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Chemical Compound Review

Precedex     4-[(1S)-1-(2,3- dimethylphenyl)ethyl]-3H...

Synonyms: CHEMBL778, Tocris-2023, AC1NSJXT, Precedex (TN), SureCN26433, ...
 
 
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Disease relevance of DEXMEDETOMIDINE

  • Thus, the dose ratio (ED50 at 60 degrees C/ED50 at 52.5 degrees C) for these three agents on the tail flick and blood pressure response was, respectively, 1.1 and 1.8 for DMET, 1.1 and 4.3 for CLON and 4.8 and 9.7 for ST-91 (mean +/- S.E.). On resting blood pressure, i.t. DMET and CLON produced a dose-dependent hypotension and bradycardia [1].
  • In the PENTO group, CBF increased from 31 +/- 3 to 137 +/- 24 mL.min-1.100 g-1 in response to hypercapnia (PCO2 approximately 90 mmHg) at pre-DEX and there was no change in normocapnic CBF or hypercapnic blood flow after DEX or atipamezole [2].
  • In mice pretreated with pertussis toxin, 2 microgram/mouse, given i.c.v. 72 h before the agonists, the decrease in cGMP induced by Dex or F was not affected, while the stimulatory effect of F was reversed to an inhibitory effect [3].
 

High impact information on DEXMEDETOMIDINE

  • CBF (radiolabeled microspheres) was determined during normocapnia and hypercapnia at baseline (pre-DEX), after DEX (10 micrograms/kg, intravenous bolus, plus an additional 5 micrograms/kg during hypercapnia), and after administration of a selective alpha 2-adrenergic receptor antagonist (atipamezole, 500 micrograms/kg, intravenous bolus) [2].
  • However, Dex significantly increased RASM cell migration, and antagonist blocked this effect [4].
 

Associations of DEXMEDETOMIDINE with other chemical compounds

References

  1. Suppression by spinal alpha-2 agonists of motor and autonomic responses evoked by low- and high-intensity thermal stimuli. Saeki, S., Yaksh, T.L. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  2. Alpha 2-adrenergic agonist effects on normocapnic and hypercapnic cerebral blood flow in the dog are anesthetic dependent. Fale, A., Kirsch, J.R., McPherson, R.W. Anesth. Analg. (1994) [Pubmed]
  3. Interaction of the alpha-2 adrenergic- and opioid receptor with the cGMP system in the mouse cerebellum. Vulliemoz, Y., Virag, L., Whittington, R.A. Brain Res. (1998) [Pubmed]
  4. Alpha 2-adrenergic receptors increase cell migration and decrease F-actin labeling in rat aortic smooth muscle cells. Richman, J.G., Regan, J.W. Am. J. Physiol. (1998) [Pubmed]
  5. Clinical efficacy of dexmedetomidine alone is less than propofol for conscious sedation during ERCP. Muller, S., Borowics, S.M., Fortis, E.A., Stefani, L.C., Soares, G., Maguilnik, I., Breyer, H.P., Hidalgo, M.P., Caumo, W. Gastrointest. Endosc. (2008) [Pubmed]
 
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