The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Estulic     N-(diaminomethylidene)-2- (2,6...

Synonyms: Intuniv, GUANFACINE, Guanfacina, Guanfacinum, CHEMBL862, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of GUANFACINE

  • The ability of low doses of guanfacine to improve memory without inducing hypotension or sedation indicates that this agonist may be an excellent candidate for treating memory disorders in man [1].
  • Tic severity decreased by 31% in the guanfacine group, compared to 0% in the placebo group [2].
  • Compared with placebo, side-effect frequency was higher for flushing and edema with isradipine, and dry mouth was more frequent with added guanfacine [3].
  • Effects of single and multiple doses of guanfacine in essential hypertension [4].
  • Our data suggest that guanfacine exerts its antihypertensive effect via the inhibition of sympathetic outflow and in part the suppression of the reninangiotensin-aldosterone system and that guanfacine is suitable for the effective treatment of hypertension associated with chronic glomerulonephritis [5].

Psychiatry related information on GUANFACINE


High impact information on GUANFACINE


Chemical compound and disease context of GUANFACINE


Biological context of GUANFACINE


Anatomical context of GUANFACINE

  • Both UK-14,304 and guanfacine were found to reduce the production of cyclic AMP (cAMP) in the spinal cord, as determined using an in vitro radioisotopic method [20].
  • A wide area of increased rCBF was seen in the frontal lobe, maximal at the central region, following guanfacine in controls and subjects with TLE [21].
  • 1. Simultaneous computer modelling of control and guanfacine-masked [3H]-MK 912 saturation curves as well as guanfacine competition curves revealed that the drugs bound to two alpha 2-adrenoceptor subtypes in the rat cerebral cortex with very different selectivities [22].
  • The tritium-labeled alpha-adrenoceptor agonist and antihypertensive drug guanfacine, N-amidino-2-(2,6-dichlorophenyl)-acetamide (sp. act. 24.2 Ci/mmole) was employed for a direct identification and characterization of alpha-adrenoceptors in rat brain membranes [19].
  • A 31 gauge needle was advanced into the renal artery for infusion of the alpha 2a/d-selective agonist, guanfacine (vehicle, 1.0, 3.0 and 10.0 nmol kg-1 min-1 in Wistar and SH rats; vehicle and 10.0 nmol kg-1 min-1 in Wistar 1K-sham and 1K-1C rats) [23].

Associations of GUANFACINE with other chemical compounds


Gene context of GUANFACINE

  • The effects of guanfacine on performance of the delayed alternation task were assessed in additional groups of wild-type versus alpha2A-AR mutant mice [27].
  • Guanfacine stimulated GH secretion significantly in four of these five patients [13].
  • In the present study, we compared the effects on GH secretion of two compounds (bromocriptine and TRH), which presumably act directly at the pituitary level, with the effect of the centrally acting alpha-adrenergic agonist guanfacine in 14 untreated acromegalic patients [13].
  • We examined the effect of intrathecal (i.t.) administration of the non-selective alpha 2-adrenoceptor agonist clonidine and the alpha 2A-adrenoceptor selective agonist guanfacine on flexor reflex excitability in decerebrate, spinalized, unanesthetized rats before and after unilateral section of the sciatic nerve [28].
  • CONCLUSION: The results indicate that guanfacine improved poor noradrenergic modulation of neuronal circuits that involve the frontal lobes in an animal model of ADHD [29].

Analytical, diagnostic and therapeutic context of GUANFACINE


  1. The alpha-2 adrenergic agonist guanfacine improves memory in aged monkeys without sedative or hypotensive side effects: evidence for alpha-2 receptor subtypes. Arnsten, A.F., Cai, J.X., Goldman-Rakic, P.S. J. Neurosci. (1988) [Pubmed]
  2. A placebo-controlled study of guanfacine in the treatment of children with tic disorders and attention deficit hyperactivity disorder. Scahill, L., Chappell, P.B., Kim, Y.S., Schultz, R.T., Katsovich, L., Shepherd, E., Arnsten, A.F., Cohen, D.J., Leckman, J.F. The American journal of psychiatry. (2001) [Pubmed]
  3. Isradipine in essential hypertension: the Belgian General Practitioners' Study. De Keyser, P., Bouvé, J., Clement, D., Degraef, R., Meurant, J.P., Rorive, G., Van Thillo, J. Am. J. Med. (1989) [Pubmed]
  4. Effects of single and multiple doses of guanfacine in essential hypertension. Zamboulis, C., Reid, J.L. Clin. Pharmacol. Ther. (1980) [Pubmed]
  5. Effects of guanfacine monotherapy on blood pressure, heart rate, plasma renin activity, aldosterone, and catecholamines in hypertensive patients with chronic glomerulonephritis. Ikeda, T., Gomi, T., Yuhara, M., Sakurai, J., Nakayama, D. Clin. Pharmacol. Ther. (1988) [Pubmed]
  6. Pharmacological options for the treatment of Tourette's disorder. Jiménez-Jiménez, F.J., García-Ruiz, P.J. Drugs (2001) [Pubmed]
  7. Clonidine, but not guanfacine, impairs choice reaction time performance in young healthy volunteers. Jäkälä, P., Riekkinen, M., Sirviö, J., Koivisto, E., Riekkinen, P. Neuropsychopharmacology (1999) [Pubmed]
  8. The alpha-2A-adrenoceptor agonist, guanfacine, increases regional cerebral blood flow in dorsolateral prefrontal cortex of monkeys performing a spatial working memory task. Avery, R.A., Franowicz, J.S., Studholme, C., van Dyck, C.H., Arnsten, A.F. Neuropsychopharmacology (2000) [Pubmed]
  9. Guanfacine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of hypertension. Sorkin, E.M., Heel, R.C. Drugs (1986) [Pubmed]
  10. Identification of vascular postsynaptic alpha 1- and alpha 2-adrenoceptors in man. Jie, K., van Brummelen, P., Vermey, P., Timmermans, P.B., van Zwieten, P.A. Circ. Res. (1984) [Pubmed]
  11. Noradrenergic modulation of space exploration in visual neglect. Malhotra, P.A., Parton, A.D., Greenwood, R., Husain, M. Ann. Neurol. (2006) [Pubmed]
  12. The noradrenergic alpha2 agonist clonidine modulates behavioural and neuroanatomical correlates of human attentional orienting and alerting. Coull, J.T., Nobre, A.C., Frith, C.D. Cereb. Cortex (2001) [Pubmed]
  13. Different responses of growth hormone secretion to guanfacine, bromocriptine, and thyrotropin-releasing hormone in acromegalic patients with pure growth hormone (GH)-containing and mixed GH/prolactin-containing pituitary adenomas. Lamberts, S.W., Klijn, J.G., van Vroonhoven, C.C., Stefanko, S.Z. J. Clin. Endocrinol. Metab. (1985) [Pubmed]
  14. Behavioral and receptor binding analysis of the alpha 2-adrenergic agonist, 5-bromo-6 [2-imidazoline-2-yl amino] quinoxaline (UK-14304): evidence for cognitive enhancement at an alpha 2-adrenoceptor subtype. Arnsten, A.F., Leslie, F.M. Neuropharmacology (1991) [Pubmed]
  15. Effects of clonidine and guanfacine in essential hypertension. Farsang, C., Varga, K., Vajda, L., Alföldi, S., Kapocsi, J. Clin. Pharmacol. Ther. (1984) [Pubmed]
  16. Guanfacine kinetics in patients with hypertension. Weiss, Y.A., Lavene, D.L., Safar, M.E., Simon, A.C., Loria, Y., Georges, D.R., Milliez, P.L. Clin. Pharmacol. Ther. (1979) [Pubmed]
  17. In summary: satellite symposium on central alpha-adrenergic blood pressure regulating mechanisms. Abrams, W.B. Hypertension (1984) [Pubmed]
  18. The influence of renal function on plasma concentration, urinary excretion and antihypertensive effect of guanfacine. Kirch, W., Köhler, H., Braun, W., von Gizycki, C. Clinical pharmacokinetics. (1980) [Pubmed]
  19. Binding characteristics of [3H]guanfacine to rat brain alpha-adrenoceptors. Comparison with [3H]clonidine. Timmermans, P.B., Schoop, A.M., van Zwieten, P.A. Biochem. Pharmacol. (1982) [Pubmed]
  20. Antinociceptive actions of alpha 2-adrenoceptor agonists in the rat spinal cord: evidence for antinociceptive alpha 2-adrenoceptor subtypes and dissociation of antinociceptive alpha 2-adrenoceptors from cyclic AMP. Uhlén, S., Persson, M.L., Alari, L., Post, C., Axelsson, K.L., Wikberg, J.E. J. Neurochem. (1990) [Pubmed]
  21. The effects of an alpha-2 adrenergic agonist, guanfacine, on rCBF in human cortex in normal controls and subjects with focal epilepsy. Swartz, B.E., Kovalik, E., Thomas, K., Torgersen, D., Mandelkern, M.A. Neuropsychopharmacology (2000) [Pubmed]
  22. [3H]-MK 912 binding delineates two alpha 2-adrenoceptor subtypes in rat CNS one of which is identical with the cloned pA2d alpha 2-adrenoceptor. Uhlén, S., Xia, Y., Chhajlani, V., Felder, C.C., Wikberg, J.E. Br. J. Pharmacol. (1992) [Pubmed]
  23. Renal alpha 2a/d-adrenoceptor subtype function: Wistar as compared to spontaneously hypertensive rats. Intengan, H.D., Smyth, D.D. Br. J. Pharmacol. (1997) [Pubmed]
  24. The alpha-adrenoceptor control of adrenocorticotropin secretion in man. Lancranjan, I., Ohnhaus, E., Girard, J. J. Clin. Endocrinol. Metab. (1979) [Pubmed]
  25. Clonidine-induced nitric oxide-dependent vasorelaxation mediated by endothelial alpha(2)-adrenoceptor activation. Figueroa, X.F., Poblete, M.I., Boric, M.P., Mendizábal, V.E., Adler-Graschinsky, E., Huidobro-Toro, J.P. Br. J. Pharmacol. (2001) [Pubmed]
  26. Yohimbine disrupts prepulse inhibition in rats via action at 5-HT1A receptors, not alpha2-adrenoceptors. Powell, S.B., Palomo, J., Carasso, B.S., Bakshi, V.P., Geyer, M.A. Psychopharmacology (Berl.) (2005) [Pubmed]
  27. Mutation of the alpha2A-adrenoceptor impairs working memory performance and annuls cognitive enhancement by guanfacine. Franowicz, J.S., Kessler, L.E., Borja, C.M., Kobilka, B.K., Limbird, L.E., Arnsten, A.F. J. Neurosci. (2002) [Pubmed]
  28. The effect of intrathecal guanfacine and clonidine on the flexor reflex in rats with intact and sectioned sciatic nerves. Xu, X.J., Wikberg, J.E., Wiesenfeld-Hallin, Z. Eur. J. Pharmacol. (1993) [Pubmed]
  29. The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Sagvolden, T. Behavioral and brain functions : BBF (2006) [Pubmed]
  30. Bradycardia during epidural anesthesia in a patient receiving guanfacine. Burney, R.G. Anesthesiology (1992) [Pubmed]
  31. The bioavailability and pharmacokinetics of guanfacine after oral and intravenous administration to healthy volunteers. Carchman, S.H., Crowe, J.T., Wright, G.J. Journal of clinical pharmacology. (1987) [Pubmed]
WikiGenes - Universities