WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319572
CAS#: 195068-07-6 (HCl)
Description: Sarizotan, also known as EMD-128130, is a Dopamine D2 receptor partial agonist and Serotonin 1A receptor agonist. Sarizotan exhibits affinity at serotonin and dopamine receptors. Sarizotan effectively suppresses levodopa-induced dyskinesia in primate and rodent models of Parkinson's disease, and tardive dyskinesia in a rodent model. Sarizotan is a full agonist at D3 and D4.4 receptors (EC50=5.6 and 5.4 nM, respectively) but a partial agonist at D2S, D2L and D4.2 receptors (EC50=29, 23 and 4.5 nM, respectively). Sarizotan is an antagonist at D2S and D2L receptors (IC50=52 and 121 nM, respectively). Sarizotan is a full agonist at D2L, D3, D4.2 and D4.4 receptors (EC50=0.51, 0.47, 0.48 and 0.23 nM, respectively) but a partial agonist at D2S receptors (EC50=0.6 nM).
Hodoodo Cat#: H319572
Name: Sarizotan HCl
CAS#: 195068-07-6 (HCl)
Chemical Formula: C22H22ClFN2O
Exact Mass: 0.00
Molecular Weight: 384.880
Elemental Analysis: C, 68.66; H, 5.76; Cl, 9.21; F, 4.94; N, 7.28; O, 4.16
Related CAS #: 195068-07-6 (HCl) 351862-32-3 (free base)
Synonym: EMD-128130; EMD128130; EMD 128130; EMD-77697; EMD-77697; EMD-77697; Sarizotan hydrochloride; Sarizotan HCl
IUPAC/Chemical Name: (R)-1-(chroman-2-yl)-N-((5-(4-fluorophenyl)pyridin-3-yl)methyl)methanamine hydrochloride
InChi Key: QDLVYMYXOLGZOD-ZMBIFBSDSA-N
InChi Code: InChI=1S/C22H21FN2O.ClH/c23-20-8-5-17(6-9-20)19-11-16(12-24-14-19)13-25-15-21-10-7-18-3-1-2-4-22(18)26-21;/h1-6,8-9,11-12,14,21,25H,7,10,13,15H2;1H/t21-;/m1./s1
SMILES Code: FC1=CC=C(C2=CN=CC(CNC[C@H]3CCC4=C(O3)C=CC=C4)=C2)C=C1.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Related CAS# 195068-07-6 ( Sarizotan HCl salt);
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The following data is based on the product molecular weight 384.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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| In vivo protocol: |
1: Kuzhikandathil EV, Bartoszyk GD. The novel antidyskinetic drug sarizotan
elicits different functional responses at human D2-like dopamine receptors.
Neuropharmacology. 2006 Sep;51(4):873-84. Epub 2006 Jul 14. PubMed PMID:
16844149.
2: Lorenc-Koci E, Wardas J, Bartoszyk GD, Wolfarth S. Contribution of the
serotonin 5-HT1A receptor agonism of 8-OH-DPAT and EMD 128130 to the regulation
of haloperidol-induced muscle rigidity in rats. Neuropharmacology. 2003
Dec;45(8):1057-69. PubMed PMID: 14614949.
