Synonym
ORM-12741; ORM12741; ORM 12741
IUPAC/Chemical Name
2H-Benzofuro(2,3-a)quinolizine, 1,3,4,6,7,12b-hexahydro-1-(methoxymethyl)-1-methyl-, (1S,12bS)-
InChi Key
OCUKPFWNSAAHRP-QZTJIDSGSA-N
InChi Code
InChI=1S/C18H23NO2/c1-18(12-20-2)9-5-10-19-11-8-14-13-6-3-4-7-15(13)21-16(14)17(18)19/h3-4,6-7,17H,5,8-12H2,1-2H3/t17-,18-/m1/s1
SMILES Code
C[C@]1(COC)CCCN2CCC3=C(OC4=CC=CC=C43)[C@]12[H]
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
285.39
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 |
1: Shahid M, Rinne JO, Scheinin M, Virta J, Marjamäki P, Solin O, Arponen E, Sallinen J, Kuokkanen K, Rouru J. Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain. EJNMMI Res. 2020 Dec 9;10(1):152. doi: 10.1186/s13550-020-00741-y. PMID: 33296042; PMCID: PMC7726058.
2: Rinne JO, Wesnes K, Cummings JL, Hakulinen P, Hallikainen M, Hänninen J, Murphy M, Riordan H, Scheinin M, Soininen H, Rouru J. Tolerability of ORM-12741 and effects on episodic memory in patients with Alzheimer's disease. Alzheimers Dement (N Y). 2016 Dec 8;3(1):1-9. doi: 10.1016/j.trci.2016.11.004. PMID: 29067315; PMCID: PMC5651366.
3: Porsteinsson AP, Antonsdottir IM. An update on the advancements in the treatment of agitation in Alzheimer's disease. Expert Opin Pharmacother. 2017 Apr;18(6):611-620. doi: 10.1080/14656566.2017.1307340. Epub 2017 Mar 28. PMID: 28300462.
4: Herrick AL, Murray AK, Ruck A, Rouru J, Moore TL, Whiteside J, Hakulinen P, Wigley F, Snapir A. A double-blind, randomized, placebo-controlled crossover trial of the α2C-adrenoceptor antagonist ORM-12741 for prevention of cold- induced vasospasm in patients with systemic sclerosis. Rheumatology (Oxford). 2014 May;53(5):948-52. doi: 10.1093/rheumatology/ket421. Epub 2014 Jan 31. PMID: 24489014.
5: Nissinen J, Andrade P, Natunen T, Hiltunen M, Malm T, Kanninen K, Soares JI, Shatillo O, Sallinen J, Ndode-Ekane XE, Pitkänen A. Disease-modifying effect of atipamezole in a model of post-traumatic epilepsy. Epilepsy Res. 2017 Oct;136:18-34. doi: 10.1016/j.eplepsyres.2017.07.005. Epub 2017 Jul 12. PMID: 28753497.
6: Uys MM, Shahid M, Harvey BH. Therapeutic Potential of Selectively Targeting the α2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective. Front Psychiatry. 2017 Aug 14;8:144. doi: 10.3389/fpsyt.2017.00144. PMID: 28855875; PMCID: PMC5558054.
