Pregabalin CAS 148553-50-8

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pregabalin vs gabapentin
Gabapentin and pregabalin vary in terms of binding affinity and potency. Pregabalin has an increased binding affinity for the alpha-2-delta protein and is a more potent analgesic in neuropathic pain compared with gabapentin.
Based on studies of gabapentin and pregabalin in epilepsy, the EC50 values of pregabalin and gabapentin were estimated to be about 9.77 mg/mL and 23.9 mg/mL, respectively.9 From these data, pregabalin was estimated to be about 2.4 times more potent. For neuropathic pain, pregabalin’s potency ratio may be even greater.
Using studies in postherpetic neuralgia, the EC50 values of pregabalin and gabapentin were estimated to be about 4.21 mg/mL and 11.7 mg/mL, respectively. Based on these values, pregabalin was estimated to be about 2.8 times more potent than gabapentin.

Pregabalin CAS 148553-50-8

1. Pregabalin CAS 148553-50-8 CAS  Product Information:

Product Name:Pregabalin
Synonyms:Lyrica;Pregabalin;Pregabalin;PREGABAIN;PREGABALIN;Neugaba 75;Pregabalin;Pregabalin;Maxgalin 75;TOS-BB-0910
CAS NO:148553-50-8
Molecular Weight:159.23
Molecular Formula:C8H17NO2
Boiling Point:274.0±23.0 °C
Melting point:194-196°C
Density:0.997±0.06 g/cm3
StorageStore at RT
Solubilitydeionized water: ≥10mg/mL
Appearance:white shiny powder
Applications:Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder.
EINECS   NO:604-639-1
Assay:99%

2. What is Pregabalin ?

Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsantanalgesic and anxiolytic medication used to treat epilepsyneuropathic painfibromyalgiarestless leg syndromeopioid withdrawal and generalized anxiety disorder (GAD).Pregabalin also has antiallodynic properties. Its use in epilepsy is as an add-on therapy for partial seizures.It is a gabapentinoid medication.When used before surgery, it reduces pain but results in greater sedation and visual disturbances. It is taken by mouth.

3.pregabalin mechanism of action

Pregabalin is structurally related to the antiepileptic drug gabapentin, and the two drugs have similar sites of action, namely the alpha2-delta (alpha2-delta) protein of the auxiliary subunit of voltage-gated calcium channels. Pregabalin subtly reduces synaptic release of several neurotransmitters, apparently by binding to the alpha2-delta subunit, and may explain its role in the body to reduce neuronal excitability and seizures.

Several studies have shown that the pharmacology of pregabalin requires binding to the alpha2-delta subunit, including structural activity analysis of compounds bound to the alpha2-delta subunit and pharmacology in mice with alpha2-delta type 1 protein binding defects. The preclinical findings to date are consistent with mechanisms that may be needed to reduce abnormal neuronal excitability by reducing neurotransmitter release.

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4. Pregabalin Use

Pregabalin is used as an anticonvulsant and antiepileptic; also used to treat neuropathic pain. Binds with high affinity and selectivity to the α2δ subunit of voltage-sensitive Ca2+ channels and modulate their activity. Displays anxiolytic-like activity in ethological and conflict models of anxiety.

5.pregabalin+methylcobalamin

pregabalin+methylcobalamin is a combination of two medicines: Pregabalin and Methylcobalamin. Pregabalin acts by decreasing the pain signals sent by a damaged nerve in the body. On the other hand, Methylcobalamin helps rejuvenate and protect damaged nerve cells by producing a substance called myelin (outer protective layer of nerve cell – neuron).

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