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Chemical Information:
CAS Number: 23239-75-0
Purity: ≥98%
Molecular Weight: 211.73 g/mol
Melting Point: 177-179°C
Molecular Formula: C12H17N•HCl
Synonyms: 4-(Phenylmethyl)piperidine hydrochloride; 4-benzylpiperidine hydrochloride; Piperidine, 4-(phenylmethyl)-, hydrochloride (1:1); 23239-75-0
PubChem CID: 31737
SMILES: c1ccc(cc1)CC2CCNCC2.Cl

Technical Information:
Application: 4-PMPD HCL is a selective catecholamine releasing agent with antidepressant properties.
Appearance: White to pale cream powder
Physical State: Solid
Solubility: Soluble 50 mg / mL in water; Soluble to 50 mg / mL in ethanol; Soluble to 50 mg / mL in isopropanol
Storage: Store at room temperature or cooler, in a sealed airtight container, protected from heat, light and humidity.
Stability: Stable for at least two years when stored as above.


Biochemical Activity:
4-(Phenylmethyl)piperidine hydrochloride (4-PMPD HCL), also known as 4-benzylpiperidine hydrochloride, is a selective catecholamine releasing agent with releasing characteristics similar to, but with lower potency than (+)Phenmetrazine, and was patented as an antidepressant in 1972.1

4-PMPD HCL was tested in mice, rats, cats, dogs and monkeys and was found to be an active antidepressant in all of these species. The compound was revealed to have an active antidepressant effect at dosages lower than the minimum dosage at which mild stimulation was observed. A mild appetite suppressant effect was also noted. 4-PMPD did not display significant anticholinergic activity in mammals, avoiding the off target activity and anticholinergic side effects of some antidepressants. 1

In addition, 4-PMPD HCL was also discovered to act as a vasodilator, potentially improving cerebral and muscular blood flow. 4-PMPD possessed a favorable therapeutic index (LD50/ED50) of 45, derived from the LD50 / antidepressant ED50 data in mice and rats.1

4-PMPD was compared in Rhesus monkeys against three other catecholamine / dopamine releasers, Amphetamine, Benzylpiperazine (BZP) and (+)Phenmetrazine, for its ability to selectively suppress cocaine- versus food-maintained responding. Treatment for 7 days with each of the four releasers produced a dose-dependent and selective reduction in self-administration of cocaine, supporting the potential utility of dopamine-selective releasers as candidate treatments for cocaine dependence.2

The dose ranges for each test compound were as follows: BZP (0.32–1.0 mg/kg/h), (+)Phenmetrazine (0.1–0.56 mg/kg per h), and 4-PMPD (0.56–1.8 mg/kg/h). The higher doses of each compound were empirically determined to decrease rates of cocaine self-administration to less than 20% of control. All compounds produced a dose- and time-dependent substitution for the training dose of 0.4 mg/kg cocaine in all monkeys. Amphetamine and phenmetrazine were roughly equipotent, and a dose of 0.32 mg/kg was the lowest dose to produce a significant increase in cocaine-appropriate responding. A higher dose of 1.0 mg/kg was required to produce a significant increase in cocaine-appropriate responding for benzylpiperazine and 4-PMPD. Both 4-PMPD and amphetamine had rapid onsets of action and produced peak effects within 10 min, whereas benzylpiperazine and phenmetrazine had slower onsets of action and typically did not produce peak effects until 30 min after their administration.2

In comparison to Benzylpiperazine (BZP) and (+)Phenmetrazine, 4-PMPD showed similarly potent and effective in vitro catecholamine releasing characteristics but with slightly better selectivity over serotonin (as measured in vivo using microdialysis to measure extracellular dopamine, norepinephrine and serotonin (5-HT) in the rat nucleus accumbens).2

4-PMPD was also found to be a weak reversible MAOI, somewhat selective for MAO-A, but the concentrations required for MAO inhibition were much greater than those enhancing dopamine release.3

Compound IC50 MAO-A IC50 MAO-B
4-PMPD 130 μM 750 μM

In a study of the effects of cocaine-induced pharmacodynamic tolerance on the DAT-mediated effects of dopamine reuptake inhibitors and dopamine releasers, it was demonstrated that, similar to cocaine, the DAT blockers nomifensine and bupropion were less effective at inhibiting dopamine uptake after cocaine self-administration; whereas the potencies of amphetamine-like dopamine releasers such as 3,4-methylenedioxymethamphetamine (MDMA), methamphetamine, amphetamine, and phentermine, as well as the non-amphetamine releaser, 4-PMPD, were all unaffected. Additionally, 4-PMPD and MDMA had comparable dopamine releasing potency and efficacy curves as measured by fast-scan cyclic voltammetry in rat brain slices.4

Unlike some more complex structural relatives, it was found that 4-PMPD did not induce pancreotoxicity. Fischer et al. suggested possible structural requirements for the high dose pancreotoxicity of cyproheptadine and related compounds containing a piperidine or piperazine ring substituted with a diphenylmethyl or similar group, finding that the structurally simplest compound which produced pancreatic islet cell vacuolization in rats was 4-diphenylmethylpiperidine5, which produced pancreatic islet cell vacuolization at doses of 34 mg / kg p.o.6 In contrast, 4-PMPD was tested up to 146 mg / kg p.o. in the rat, and 4-PMPD-treated rats exhibited normal pancreatic islet morphology at all doses.6

References:
1. Gray, Allan P., Donald E. Heitmeier, and Morton E. Goldberg. US Patent 3632767, issued 1972.
2. Negus SS, Baumann MH, Rothman RB, Mello NK, Blough BE. Selective suppression of cocaine- versus food-maintained responding by monoamine releasers in rhesus monkeys: benzylpiperazine, (+)phenmetrazine, and 4-benzylpiperidine. J Pharmacol Exp Ther. 2009;329(1):272-81. PMID: 19151247
3. Arai Y, Hamamichi N, Kinemuchi H. Time-dependent inhibition of rat brain monoamine oxidase by an analogue of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), 4-(4-chlorophenyl)-1,2,3,6-tetrahydropyridine. Neurosci Lett. 1986;70(2):255-60. PMID: 3490636
4. Ferris MJ, Calipari ES, Mateo Y, Melchior JR, Roberts DC, Jones SR. Cocaine self-administration produces pharmacodynamic tolerance: differential effects on the potency of dopamine transporter blockers, releasers, and methylphenidate. Neuropsychopharmacology. 2012;37(7):1708-16. PMID: 22395730
5. Hintze KL, Aboul-enein HY, Fischer LJ. Isomeric specificity of diphenylmethylpiperidine in the production of rat pancreatic islet cell toxicity. Toxicology. 1977;7(2):133-40. PMID: 324024
6. Fischer LJ, Wold JS, Rickert DE. Structure-activity relationships in drug-induced pancreatic islet cell toxicity. Toxicol Appl Pharmacol. 1973;26(2):288-98. PMID: 4356363

Czy mial ktos stycznosc z tym ?
Czy to legal czy nie ?

[Bogdan1988]

Kiedys kuz przewinela sie informacja ze moze byc za silne,pozniej pojawilo sie u jednego vendora.Ciekawa substancja chyba legalna.

scalanie - WRB

Dawkowanie 20-40mg
Czas dzialania 4-6h
Porownuja ja niektorzy do DMAA (suplementy diety)stosowanego przez kulturystow stymulantu do cwiczen zbabnowanego przez FDA
Po tym jak powoduje zwaly,arytmie zjazd.
Jest takze porownanie do noontropu stymulujacego czyli bylaby to po bromanatanie druga substancja noontropowo stymulujaca.
Efekty uboczne sa tez wedlug niektorych porownywalne do kawy.
Jest takze opinia ze jest imao-a nie powinien brany byc w ciagu wiecej jak 3dni.