175013-84-0 Usage
Uses
Different sources of media describe the Uses of 175013-84-0 differently. You can refer to the following data:
1. It is a cholinesterase inhibitor for treating and preventing migraine. An antimigraine agent
2. It is a cholinesterase inhibitor for treating and preventing migraine. An antimigraine agent.
Biological Activity
migraine is a common, recurrent and primary headache disorder. optimisation of novel cis- and trans-4-(substituted-anfido)benzopyran-3-ol derivatives has led to the identification of tonabersat (sb-220453) with potential antimigraine activity.
Biochem/physiol Actions
Tonabersat (SB-220453) exhibits anticonvulsant property. It is a member of the family of novel benzoylamino-benzopyran compounds. Tonabersat is used as a therapeutic for trigeminal nerve-induced neurovascular reflexes. In addition, it acts as a putative migraine prophylactic agent containing an unique stereospecific binding site in the brain.
in vitro
topiramate targets multiple cortical and subcortical loci, altering voltage-gated ion channels and chemical transmission to decrease abnormal brain excitability. preclinical studies have identified four properties that may account for the drug’s efficacy in epilepsy and migraine prophylaxis: (i) blockage of voltage-dependent sodium channels; (ii) augmentation of the activity of the neurotransmitter g-aminobutyric acid (gaba) at some subtypes of the gaba-a receptor; (iii) antagonism of the ampa/kainate subtype of the glutamate receptor; and (iv) inhibition of the carbonic anhydrase enzymes, particularly isozymes ii and iv [1].
in vivo
tonabersat binds selectively to a unique site in the brain. moreover, tonabersat could markedly reduce cortical spreading depression (csd) and csd-associated events and inhibite gap-junction communication between neurons and satellite glial cells in the trigeminal ganglion. together, these findings indicate that tonabersat should have clinical application in preventing migraine attacks [2].
references
[1] silberstein sd. tonabersat, a novel gap-junction modulator for the prevention of migraine. cephalalgia. 2009;29 suppl 2:28-35. [2] durham pl, garrett fg. neurological mechanisms of migraine: potential of the gap-junction modulator tonabersat in prevention of migraine. cephalalgia. 2009;29 suppl 2:1-6. [3] hauge aw, asghar ms, schytz hw, christensen k, olesen j. effects of tonabersat on migraine with aura: a randomised, double-blind, placebo-controlled crossover study. lancet neurol. 2009;8(8):718-23.
Check Digit Verification of cas no
The CAS Registry Mumber 175013-84-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,5,0,1 and 3 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 175013-84:
(8*1)+(7*7)+(6*5)+(5*0)+(4*1)+(3*3)+(2*8)+(1*4)=120
120 % 10 = 0
So 175013-84-0 is a valid CAS Registry Number.
InChI:InChI=1/C20H19ClFNO4/c1-10(24)11-5-7-16-13(8-11)17(18(25)20(2,3)27-16)23-19(26)12-4-6-15(22)14(21)9-12/h4-9,17-18,25H,1-3H3,(H,23,26)/t17-,18-/m0/s1
175013-84-0Relevant articles and documents
PRODRUG COMPOUNDS
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Page/Page column 31; 32; 33, (2015/07/15)
A compound of formula (Ia) or (Ib), or a pharmaceutically acceptable salt thereof, Wherein Q, R2, Ar, A and R1 are as defined in claim 1. The claimed compounds are gap junction blockers useful for the treatment or prevention of a ran
Treatment
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, (2008/06/13)
The invention relates to certain cis and trans benzopyrans having substituted benzamides at position C-4 and to their use in treating and/or preventing certain CNS disorders.
