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Dimethocaine is a local anesthetic and a stimulant that has some cocaine-like activity.

It’s generally reported to be weaker than cocaine and amphetamine.

A minimal amount of recreational use has been reported since the late 2000s.

The substance was previously used in the 1930s as an anesthetic.



Buy Dimethocaine Online

Buy Dimethocaine Online, Dimethocaine is a local anesthetic that, because of its similarity in action to cocaine has the potential for abuse.

This compound completely inhibits dopamine uptake in rat striatal synaptosomes with an IC50 value of 1.2 µM comparable to that of cocaine (IC50 = 0.7 µM).

1 As a result, dimethicone dose-dependently substitutes for cocaine in drug discrimination tests in rats and rhesus monkeys.

2,3 This product is intended for forensic and research purposes.

Technical Information

Formal Name 3-(diethylamino)-2,2-dimethyl-1-(4-aminobenzoate)-1-propanol, monohydrochloride

CAS Number 553-63-9

Molecular Formula C16H26N2O2 • HCl

Formula Weight     314.9

Purity     ≥98%

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Formulation A crystalline solid

Increased talkativeness
Mood lift
Difficulty breathing
Chest pain
There are a limited number of reports about the drug’s effects. Most point to little activity or, at most, mild euphoria and mild stimulation.

Stimulation and euphoria offered by the drug is generally said to be weaker than what’s offered by cocaine or amphetamine.

The local anesthetic effect generally leads to numbness in the nasal region when taken intranasally.

Some users have experienced fatigue and slight mental impairment when the effects dissipate and even a lasting CNS depressant effect into the following day.

However, the lack of experience reports makes it difficult to tell how common these after effects are.

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Animal studies

It had a memory impairing effect in mice in a maze test.

This was hypothesized in the paper to come from a dopamine mechanism.

Lidocaine, which lacks similar dopaminergic activity, didn’t have the same response.

Greater locomotor activity and cocaine-like behavior effects were observed in mice.

Anxiogenic effects were seen at 10 mg/kg and 20 mg/kg in a maze test in mice.

Dimethocaine had some apparent dose-dependent antinociceptive effects in mice, including in writhing and hot-plate tests.

Chemistry & Pharmacology
Dimethocaine has a structure that’s closer to procaine, a drug that lacks psychoactive effects, than cocaine. A major difference is that it lacks a tropane ring.

It functions as a dopamine reuptake inhibitor.

Possible actions at other sites haven’t been examined.

The drug was only slightly less potent than cocaine for displacing mazindol at the dopamine transporter (DAT).

DA reuptake inhibition potency appears to go in this order:

Cocaine > Dimethocaine > Tetracaine > Procaine > Chloroprocaine.

Dimethocaine elevated dopamine in the nucleus accumbens in rats.

It’s also been shown to elevate dopamine levels in the striatum.

EC500 (concentration for 500% basal level) in str

It’s been found to be 2-3x less potent than cocaine in some drug discrimination studies.

Dimethocaine fully substituted for cocaine when rats were trained to discriminate cocaine from saline.

It also fully substituted when rats were trained to discriminate cocaine from procaine, further indicating cocaine-like effects.

Investigation of its pharmacokinetics in rats showed extensive metabolism.

The most important phase 1 steps were hydroxylation and deethylation.

The most important phase 2 steps were acetylation and glucuronidation.

In vitro tests found roles for CYP1A2, CYP2C19, CYP2D6, and CYP3A4.

N-acetylation was carried out by NAT2, but not NAT1.

Additional information


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