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Sarizotan

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Sarizotan
Clinical data

Pregnancy category	N/A
Routes of administration	Oral
ATC code	none
Legal status
Legal status	Discontinued
Identifiers
IUPAC name 1-[(2R)-3,4-dihydro-2H-chromen-2-yl]-N-([5-(4-fluorophenyl)pyridin-3-yl]methyl)methanamine
CAS Number	351862-32-3
PubChem CID	6918388
ChemSpider	2319847
UNII	467LU0UCUW
CompTox Dashboard (EPA)	DTXSID80956632
Chemical and physical data
Formula	C₂₂H₂₁FN₂O
Molar mass	348.421 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1CC2=CC=CC=C2O[C@H]1CNCC3=CN=CC(=C3)C4=CC=C(C=C4)F

Sarizotan (EMD-128,130) is a selective 5-HT_1A receptor agonist and D₂ receptor antagonist,^[1] which has antipsychotic effects,^[2]^[3] and has also shown efficacy in reducing dyskinesias resulting from long-term anti-Parkinsonian treatment with levodopa.^[4]^[5]^[6]^[7]

In June 2006, the developer Merck KGaA announced that the development of sarizotan was discontinued, after two sarizotan Phase III studies (PADDY I, PADDY II) failed to meet the primary efficacy endpoint and neither the Phase II findings nor the results from preclinical studies could be confirmed. No statistically significant difference of the primary target variable between sarizotan and placebo could be demonstrated.^[8]^[9]

References[edit]

^ Rabiner EA, Gunn RN, Wilkins MR, Sedman E, Grasby PM (September 2002). "Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with [11C]WAY-100635 and [11C]raclopride". Journal of Psychopharmacology. 16 (3): 195–9. doi:10.1177/026988110201600301. PMID 12236624. S2CID 12943982.

^ Assié MB, Ravailhe V, Faucillon V, Newman-Tancredi A (October 2005). "Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain". The Journal of Pharmacology and Experimental Therapeutics. 315 (1): 265–72. doi:10.1124/jpet.105.087163. PMID 15987834. S2CID 9262233.

^ Auclair AL, Galinier A, Besnard J, Newman-Tancredi A, Depoortère R (July 2007). "Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats". Psychopharmacology. 193 (1): 45–54. doi:10.1007/s00213-007-0762-7. PMID 17393144. S2CID 23379049.

^ Bibbiani F, Oh JD, Chase TN (November 2001). "Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models". Neurology. 57 (10): 1829–34. doi:10.1212/wnl.57.10.1829. PMID 11723272. S2CID 24836560.

^ Bartoszyk GD, Van Amsterdam C, Greiner HE, Rautenberg W, Russ H, Seyfried CA (February 2004). "Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile". Journal of Neural Transmission. 111 (2): 113–26. doi:10.1007/s00702-003-0094-7. PMID 14767715. S2CID 25419329.

^ Bara-Jimenez W, Bibbiani F, Morris MJ, Dimitrova T, Sherzai A, Mouradian MM, Chase TN (August 2005). "Effects of serotonin 5-HT1A agonist in advanced Parkinson's disease". Movement Disorders. 20 (8): 932–6. doi:10.1002/mds.20370. PMID 15791634. S2CID 46098045.

^ Grégoire L, Samadi P, Graham J, Bédard PJ, Bartoszyk GD, Di Paolo T (July 2009). "Low doses of sarizotan reduce dyskinesias and maintain antiparkinsonian efficacy of L-Dopa in parkinsonian monkeys". Parkinsonism & Related Disorders. 15 (6): 445–52. doi:10.1016/j.parkreldis.2008.11.001. PMID 19196540.

^ "Merck KGaA: Development of Sarizotan to treat Parkinson's patients will not be pursued". Ad Hoc News. 23 June 2006.

^ "Merck KGaA discontinues development of Parkinson drug Sarizotan UPDATE". Forbes. 23 June 2006.^{[dead link]}

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
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Antiparkinson agents (N04)

Dopaminergics

DA precursors	Levodopa^# (+benserazide) Melevodopa
DA receptor agonists	Ergoline: Bromocriptine Cabergoline Dihydroergocryptine Lisuride Pergolide Non-ergoline: Apomorphine Piribedil Pramipexole Ropinirole Rotigotine Talipexole
MAO-B inhibitors	Rasagiline Safinamide Selegiline
COMT inhibitors	Entacapone Opicapone Tolcapone
AAAD inhibitors	Benserazide (+levodopa) Carbidopa^#