Tenilapine

Tenilapine is an atypical antipsychotic which has never been marketed in the US.

Tenilapine
INN: tenilapine
Identifiers
IUPAC name
  • (2E)-[5-(4-Methyl-1-piperazinyl)-9H-bisthieno[3,4-b:3',4'-e]azepin-9-ylidene]acetonitrile
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC17H16N4S2
Molar mass340.46 g·mol−1
3D model (JSmol)
SMILES
  • CN1CCN(CC1)C2=NC3=CSC=C3/C(=C/C#N)/C4=CSC=C42
InChI
  • InChI=1S/C17H16N4S2/c1-20-4-6-21(7-5-20)17-15-10-22-8-13(15)12(2-3-18)14-9-23-11-16(14)19-17/h2,8-11H,4-7H2,1H3/b12-2+
  • Key:RVQVUMIXBGFJLZ-SWGQDTFXSA-N

Pharmacodynamics

Tenilapine has a relatively high affinity for the 5-HT2A receptor, and relatively low (micromolar) affinities for dopamine receptors.

Binding affinities
ReceptorKi (nM)
D21584[1]
D4721±300[1]
5-HT2A40[1]

The ratio of D2 to D4 bonding is similar to that of clozapine.[1] Like many other atypical antipsychotics, it is a potent 5-HT2C antagonist.[2]

References
  1. Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY (August 1995). "D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs". Psychopharmacology (Berl). 120 (3): 365–8. doi:10.1007/BF02311185. PMID 8524985.
  2. Di Giovanni G, Esposito E, Di Matteo V (2011). "The 5-HT2C Receptor Subtype Controls Central Dopaminergic Systems: Evidence from Electrophysiological and Neurochemical Studies". 5-HT2C Receptors in the Pathophysiology of CNS Disease. The Receptors. Vol. 22. Totowa, NJ: Humana Press. doi:10.1007/978-1-60761-941-3_11.
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