盐酸普鲁卡因 (0.01-100 µM) 减少全细胞膜片钳记录中 5-HT3 受体介导的内向电流。普鲁卡因似乎对 5-HT3 受体产生竞争性抑制，KD 为 1.7 microM[1]。是一种 DNA 去甲基化化学物质，通过高性能毛细管电泳或总 DNA 酶消化评估，可使 5-甲基胞嘧啶 DNA 浓度降低 40%。普鲁卡因还可以使高度甲基化的 CpG 岛去甲基化。普鲁卡因还在恶性癌细胞中表现出生长抑制作用，导致有丝分裂停滞[2]。普鲁卡因作为边缘系统细胞的兴奋剂，并且普鲁卡因改变杏仁核的一些但不是全部输出通路中的突触传递[3]。

普鲁卡因是边缘系统细胞的兴奋剂。 15 mg/kg Procaine 增加唤醒猫的杏仁核腹侧海马、伏隔核、颞叶新皮质和腹内侧下丘脑的细胞活性。普鲁卡因促进诱发的兴奋活动从杏仁核传递到下丘脑腹内侧。普鲁卡因影响网状引发的海马节律性慢活动的频率和幅度。普鲁卡因（0.5 μL，20% wt/vol）在乳头上核之前的升行系统点、内侧前脑束区域或内侧隔膜中注射，可降低网状诱发的节律性慢活动（RSA）的幅度但对其频率没有影响。普鲁卡因注射在上行系统中从网状形成刺激位点前面直至乳头上核的点，可降低网状引发的 RSA 的频率和幅度。普鲁卡因 (80mg/kg) 会增加大鼠杏仁核电刺激产生的癫痫样后放电 (AD) 的持续时间和传播。猪卡因还会增加因反复刺激杏仁核而产生的癫痫发作（点燃）的速度。普鲁卡因本身会在点燃良好的受试者中起到惊厥作用。普鲁卡因产生微弱但显着的经胼胝体诱发电位振幅增加。普鲁卡因影响听觉脑干反应（ABR）的产生。将普鲁卡因（30 μL 1% 溶液）注射到豚鼠的梯形体中会影响头皮源性 ABR 的许多成分：N2 延迟，使 P2 持续时间变长，P3 和 N3 丢失，P4 潜伏期缩短，持续时间变宽，但幅度不受影响，并且 N4 显着衰减。只有 P1 和 N1 不受普鲁卡因注射的影响。普鲁卡因通过提高顺铂的抗肿瘤活性、降低其肾毒性来提高顺铂的治疗指数。对 BDF1 小鼠同时给予顺铂和普鲁卡因 (40 mg/kg)，产生的 50% 致死剂量 (LD50) 和 90% 致死剂量 (LD90) 值比单独使用顺铂时观察到的值高出大约两倍。与单独使用顺铂相比，同时给药的治愈率更高（50% vs 9%）。单次给予顺铂后 4-7 天观察到的血尿素氮 (BUN) 水平升高，以及通过光学显微镜检测到的肾小管退行性变化，在同时给予相同剂量的顺铂和普鲁卡因时没有观察到。

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.

Toxicity Summary
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.

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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.

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Toxicity Data
LD50: 350 mg/kg (Oral, mouse).

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Interactions
WELL-KNOWN CLASS OF PROLONGING AGENTS...SKF-525-A...INHIBITS...MICROSOMAL ESTERASE ACTIVITY TOWARDS PROCAINE.
... /PROCAINE/ IS HYDROLYZED IN VIVO TO PRODUCE PARAAMINOBENZOIC ACID, WHICH INHIBITS THE ACTION OF SULFONAMIDES. THUS, LARGE DOSES SHOULD NOT BE ADMINISTERED TO PATIENTS TAKING SULFONAMIDE DRUGS.
PROCAINE IM CAN POTENTIATE PENTOBARBITAL ANESTHESIA... SYMPATHOMIMETICS...& MONOAMINE OXIDASE INHIBITORS MAY HAVE THEIR HYPERTENSIVE EFFECTS POTENTIATED BY PROCAINE. ...MAY POTENTIATE OR BE POTENTIATED BY PHENOTHIAZINE TRANQUILIZERS, CHOLINESTERASE INHIBITORS...& MUSCLE RELAXANTS SUCH AS SUCCINYLCHOLINE.
SUBSTRATE COMPETITION PROBABLY ACCOUNTS FOR INHIBITION OF SUCCINYLCHOLINE HYDROLYSIS BY PROCAINE.
For more Interactions (Complete) data for PROCAINE (17 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Rat sc 600 mg/kg
LD50 Mouse oral 350 mg/kg
LD50 Mouse ip 124 mg/kg
LD50 Mouse sc 300 mg/kg
LD50 Mouse iv 45 mg/kg

[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.

Therapeutic Uses
Anesthetics, Local
PROCAINE SOLN ARE USED FOR INFILTRATION ANESTHESIA ..., NERVE BLOCK ..., & SPINAL ANESTHESIA (DOSE VARIES WITH TECHNIC EMPLOYED). FOR CONTINUAL CAUDAL ANALGESIA ... /HYDROCHLORIDE/
OBJECTIVE OF CONTINUOUS SPINAL ANESTHESIA IS TO ... PRODUCE LEVEL, DEGREE, & DURATION OF ANESTHESIA DESIRED. ... LOCAL ANESTHETIC OF SHORT DURATION, SUCH AS PROCAINE, CAN BE USED TO INCR CONTROLLABILITY FURTHER.
/Procaine hydrochloride/ is injected locally adjacent to the muscle cone ... or in the region of the facial nerve ... to reduce pain and to prevent eye and lid movements during surgery. ... Used to block nerve endings in the immediate area of surgery (infiltration anesthesia) for procedures such as minor lid operations. /Procaine hydrochloride/
For more Therapeutic Uses (Complete) data for PROCAINE (14 total), please visit the HSDB record page.

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Drug Warnings
MAJOR CAUSE OF SYSTEMIC REACTIONS TO LOCAL ANESTHETICS IS HIGH BLOOD CONCN OF DRUG. ... BECAUSE OF THREAT OF HIGH BLOOD CONCN ... IT IS IMPORTANT TO ADMIN SMALLEST AMT THAT WILL BE EFFECTIVE. /LOCAL ANESTHETICS/
EXTREMELY RARE EVENT IS ACCIDENTAL INJECTION OF LOCAL ANESTHETIC DIRECTLY INTO FETUS; THIS RESULTS IN APNEA, BRADYCARDIA, & CONVULSIONS IN FIRST MIN OF LIFE.
Since aminobenzoic acid, a metabolite of procaine, may antagonize the activity of aminosalicylic acid and sulfonamides, some clinicians have suggested procaine should not be used in patients receiving these drugs. IV administration of procaine hydrochloride is contraindicated in patients with myasthenia gravis or in those patients receiving digitalis, anticholinesterase drugs, or succinylcholine.
High plasma concentrations of local anesthetics affect the CNS and cardiovascular system. Generally, high plasma concentrations of the drugs initially produce CNS stimulatory effects manifested by anxiety, apprehension, restlessness, nervousness, disorientation, confusion, dizziness, blurred vision, tremors, twitching, shivering, and seizures, followed by CNS depression manifested of drowsiness, unconsciousness, and respiratory arrest. Nausea, vomiting, chills, miosis, and tinnitus may also occur. /Local anesthetics/
For more Drug Warnings (Complete) data for PROCAINE (15 total), please visit the HSDB record page.

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Pharmacodynamics
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine.

C13H20N2O2.HCL

272.77

272.129

51-05-8

Procaine;59-46-1;Procaine-d4 hydrochloride

4914

White to off-white solid powder

195-196°C 17mm

155-156 °C(lit.)

195-196°C/17mm

3.15

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： (1). 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。  (2). 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)

配方 1 中的溶解度: 130 mg/mL (476.59 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。

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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。