Apomorphine, is an aporphine derivative of the dibenzoquinoline class. Apomorphine is very lipophilic and moderately soluble in water and normal saline. Oxidation upon exposure to air and light is rapid, but can be prevented by the use of strong acids (e.g., hydrochloric acid or zinc chloride) and antioxidants. Apomorphine activates D1-like (D1, D5) and D2-like (D2, D3, D4) receptors (and is thus classified as a non-selective dopamine agonist), serotonin receptors (5HT1A, 5HT2A, 5HT2B, and 5HT2C), and α-adrenergic receptors (α1B, α1D, α2A, α2B, and α2C) . Apomorphine’s dopaminergic activity is due to its polycyclic and tertiary amine structures.
Apomorphine has been used in a variety of treatments ranging from the treatment of addiction (i.e., to heroin, alcohol or cigarettes), for treatment of erectile dysfunction to the treatment of patients with Parkinson's disease. Currently, Apomorphine is used in patients with advanced Parkinson's disease, for the treatment of persistent and disabling motor fluctuations which do not respond to levodopa or other dopamine agonists, either on its own or in combination with deep brain stimulation. Recently, a new and potentially important therapeutic role for Apomorphine in the treatment of Alzheimer’s disease has been suggested; Apomorphine seems to stimulate A β catabolism in animal models and cell culture, thus reducing the rate of A β oligomerisation and consequent neural cell death.
Additional Information
|
Synonyms | Hemihydrate |
|---|
|
Product # | A-2549 |
|---|
|
CAS # | 314-19-2 |
|---|
|
Chemical Name | (6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol |
|---|
|
Formula | C17 H17 N O2 |
|---|
|
MW | 312.8 |
|---|
|
Appearance | Solid |
|---|
|
Purity | >98% (TLC); NMR (Conforms) |
|---|
|
Solubility | May be dissolved in water (20mg/ml) |
|---|
|
Storage Temp | Store desiccated as supplied at room temperature for up to 2 years. Store solutions at - 20º C for upto 1 week. |
|---|
|
Therapeutic Area | Neurological Disorders |
|---|
|
Use | Dopamine agonist use in Parkinson's Disease |
|---|
Additional Information
| MDL Number | MFCD00069236 |
|---|
| ChemACX | X1008102-2 |
|---|
| InChI | InChI=1S/C17H17NO2.ClH/c1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12;/h2-6,13,19-20H,7-9H2,1H3;1H/t13-;/m1./s1 |
|---|
| SMILES | CN1CCc2cccc-3c2[C@H]1Cc4c3c(c(cc4)O)O.Cl |
|---|
