Harmane-d
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 183.23 |
| Molecular Formula | C12H9DN2 |
| SMILES | CC1=NC([2H])=CC2=C1NC3=C2C=CC=C3 |
Summary
Harmane-d1 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor ( IC 50 =30 nM) over α2-adrenoceptor ( IC 50 =18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) ( IC 50 s=0.5 and 5 μM for human MAO A/B , respectively) [1] [2] [3] [4] .
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL ( 272.88 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.4576 mL | 27.2881 mL | 54.5762 mL |
| 5 mM | 1.0915 mL | 5.4576 mL | 10.9152 mL |
| 10 mM | 0.5458 mL | 2.7288 mL | 5.4576 mL |
References
- [1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
- [2] Louis ED, et, al. Blood harmane concentrations and dietary protein consumption in essential tremor. Neurology. 2005 Aug 9;65(3):391-6.
- [3] Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9.
- [4] Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications
- [5] Umezawa K, et, al. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30.