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Diazoxide

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Diazoxide chemical structure
Diazoxide

7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
IUPAC name
CAS number
364-98-7
ATC code

C02DA01 .

PubChem
3019
DrugBank
APRD00914
Chemical formula {{{chemical_formula}}}
Molecular weight 230.672 g/mol
Bioavailability
Metabolism Hepatic oxidation and sulfate conjugation
Elimination half-life 21-45 hours
Excretion Renal
Pregnancy category {{{pregnancy_category}}}
Legal status {{{legal_status}}}
Routes of administration Oral, intravenous

Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.

It is used as a vasodilator in the treatment of acute hypertension, and also to decrease the secretion of insulin in disease states such as insulinoma (a tumor producing insulin).


Diazoxide chemical structure
Diazoxide

7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
IUPAC name
CAS number
364-98-7
ATC code

C02DA01 .

PubChem
3019
DrugBank
APRD00914
Chemical formula {{{chemical_formula}}}
Molecular weight 230.672 g/mol
Bioavailability
Metabolism Hepatic oxidation and sulfate conjugation
Elimination half-life 21-45 hours
Excretion Renal
Pregnancy category {{{pregnancy_category}}}
Legal status {{{legal_status}}}
Routes of administration Oral, intravenous

Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.

It is used as a vasodilator in the treatment of acute hypertension, and also to decrease the secretion of insulin in disease states such as insulinoma (a tumor producing insulin).

ReferencessEdit

  • Avshalumov, M. V., Chen, B. T., Koos, T., Tepper, J. M., & Rice, M. E. (2005). Endogenous Hydrogen Peroxide Regulates the Excitability of Midbrain Dopamine Neurons via ATP-Sensitive Potassium Channels: Journal of Neuroscience Vol 25(17) Apr 2005, 4222-4231.
  • Chi, X. X., Jiang, X., & Nicol, G. D. (2007). ATP-sensitive potassium currents reduce the PGE-sub-2-mediated enhancement of excitability in adult rat sensory neurons: Brain Research Vol 1145 May 2007, 28-40.
  • Cockhill, L. A., & Remick, R. A. (1987). Blood pressure effects of monoamine oxidase inhibitors: The highs and lows: The Canadian Journal of Psychiatry / La Revue canadienne de psychiatrie Vol 32(9) Dec 1987, 803-808.
  • Farkas, E., Institoris, A., Domoki, F., Mihaly, A., Luiten, P. G. M., & Bari, F. (2004). Diazoxide and dimethyl sulphoxide prevent cerebral hypoperfusion-related learning dysfunction and brain damage after carotid artery occlusion: Brain Research Vol 1008(2) May 2004, 252-260.
  • Hensley, I. E. (2000). Effects of diazoxide on NPY content in discrete brain nuclei of lean and obese zucker rats. Dissertation Abstracts International: Section B: The Sciences and Engineering.
  • Khalilzadeh, O., Anvari, M., Khalilzadeh, A., Sahebgharani, M., & Zarrindast, M. R. (2008). Involvement of amlodipine, diazoxide, and glibenclamide in development of morphine tolerance in mice: International Journal of Neuroscience Vol 118(4) Apr 2008, 503-518.
  • Kong, L.-L., & Yu, L.-C. (2006). It is AMPA receptor, not kainate receptor, that contributes to the NBQX-induced antinociception in the spinal cord of rats: Brain Research Vol 1100(1) Jul 2006, 73-77.
  • Niaki, S. E. A., Shafaroodi, H., Ghasemi, M., Shakiba, B., Fakhimi, A., & Dehpour, A. R. (2008). Mouth breathing increases the pentylenetetrazole-induced seizure threshold in mice: A role for ATP-sensitive potassium channels: Epilepsy & Behavior Vol 13(2) Aug 2008, 284-289.
  • Yang, Y., Liu, X., Long, Y., Wang, F., Ding, J.-H., Liu, S.-Y., et al. (2006). Activation of mitochondrial ATP-sensitive potassium channels improves rotenone-related motor and neurochemical alterations in rats: International Journal of Neuropsychopharmacology Vol 9(1) Feb 2006, 51-61.
  • Zarrindast, M. R., Jafari, M. R., Shafaghi, B., & Djahanguiri, B. (2004). Influence of potassium channel modulators on morphine state-dependent memory of passive avoidance: Behavioural Pharmacology Vol 15(2) Mar 2004, 103-110.

Template:Antihypertensives and diuretics


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