5-HT receptor



In the field of anxiolytic treatments. [1]

 

Classification

With the exception of the second messenger cascade.

Families

Family Type Mechanism
cAMP
5-HT2 Gq/G11 coupled increasing cellular levels of inositol trisphosphate (IP3) and diacylglycerol (DAG)
K+ cation channel depolarizing plasma membrane
5-HT4 Gs coupled increasing cellular levels of cAMP
5-HT5A adenylate cyclase activity.[2]
5-HT7 Gs coupled increasing cellular levels of cAMP

Specific proteins/genes

Within these general classes of 5-HT receptors, a number of specific types have been characterized:

Summary of characterized 5-HT receptors, with selected high affinity agonist and antagonist ligands
Receptor Gene Actions Agonists Antagonists
5-HT1A HTR1A
  • CNS: neuronal inhibition, behavioural effects (sleep, feeding, thermoregulation, aggression, anxiety)
5-HT1B HTR1B
  • CNS: presynaptic inhibition, behavioural effects
  • vascular: pulmonary vasoconstriction
5-HT1D HTR1D
  • CNS: locomotion, anxiety;
  • vascular: cerebral vasoconstriction
  • 5-(Nonyloxy)tryptamine,[3]
  • sumatriptan
  • methiothepin
  • yohimbine
  • metergoline
  • ergotamine
5-HT1E HTR1E
5-HT1F HTR1F
5-HT2A HTR2A
  • CNS: neuronal excitation, behavioural effects, learning, anxiety
  • smooth muscle: contraction, vasoconstriction / vasodilatation
  • platelets: aggregation
5-HT2B HTR2B
  • stomach: contraction
5-HT2C HTR2C
  • CNS: anxiety, choroid plexus: cerebrospinal fluid (CSF) secretion
5-HT3 HTR3A, HTR3B
  • CNS, PNS: neuronal excitation, anxiety, emesis
  • 2-methyl-5-HT
5-HT4 HTR4
  • GIT, CNS: neuronal excitation, gastrointestinal motility, behavioural effects
  • GR113808
5-HT5A HTR5A
  • CNS (cortex, hippocampus, cerebellum): unknown
unknown
5-HT6 HTR6
  • CNS: unknown
  • LSD
SB271046 [5]
5-HT7 HTR7
  • CNS, GIT, blood vessels: unknown
  • 5-carboxytryptamine
  • LSD
  • methiothepin
  • risperidone

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor.

Therapeutic modulation

Various drugs are used to modulate the 5-HT system including some antiemetics, antipsychotics and anti-migraine agents.

References

  1. ^ Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacol. Rev. 46 (2): 157–203. PMID 7938165.
  2. ^ a b Nelson DL (2004). "5-HT5 receptors". Current drug targets. CNS and neurological disorders 3 (1): 53–8. PMID 14965244.
  3. ^ Glennon RA, Hong SS, Dukat M, Teitler M, Davis K (1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist". J. Med. Chem. 37 (18): 2828–30. doi:10.1021/jm00044a001. PMID 8071931.
  4. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 187
  5. ^ Target Schizophrenia - Possible future developments. Retrieved on 2007-07-06.
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "5-HT_receptor". A list of authors is available in Wikipedia.