FSL0364

Structure

• InChI=1S/C17H17NO2/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/t13-/m1/s1
• InChIKey=VMWNQDUVQKEIOC-CYBMUJFWSA-N

Synonyms

• 41372-20-7
• Apomorphine hydrochloride hemihydrate

Origin

Chemically synthesized

Biological activities

Nonselective dopamne agonist

Therapeutic

Antiparkinsonian

Target

Dopamine receptor

Assay information

Non-ergoline dopamine agonist with high in vitro binding affinity for the dopamine D4 receptor (K_i = 4.4 nM), moderate affinity for the dopamine D2, D3, and D5 (K_i = 35-83, 26, and 15 nM, respectively), and adrenergic
Affinities (pK_i values) for recombinant human dopamine receptors (hD1, hD2S, hD2L, hD3, hD4, hD5) are 6.43, 7.46, 7.08, 7.59, 8.36, 7.83, respectively
Affinities (pK_i values) for recombinant human hα1-, hα2-, and hβ-adrenoceptors and native rat rα2D-ARs (hα1A, hα1B, hα1D, rα2D, hα2A, hα2B, hα2C, hβ1, hβ2
Affinities (pK_i values) for serotonin h5-HT1 and h5-HT2 receptor subtypes and native histamine H1 receptors (h5-HT1A, h5-HT1B, h5-HT1D, h5-HT2A, h5-HT2B, h5-HT2C, H1) are 6.93, 5.53, 5.91, 6.92, 6.88, 6.99,

References

• Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A
  Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
  J Pharmacol Exp Ther, 303(2): 791-804 (2002)  12388666  doi: 10.1124/jpet.102.039867
• Murrell W
  On the Action of Apomorphine and Apocodeine, with Reference to their Value as Expectorants in the Treatment of Chronic Bronchitis.
  Br Med J, 1(1574): 452-456 (1891)  20753261