Xylazine CAS NO: 7361-61-7 Rompun, Anased, Sedazine, Chanazine
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Usage
Medical use
Toluene thiazide is commonly used as a sedative, muscle relaxant and analgesic. It is often used to treat tetanus. Xylazine is very similar to drugs such as phenothiazine, tricyclic antidepressants and clonidine. As an anesthetic, it is often used in combination with ketamine. Xylazine appears to reduce the body's sensitivity to insulin and glucose uptake. Yohimbine is an alpha2 adrenergic receptor antagonist that has been used to reduce glucose levels to healthy levels. Yohimbine reverses the side effects of toluene thiazide in a clinical setting if administered intravenously shortly after toluene thiazide is administered
pharmacodynamics
Xylazine is a potent alpha 2 adrenergic agonist. Toluene thiazide and other alpha2 adrenergic receptor agonists are distributed throughout the body within 30-40 minutes when given. Due to its high lipophilicity, toluene thiazide directly stimulates central α2 receptors as well as peripheral αadrenergic receptors in a variety of tissues. As an agonist, toluene thiazide results in reduced neurotransmission of norepinephrine and dopamine in the central nervous system. It does so by mimicking the binding of norepinephrine to autoreceptors on the presynaptic surface, which results in feedback inhibition of norepinephrine.
Xylazine also acts as a transport inhibitor by inhibiting norepinephrine transport function by competitively inhibiting substrate transport. Thus, toluene thiazide significantly increased K m and did not affect V max. This may occur through direct interaction with regions that overlap with antidepressant binding sites. For example, toluene thiazide and clonidine inhibit the uptake of MIBG (a norepinephrine analogue) by neuroblastoma cells. Xylazine has different affinities for cholinergic, serotonergic, dopaminergic, alpha1, adrenergic, H 2-histamine, and opioid receptors. Its chemical structure is very similar to that of phenothiazines, tricyclic antidepressants and clonidine