AVN-211

AVN-211
Clinical data
Other names	CD-008-0173
Identifiers
	IUPAC name 5,7-dimethyl-2-(methylsulfanyl)-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine;
CAS Number	1173103-84-8;
ChemSpider	26387125;
ChEMBL	ChEMBL1668500;
CompTox Dashboard (EPA)	DTXSID001032056 ;
Chemical and physical data
Formula	C15H15N3O2S2
Molar mass	333.42 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1cc(n2c(n1)c(c(n2)SC)S(=O)(=O)c3ccccc3)C;
	InChI InChI=1S/C15H15N3O2S2/c1-10-9-11(2)18-14(16-10)13(15(17-18)21-3)22(19,20)12-7-5-4-6-8-12/h4-9H,1-3H3; Key:KSAUCBGUWGWPDL-UHFFFAOYSA-N;

AVN-211 (CD-008-0173) is a drug which acts as a highly selective 5-HT₆ receptor antagonist and is under development by Avineuro Pharmaceuticals for the treatment of schizophrenia.^[1]^[2]^[3] In early 2011, it successfully completed phase IIa clinical trials,^[1]^[4] with benefits on positive symptoms and some procognitive effects observed,^[5] and in mid 2013, phase IIb clinical trials for schizophrenia began.^[6] Avineuro Pharmaceuticals also expressed intention to start clinical trials of AVN-211 for Alzheimer's disease in 2015.^[6]^[7]^{[needs update]}

References

^ ^a ^b Ellenbroek BA, Cesura AM (13 October 2014). "Antipsychotics and the Dopamine-Serotonin Connection". In Celanire S, Poli S (eds.). Small Molecule Therapeutics for Schizophrenia. Springer. pp. 31, 37. ISBN 978-3-319-11502-3.
^ Pharmacology of 5-HT6 receptors. Academic Press. 7 December 2010. pp. 164–. ISBN 978-0-12-384977-9.
^ "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595. S2CID 8513976.
^ "Avineuro Pharmaceuticals, Inc. Reports positive Phase 2a clinical proof of concept trial results on AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.
^ Morozova MA, Lepilkina TA, Rupchev GE, Beniashvily AG, Burminskiy DS, Potanin SS, et al. (August 2014). "Add-on clinical effects of selective antagonist of 5HT6 receptors AVN-211 (CD-008-0173) in patients with schizophrenia stabilized on antipsychotic treatment: pilot study". CNS Spectrums. 19 (4): 316–323. doi:10.1017/S1092852913000394. PMID 23768250. S2CID 25486838.
^ ^a ^b "Avineuro Pharmaceuticals, Inc. Announces beginning of Phase 2b clinical studies of AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.
^ Ivachtchenko AV, Lavrovsky Y, Ivanenkov YA (March 2016). "AVN-211, Novel and Highly Selective 5-HT6 Receptor Small Molecule Antagonist, for the Treatment of Alzheimer's Disease". Molecular Pharmaceutics. 13 (3): 945–963. doi:10.1021/acs.molpharmaceut.5b00830. PMID 26886442.

External links

Pipeline - Avineuro Pharmaceuticals, Inc.

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[CelanirePoli2014-1] Ellenbroek BA, Cesura AM (13 October 2014). "Antipsychotics and the Dopamine-Serotonin Connection". In Celanire S, Poli S (eds.). Small Molecule Therapeutics for Schizophrenia. Springer. pp. 31, 37. ISBN 978-3-319-11502-3.

[2] Pharmacology of 5-HT6 receptors. Academic Press. 7 December 2010. pp. 164–. ISBN 978-0-12-384977-9.

[3] "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595. S2CID 8513976.

[Avineuro2011-4] "Avineuro Pharmaceuticals, Inc. Reports positive Phase 2a clinical proof of concept trial results on AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.

[MorozovaLepilkina2013-5] Morozova MA, Lepilkina TA, Rupchev GE, Beniashvily AG, Burminskiy DS, Potanin SS, et al. (August 2014). "Add-on clinical effects of selective antagonist of 5HT6 receptors AVN-211 (CD-008-0173) in patients with schizophrenia stabilized on antipsychotic treatment: pilot study". CNS Spectrums. 19 (4): 316–323. doi:10.1017/S1092852913000394. PMID 23768250. S2CID 25486838.

[Avineuro2013-6] "Avineuro Pharmaceuticals, Inc. Announces beginning of Phase 2b clinical studies of AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.

[7] Ivachtchenko AV, Lavrovsky Y, Ivanenkov YA (March 2016). "AVN-211, Novel and Highly Selective 5-HT6 Receptor Small Molecule Antagonist, for the Treatment of Alzheimer's Disease". Molecular Pharmaceutics. 13 (3): 945–963. doi:10.1021/acs.molpharmaceut.5b00830. PMID 26886442.

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v t e Antipsychotics (N05A)
Typical	Butyrophenones: Benperidol Bromperidol Bromperidol decanoate Droperidol Haloperidol^# Haloperidol decanoate Moperone Pipamperone Spiperone Timiperone Trifluperidol Diphenylbutylpiperidines: Fluspirilene Penfluridol Pimozide Phenothiazines: Acepromazine Acetophenazine Butaperazine Carphenazine (carfenazine)^‡ Chlorpromazine Cyamemazine Dixyrazine Fluphenazine Fluphenazine decanoate Fluphenazine enanthate Levomepromazine (methotrimeprazine) Mesoridazine Perazine Periciazine Perphenazine BL-1020 Perphenazine decanoate Perphenazine enanthate Piperacetazine Pipotiazine Pipotiazine palmitate Pipotiazine undecylenate Prochlorperazine Promazine Sulforidazine Thiopropazate Thioproperazine Thioridazine Trifluoperazine Triflupromazine Thioxanthenes: Chlorprothixene Clopenthixol Clopenthixol decanoate Flupentixol Flupentixol decanoate Tiotixene (thiothixene) Zuclopenthixol Zuclopenthixol acetate Zuclopenthixol decanoate
Disputed	Benzamides: Amisulpride Levosulpiride Nemonapride Remoxipride^‡ Sulpiride Sultopride Tiapride Veralipride^‡ Butyrophenones: Melperone Tricyclics: Carpipramine Clocapramine Clorotepine Clotiapine Loxapine Mosapramine Oxyprothepin decanoate Others: Molindone
Atypical	Benzisoxazole/benzisothiazoles: Iloperidone Lurasidone Paliperidone Paliperidone palmitate Perospirone Risperidone^# Ziprasidone Butyrophenones: Lumateperone Phenylpiperazines/quinolinones: Aripiprazole Aripiprazole lauroxil Brilaroxazine^† Brexpiprazole Cariprazine Tricyclics: Asenapine Clozapine^# Olanzapine (+samidorphan) Quetiapine Zotepine Others: Blonanserin Pimavanserin Sertindole
Others	Monoamine-depleting agents: Oxypertine Reserpine Tetrabenazine Others/unknown: Azacyclonol Xanomeline/trospium chloride
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

See also

References

External links