOMEN UNDERGOING HYSTERECTOMY. STEADY-STATE PLASMA LEVELS WERE ACHIEVED WITHIN 20-30 MIN AFTER COMMENCEMENT OF INFUSION. AFTER TERMINATION OF INFUSION DISTRIBUTION T/2 OF 2.49 MIN & ELIMINATION T/2 OF 7.69 MIN.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
The term "Novocaine" (procaine) is often equated to local anesthetic. The exact identity of any local anesthetic should be verified, especially since procaine is no longer marketed in in the US as a single ingredient product. No information is available on the use of procaine during breastfeeding. Based on the short half-life of procaine in the plasma and the low excretion of other local anesthetics into breastmilk, a single dose of procaine during breastfeeding is unlikely to adversely affect the breastfed infant. However, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[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]. 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.

Procaine is a benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol. It has a role as a local anaesthetic, a central nervous system depressant, a peripheral nervous system drug and a drug allergen. It is a benzoate ester, a substituted aniline and a tertiary amino compound. It is functionally related to a 2-diethylaminoethanol and a 4-aminobenzoic acid. It is a conjugate base of a procaine(1+).
A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients.
Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.
Procaine is only found in individuals that have used or taken this drug. It is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). [PubChem]Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. 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.
A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).
See also: Procaine Hydrochloride (has salt form); Penicillin G Procaine (is active moiety of); Procaine Merethoxylline (has salt form) ... View More ...

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Drug Indication
Used as a local anesthetic primarily in oral surgery

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Mechanism of Action
Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. 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.
LOCAL ANESTHETICS BLOCK CONDUCTION BY DECREASING OR PREVENTING THE LARGE TRANSIENT INCREASE IN THE PERMEABILITY OF EXCITABLE MEMBRANES TO SODIUM IONS THAT NORMALLY IS PRODUCED BY A SLIGHT DEPOLARIZATION OF THE MEMBRANE. /LOCAL ANESTHETIC/
LOCAL ANESTHETICS BLOCK CONDUCTION IN NERVE PERHAPS BY COMPETING WITH CALCIUM @ SOME SITE THAT CONTROLS PERMEABILITY OF MEMBRANE. ... LOCAL ANESTHETICS ALSO REDUCE PERMEABILITY OF RESTING NERVE TO POTASSIUM AS WELL AS TO SODIUM IONS. /LOCAL ANESTHETICS/
AS THE ANESTHETIC ACTION PROGRESSIVELY DEVELOPS IN A NERVE, THE THRESHOLD FOR ELECTRICAL EXCITABILITY GRADUALLY INCREASES, THE RATE OF RISE OF THE ACTION POTENTIAL DECLINES, IMPULSE CONDUCTION SLOWS, & THE SAFETY FACTOR FOR CONDUCTION DECREASES; THESE FACTORS DECREASE THE PROBABILITY OF PROPAGATION OF THE ACTION POTENTIAL, AND NERVE CONDUCTION FAILS. /LOCAL ANESTHETICS/
POSTSYNAPTIC ACTION ... END-PLATE CURRENT IS MUCH PROLONGED BY PROCAINE. SIMILARLY, WHEN ... ADDED TO FLUID PERFUSING GANGLION, PREGANGLIONIC STIMULATION FAILS TO ELICIT POSTGANGLIONIC DISCHARGES & GANGLION CELLS BECOME INSENSITIVE TO STIMULATION BY ACETYLCHOLINE.
IN ADDITION TO BLOCKING CONDITIONS IN NERVE AXONS IN THE PERIPHERAL NERVOUS SYSTEM, LOCAL ANESTHETICS INTERFERE WITH THE FUNCTION OF ALL ORGANS IN WHICH CONDUCTION OR TRANSMISSION OF IMPULSES OCCURS. ... EFFECTS ON ... CNS, THE AUTONOMIC GANGLIA, THE NEUROMUSCULAR JUNCTION, & ALL FORMS OF MUSCLE. /LOCAL ANESTHETICS/

C₁₃H₂₀N₂O₂

236.31

236.152

59-46-1

Procaine hydrochloride;51-05-8

4914

White to off-white solid powder

1.1±0.1 g/cm3

373.6±22.0 °C at 760 mmHg

61ºC

179.8±22.3 °C

0.0±0.8 mmHg at 25°C

1.543

2.36

55.56

1

4

7

17

222

0

MFDFERRIHVXMIY-UHFFFAOYSA-N

InChI=1S/C13H20N2O2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3

2-(diethylamino)ethyl 4-aminobenzoate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 该产品在溶液状态不稳定，请现配现用。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~423.17 mM)
H2O : ~1 mg/mL (~4.23 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.58 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (10.58 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (10.58 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 2 mg/mL (8.46 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶 (<60°C).

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。