Pregabalin Raw Materials Pregabalin Powder

CAS:148553-50-8

MF:C8H17NO2

MW:159.23

EINECS:604-639-1

Specification: 99% min PregabalinPowder

Sample:Pregabalin Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Pregabalin Powder Usage and Synthesis.

Pregabalin may reduce calcium-dependent release of some neurotransmitters by modulating calcium channel function.

Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or benzodiazepine-like receptors, does not increase GABAA responses in in vitro-cultured neurons, does not alter GABA concentrations in rat brain, and has no acute effects on GABA uptake or degradation.

However, it was found that prolonged exposure of in vitro cultured neurons to pregabalin increased GABA transporter protein density and functional GABA transport rate.

Pregabalin does not block sodium channels, is inactive at opioid receptors, does not alter cyclooxygenase activity, is inactive at dopamine and 5-hydroxytryptamine receptors, and does not inhibit dopamine, 5-hydroxytryptamine, or norepinephrine reuptake.

Uses and functions of Pregabalin.

Pregabalin is primarily used for the treatment of peripheral neuralgia as well as adjunctive treatment of limited partial seizures.

Pharmacological Effect of Pregabalin.

Pregabalin has a favourable therapeutic effect on epilepsy, and studies in various animal seizure models have shown that pregabalin significantly blocks seizures at doses that produce active effects 3-10 times lower than gabapentin.

Pregabalin was found to reduce sensory and motor spinal reflexes stimulated by toe-clamping in rats, reduce behaviours associated with diabetes mellitus, peripheral nerve injury, or chemotherapeutic neurological animal models of pain, and inhibit or reduce behaviours associated with pain induced by spinal administration of stimulants.

Experimental animal studies have found that pregabalin may be advantageous in combination with opioids. Pregabalin offers a new option for the clinical treatment of neuropathic pain.

Synthetics of  Bulk Pregabalin Powder.

Condensation of diethyl malonate and 3-methylbutyraldehyde in the presence of diisopropylamine gave 98. The latter was subjected to double bond addition with KCN and hydrolysed and decarboxylated to give the racemic pregabalin 96. Racemic pregabalin was subjected to crystallographic splitting by formation of a diastereoisomeric salt with S-(+)-mandelic acid to give the optically pure S-isomer.