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執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: S38093 is an inverse agonist at histamine H3 receptors. S 38093 displays a moderate affinity for rat, mouse and human H3 receptors (Ki=8.8, 1.44 and 1.2µM, respectively) with no affinity for other histaminergic receptors. In cellular models, the compound was able to antagonize mice H3 receptors (KB=0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11µM).
Name: S38093 free base
CAS#: 862896-30-8 (free base)
Chemical Formula: C17H24N2O2
Exact Mass: 288.1838
Molecular Weight: 288.391
Elemental Analysis: C, 70.80; H, 8.39; N, 9.71; O, 11.10
Related CAS #: 862896-30-8 (free base) 1222097-72-4 (HCl)
Synonym: S38093 free base; S-38093; S 38093;
IUPAC/Chemical Name: 4-(3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide
InChi Key: MRNMYWNBLVJWKG-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H24N2O2/c18-17(20)13-5-7-16(8-6-13)21-10-2-9-19-11-14-3-1-4-15(14)12-19/h5-8,14-15H,1-4,9-12H2,(H2,18,20)
SMILES Code: C1=C(OCCCN2CC3CCCC3C2)C=CC(C(=O)N)=C1
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
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).
Harmonized System Code: 293490
REFERENCES
1: Chaumette T, Chapuy E, Berrocoso E, Llorca-Torralba M, Bravo L, Mico JA, Chalus M, Eschalier A, Ardid D, Marchand F, Sors A. Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur J Pain. 2018 Jan;22(1):127-141. doi: 10.1002/ejp.1097. Epub 2017 Sep 6. PubMed PMID: 28877402.
2: Sors A, Panayi F, Bert L, Favale D, Nosjean O, Audinot V, Arrang JM, Buisson B, Steidl E, Delbos JM, Huhtala T, Kontkanen O, Chollet AM, Casara P, Lestage P. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23. doi: 10.1016/j.ejphar.2017.03.013. Epub 2017 Mar 21. PubMed PMID: 28336400.
3: Panayi F, Sors A, Bert L, Martin B, Rollin-Jego G, Billiras R, Carrié I, Albinet K, Danober L, Rogez N, Thomas JY, Pira L, Bertaina-Anglade V, Lestage P. In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist. Eur J Pharmacol. 2017 May 15;803:1-10. doi: 10.1016/j.ejphar.2017.03.008. Epub 2017 Mar 14. PubMed PMID: 28315340.
4: Guilloux JP, Samuels BA, Mendez-David I, Hu A, Levinstein M, Faye C, Mekiri M, Mocaer E, Gardier AM, Hen R, Sors A, David DJ. S 38093, a histamine H(3) antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. doi: 10.1038/srep42946. PubMed PMID: 28218311; PubMed Central PMCID: PMC5317168.
5: Sors A, Krazem A, Kehr J, Yoshitake T, Dominguez G, Henkous N, Letondor C, Mocaer E, Béracochéa DJ. The Synergistic Enhancing-Memory Effect of Donepezil and S 38093 (a Histamine H(3) Antagonist) Is Mediated by Increased Neural Activity in the Septo-hippocampal Circuitry in Middle-Aged Mice. Front Pharmacol. 2016 Dec 22;7:492. doi: 10.3389/fphar.2016.00492. eCollection 2016. PubMed PMID: 28066242; PubMed Central PMCID: PMC5177663.
