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Unlike the S enantiometer, the FDA has not given approval to Arketamine as an antidepressant–yet. However, there are both promising preclinical research and open-label trials showing Arketamine may be superior for severe depression. Arketamine shows weaker activity at the NMDA and sigma receptors. As a result, it produces fewer hallucinogenic and dissociative effects than esketamine.

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sketamine: new therapy for severe depression

Intranasal esketamine, the S-enantiomer of ketamine, was recently approved in the United States for the treatment of treatment-resistant depression (TRD). The findings from limited clinical trials indicate that intranasal esketamine is effective and safe in patients with TRD, although the optimum dose, duration and frequency of use are not fully understood. Its use in practice may be limited by cost and administrative regulation, and further long-term data are required.

GENERAL MECHANISM OF ACTION

Buy The Best R ketamineproduces its neurotherapeutic effects by binding to the NMDA receptor, a glutamate-gated ion-channel receptor located at most excitatory synapses in the brain and the spinal cord.^26, 27 The NMDA receptor is vital for memory, learning and synaptic plasticity.²⁷ Findings show that the NMDA receptor induces synaptic plasticity in response to glutamate signalling. Changes in synaptic plasticity are associated with many neurological diseases.^27, 28 According to clinical findings, synaptic plasticity and neurogenesis play a major role in the pathophysiology of MDD.²⁹

Ketamine noncompetitively antagonizes the activation of NMDA receptors resulting in decreased synaptic plasticity.²⁶ However, there are a number of theories regarding ketamine’s mechanism of action as an antidepressant. This includes blockage of the NMDA receptor, GABAergic interneuron disinhibition and direct actions of its hydroxynorketamine (HNK) metabolites.³⁰ The most discussed hypothesis is the inhibition of the NMDA receptor and the activation of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, resulting in antidepressant efficacy.³¹

Activation of AMPA receptors also leads to other downstream mechanisms including the release of brain-derived neurotrophic factor (BDNF) and the induction of mechanistic target of rapamycin involved in the regulation of synaptic plasticity.^32, 33 Ketamine and esketamine have a rapid onset of antidepressant effects via the activation of AMPA receptors.³⁴ Interestingly, Ho et al., showed that the expression of AMPA receptors can be augmented by oestradiol (E2) via oestrogen receptor (ER) in vitro.³⁴ It was shown that ketamine and its metabolites can bind to ER alpha (Erα), resulting in transcriptional inductive expression of AMPA receptors.³⁴