|Molar mass||235.324 g/mol|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
|(: / ?)|
Aporphine is one of a class of quinoline alkaloids. Many different relatives of this compound have been purified from plants. One commonly used aporphine derivative is apomorphine, although it does not occur naturally.
Aporphine is a 5-HT1a partial agonist with a ki of 80nM and a 5-HT7 antagonist with a ki of 88nM. Aporphine is a Dopamine D1 antagonist with a ki of 717nM and a dopamine D2 antagonist with a ki of 527nM. Aporphine and its related alkaloids bulbocapnine, boldine, glaucine and corytuberine are antipsychotic, exert naloxone-reversible antinociceptive activity and with the exception of corytuberine are anticonvulsant. Some derivatives of aporphine such as S(+)-N-propylnorapomorphine have potential as low side effect profile antipsychotics. S(+)-N-propylnorapomorphine is highly selective for meso-limbic dopaminergic tracts and function as efficacious partial agonists, with no elevation in prolactin.
- List of entheogens
- Stévigny, C.; Bailly, C.; Quetin-Leclercq, J. (2005). "Cytotoxic and antitumor potentialities of aporphinoid alkaloids". Current medicinal chemistry. Anti-cancer agents 5 (2): 173–182.
- Leopoldo M, Lacivita E, Berardi F, Perrone R, Hedlund PB (February 2011). "Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders". Pharmacology & Therapeutics 129 (2): 120–48.
- Hedberg MH, Linnanen T, Jansen JM; et al. (August 1996). "11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions". Journal of Medicinal Chemistry 39 (18): 3503–13.
- Linnanen T, Brisander M, Unelius L; et al. (April 2001). "Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists". Journal of Medicinal Chemistry 44 (9): 1337–40.
- Zetler G (1988). "Neuroleptic-like, anticonvulsant and antinociceptive effects of aporphine alkaloids: bulbocapnine, corytuberine, boldine and glaucine". Archives Internationales De Pharmacodynamie Et De Thérapie 296: 255–81.
- Baldessarini RJ, Campbell A, Ben-Jonathan N, Ellingboe J, Zong R, Neumeyer JL (August 1994). "Effects of aporphine isomers on rat prolactin". Neuroscience Letters 176 (2): 269–71.