Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCPG9S)

• DTT Name: 5-HT 1E receptor (HTR1E)
• Synonyms: Serotonin receptor 1E; S31; 5-hydroxytryptamine receptor 1E; 5-HT1E; 5-HT-1E; 5-HT 1E
• Gene Name: HTR1E
• DTT Type: Successful target; [1]
• Related Disease: Pituitary gland disorder [ICD-11: 5A60-5A61]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT1E_HUMAN
• TTD ID: T84117
• Sequence:
  MNITNCTTEASMAIRPKTITEKMLICMTLVVITTLTTLLNLAVIMAIGTTKKLHQPANYL
  ICSLAVTDLLVAVLVMPLSIIYIVMDRWKLGYFLCEVWLSVDMTCCTCSILHLCVIALDR
  YWAITNAIEYARKRTAKRAALMILTVWTISIFISMPPLFWRSHRRLSPPPSQCTIQHDHV
  IYTIYSTLGAFYIPLTLILILYYRIYHAAKSLYQKRGSSRHLSNRSTDSQNSFASCKLTQ
  TFCVSDFSTSDPTTEFEKFHASIRIPPFDNDLDHPGERQQISSTRERKAARILGLILGAF
  ILSWLPFFIKELIVGLSIYTVSSEVADFLTWLGYVNSLINPLLYTSFNEDFKLAFKKLIR
  CREHT
• Function: Functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[1]

15 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[1]
2-(5-fluoro-1H-indol-3-yl)ethanamine	DMHW5FT	Discovery agent	N.A.	Investigative	[1]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[2]
5-BODMT	DM7BWG5	Discovery agent	N.A.	Investigative	[3]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[1]
9-OH-risperidone	DMGORXQ	Discovery agent	N.A.	Investigative	[4]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[1]
B173	DMN2XTQ	Discovery agent	N.A.	Investigative	[5]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[6]
BRL54443	DM3TWBU	Discovery agent	N.A.	Investigative	[7]
EDMT	DMS3AXK	Discovery agent	N.A.	Investigative	[8]
lysergol	DM1OHF8	Discovery agent	N.A.	Investigative	[9]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[1]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[1]
[3H]5-HT	DMYJXV7	Discovery agent	N.A.	Investigative	[10]

References

• [1] Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. Eur J Pharmacol. 2004 Jan 26;484(2-3):127-39.
• [2] Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A. 1993 Jan 15;90(2):408-12.
• [3] Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-7.
• [4] Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
• [5] The gamma-aminobutyric acid-B receptor agonist baclofen attenuates responding for ethanol in ethanol-dependent rats. Alcohol Clin Exp Res. 2007 Jan;31(1):11-8.
• [6] SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
• [7] Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
• [8] 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
• [9] Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
• [10] Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5517-21.