Sarizotan HCl

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MedKoo CAT#: 319572

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).


Chemical Structure

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Sarizotan HCl
CAS# 195068-07-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 319572
Name: Sarizotan HCl
CAS#: 195068-07-6 (HCl)
Chemical Formula: C22H22ClFN2O
Exact Mass:
Molecular Weight: 384.88
Elemental Analysis: C, 68.66; H, 5.76; Cl, 9.21; F, 4.94; N, 7.28; O, 4.16

Size Price Shipping out time Quantity
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Pricing updated 2021-02-25. Prices are subject to change without notice.

Sarizotan hydrochloride is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

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

Handling Instructions:

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.



Additional Information

Related CAS#
195068-07-6 ( Sarizotan HCl salt);