Pharmacology of vorozole

Wouters, Walter; Ginckel, R. Van; Krekels, Marita D.W.G.; Bowden, Charles R.; Coster, R. De

doi:10.1016/0960-0760(93)90268-2

Cited by 29 publications

(9 citation statements)

References 11 publications

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“…The (þ) enantiomer was found to be a highly potent inhibitor, being 1.5 and 10 times more active than its racemate and the (À) enantiomer, respectively. This result confirms the importance of the chiral center configuration towards aromatase inhibition, as previously observed for vorozole [23] and for indole derivatives [21].…”

Section: Aromatase Inhibitory Activitysupporting

confidence: 89%

Lead optimization of 4-imidazolylflavans: New promising aromatase inhibitors

Yahiaoui

Pouget

Buxeraud

et al. 2011

European Journal of Medicinal Chemistry

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Section: Aromatase Inhibitory Activitysupporting

confidence: 89%

Lead optimization of 4-imidazolylflavans: New promising aromatase inhibitors

Yahiaoui

Pouget

Buxeraud

et al. 2011

European Journal of Medicinal Chemistry

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“…In a first experiment, half of the subjects in each group were injected intraperitoneally with the nonsteroidal aromatase inhibitor vorozole (4.8 mg/kg body weight; Janssen Pharmaceutica, Beerse, Belgium) (Wouters et al, 1993). The other half received the vehicle solution (mix of polyethylene glycol and 0.9% saline, 3/1 v/v; also used for all steroids injected in this study).…”

Section: Methodsmentioning

confidence: 99%

Rapid Regulation of Pain by Estrogens Synthesized in Spinal Dorsal Horn Neurons

2004

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In addition to exerting genomic actions via nuclear receptors within hours to days, estrogens also regulate neuronal activity much faster (within seconds) by activating neuronal membrane receptors coupled to intracellular second-messenger pathways. To date, the origin of estrogens inducing rapid effects in the brain remains unclear, although it is often ascribed to the gonads. We report here that an acute blockade of the endogenous synthesis of estrogens in the quail spinal dorsal horn markedly reduced, within 1 min, the behavioral responsiveness to a thermal painful stimulus. Similar rapid effects in the opposite direction were induced by estradiol. This finding identifies a new paracrine and nongenomic mechanism for the regulation of pain by estrogens. Such regulation was assumed previously to result only from slow genomic actions of estrogens arising from the ovaries. Also, quite importantly, this finding suggests that the numerous rapid nongenomic effects of estrogens in the CNS could depend on their immediate local production by the enzyme aromatase, independently from the gonads.

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“…FMTO visualizes adrenal cortical tumours (41–43), and FVOZ targets the enzyme aromatase (44). The likelihood is low that AAA tissue would have receptors for astrocytes, CEA, mitochondrial cytochrome P-450 species found in the adrenal cortex, or aromatase, but it cannot be entirely ruled out.…”

Section: Discussionmentioning

confidence: 99%

“…Vorozole, 6-[(4-chlorophenyl)(1,2,4-triazol-1-yl)methyl]-1-methylbenzotriazole, is a selective and potent non-steroidal aromatase enzyme inhibitor (44). [ 18 F]Vorozole (45) is an analogue with similar affinity to aromatase (K d = 0.21 nM) (46), an enzyme that converts androgen to estrogens.…”

Section: Methodsmentioning

confidence: 99%

Autoradiography screening of potential positron emission tomography tracers for asymptomatic abdominal aortic aneurysms

Tegler

Estrada

Hall

et al. 2014

Upsala Journal of Medical Sciences

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Objective The aetiology and early pathophysiological mechanisms of aortic aneurysm formation are still unknown and challenging to study in vivo. Positron emission tomography (PET) is a potentially valuable instrument for non-invasive in vivo pathophysiological studies. No specific tracer to identify the pathophysiological process of aneurysmal dilatation is yet available, however. The aim of this study was to explore if different PET tracers could be useful to image aneurysmal disease.Methods and results Human aneurysmal aortic tissue, collected during elective resection of abdominal aortic aneurysm (AAA) of asymptomatic patients, was investigated in vitro by means of autoradiography with [68Ga]CRP-binder targeting C-reactive protein, [11C]DAA1106 targeting translocator protein (18 kDa), [11C]D-deprenyl with unknown target receptor, [11C]deuterium-L-deprenyl targeting astrocytes, [18F]fluciclatide targeting integrin αVβ3, [68Ga]IMP461 and bi-specific antibody TF2 052107 targeting carcinoembryonic antigen, [18F]F-metomidate targeting mitochondrial cytochrome P-450 species in the adrenal cortex, and [18F]vorozole targeting aromatase. Of the investigated tracers, only [18F]fluciclatide exhibited specific binding, whereas the other PET tracers failed to show specific uptake in the investigated tissue and are probably not useful for the intended purpose.Conclusion It seems likely that αVβ3 integrin expression in AAA can be visualized with PET and that the αVβ3 selective tracer, [18F]fluciclatide, may be suitable for in vivo molecular imaging of asymptomatic AAA. Additional evaluation of [18F]fluciclatide and αVβ3 integrin expression in AAA will be performed in vitro as well as in vivo.

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Pharmacology of vorozole

Cited by 29 publications

References 11 publications

Lead optimization of 4-imidazolylflavans: New promising aromatase inhibitors

Lead optimization of 4-imidazolylflavans: New promising aromatase inhibitors

Rapid Regulation of Pain by Estrogens Synthesized in Spinal Dorsal Horn Neurons

Autoradiography screening of potential positron emission tomography tracers for asymptomatic abdominal aortic aneurysms

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