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Fabomotizole

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Fabomotizole.svg
Structure of FABOMOTIZOLE

Fabomotizole

Afobazole

  • Molecular FormulaC15H21N3O2S
  • Average mass307.411 Da

0F8K1X115C

173352-21-1[RN] 173352-21-1 (free base) 173352-39-1 (HCl) 189638-30-0 (2HCl) 

1H-Benzimidazole, 6-ethoxy-2-[[2-(4-morpholinyl)ethyl]thio]-

Obenoxazine, Afobazol, Afobazole, Aphobazole, Fabomotizole dihydrochloride, CM-346, CM346, CM 346,

фабомотизол[Russian][INN]

فابوموتيزول[Arabic][INN]

法莫替唑[Chinese][INN]

img

Fabomotizole dihydrochloride
CAS#: 189638-30-0 (2HCl)
Chemical Formula: C15H23Cl2N3O2S

Molecular Weight: 380.33

Fabomotizole (also known as Afobazole) is a selective non-benzodiazepine anxiolytic which was developed in Russia and launched in 2006. The drug is used for the treatment of wide range of diseases: generalized anxious disorders, neurasthenia, adaptation disorders, sleep disorders, for alleviation of withdrawal syndrome. According to the drug label (in Russian), its action is related to the interaction with sigma-1 receptors.

Fabomotizole (INN;[1] brand name Afobazole) is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions.[citation needed] Its mechanism of action remains poorly defined however, with GABAergicNGF– and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors.[2][3][4][5][6] Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety.[7]

Experiments of mice have shown antimutagenic and antiteratogenic properties.[8]

Fabomotizole has found little clinical use outside Russia and has not been evaluated by the FDA.

PATENT

WO 9534304

https://patents.google.com/patent/WO1995034304A1/en

Figure imgf000006_0001

PAPER

European Journal of Medicinal Chemistry (2021), 211, 113110

https://www.sciencedirect.com/science/article/abs/pii/S0223523420310825?

A ligand-based virtual screening study to search for giardicidal compounds on a 6551 ChEMBL drugs database was carried out using molecular similarity. Three fingerprints implemented in MayaChemTools with different design and validated by ROC curves, were used. Twelve compounds were retrieved from this screening, from which, four representative compounds were selected to carry out biological assays. Whereas two compounds were commercially available, the additional two compounds were synthesized during the development of this work. The biological assays revealed that the compounds possess in vitro activity against five strains of Giardia intestinalis, each with different susceptibility/resistance rates to metronidazole, albendazole and nitazoxanide. Particularly, tenatoprazole showed the best effect against the WB and IMSS strains. Furthermore, fabomotizole, tenatoprazole and ipriflavone showed a higher activity against resistant strains than the reference drugs: metronidazole, albendazole and nitazoxanide.

Graphical abstract

Image 1

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Clinical data
Trade namesAfobazole
Other namesFabomotizole
Routes of
administration
Oral
ATC codeN05BX04 (WHO)
Legal status
Legal statusUS: Unscheduled Not FDA approved
Pharmacokinetic data
Bioavailability43.64%, pronounced first-pass effect
Metabolismextensive hepatic
Onset of action0.85±0.13 hours
Elimination half-life0.82±0,54 hours
Identifiers
showIUPAC name
CAS Number173352-39-1 
PubChem CID9862937
ChemSpider8038633 
UNIIHDO6HX6NZU
CompTox Dashboard (EPA)DTXSID00169606 
Chemical and physical data
FormulaC15H21N3O2S
Molar mass307.41 g·mol−1
3D model (JSmol)Interactive image
showSMILES
showInChI
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References

  1. ^ “International Nonproprietary Names for Pharmaceutical Substances (INN)” (PDF). WHO Drug Information26 (1): 63. 2012. Retrieved 21 March 2015.
  2. ^ Neznamov, GG; Siuniakov, SA; Chumakov, DV; Bochkarev, VK; Seredenin, SB (2001). “Clinical study of the selective anxiolytic agent afobazol”. Eksperimental’naia i Klinicheskaia Farmakologiia64 (2): 15–9. PMID 11548440.
  3. ^ Silkina, IV; Gan’shina, TC; Seredin, SB; Mirzoian, RS (2005). “Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon”. Eksperimental’naia i Klinicheskaia Farmakologiia68 (1): 20–4. PMID 15786959.
  4. ^ Seredin, SB; Melkumian, DS; Val’dman, EA; Iarkova, MA; Seredina, TC; Voronin, MV; Lapitskaia, AS (2006). “Effects of afobazole on the BDNF content in brain structures of inbred mice with different phenotypes of emotional stress reaction”. Eksperimental’naia i Klinicheskaia Farmakologiia69 (3): 3–6. PMID 16878488.
  5. ^ Antipova, TA; Sapozhnikova, DS; Bakhtina, LIu; Seredenin, SB (2009). “Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons”. Eksperimental’naia i Klinicheskaia Farmakologiia72 (1): 12–4. PMID 19334503.
  6. ^ Seredenin, SB; Antipova, TA; Voronin, MV; Kurchashova, SY; Kuimov, AN (2009). “Interaction of afobazole with sigma1-receptors”. Bulletin of Experimental Biology and Medicine148 (1): 42–4. doi:10.1007/s10517-009-0624-xPMID 19902093S2CID 37411324.
  7. ^ Medvedev, VE; Trosnova, AP; Dobrovol’skiĭ, AV (2007). “Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole”. Zh Nevrol Psikhiatr Im S S Korsakova107 (7): 25–9. PMID 18379478.
  8. ^ Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB (Jan–Feb 2009). “Antimutagenic and antiteratogenic properties of afobazole”. Eksp Klin Farmakol72 (1): 46–51. PMID 19334511.

//////////////Fabomotizole, Afobazole, фабомотизол , فابوموتيزول , 法莫替唑 , Obenoxazine, Afobazol, Afobazole, Aphobazole, Fabomotizole dihydrochloride, CM-346, CM346, CM 346,

 CCOc1ccc2c(c1)[nH]c(n2)SCCN3CCOCC3.Cl.Cl

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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