RT Book, Section
A1 Nichols, Charles D.
A1 Amara, Susan G.
A1 Sibley,  David R.
A2 Brunton, Laurence L.
A2 Knollmann, Björn C.
SR Print(0)
ID 1193229008
T1 5-Hydroxytryptamine (Serotonin) and Dopamine
T2 Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 14th Edition
YR 2023
FD 2023
PB McGraw-Hill Education
PP New York, NY
SN 9781264258079
LK accessmedicine.mhmedical.com/content.aspx?aid=1193229008
RD 2024/04/19
AB 5-Hydroxytryptamine  (5HT,  serotonin)  and  dopamine  (DA)  are  neurotransmitters  in  the  central  nervous  system  (CNS)  that  also  have  prominent  peripheral  actions.  Although  high  concentrations  of  5HT  are  present  in  the  CNS,  about  95%  of  all  5HT  in  the  human  body  is  located  in  the  periphery,  with  high  levels  in  enterochromaffin  cells  throughout  the  gastrointestinal  (GI)  tract  and  in  storage  granules  in  platelets.  The  highest  concentrations  of  DA  are  found  in  the  brain,  but  DA  stores  are  also  present  peripherally  in  the  adrenal  medulla,  in  the  plexuses  of  the  GI  tract,  and  in  the  enteric  nervous  system.  Fourteen  mammalian  5HT  receptor  subtypes,  categorized  into  seven  subfamilies,  and  five  DA  receptor  subtypes,  categorized  into  two  subfamilies,  have  been  delineated  by  structural  and  pharmacological  analyses  and  are  encoded  by  separate  genes.  For  some  receptors,  alternative  RNA  splicing  or  editing  creates  additional  heterogeneity;  for  example,  over  30  isoforms  of  the  5HT2C  receptor  subtype  arise  from  RNA  editing.  The  identification  of  individual  receptor  subtypes  has  facilitated  development  of  subtype-selective  drugs  and  elucidation  of  actions  of  5HT  and  DA  at  a  molecular  level.  Increasingly,  therapeutic  goals  are  being  achieved  by  using  drugs  that  selectively  target  one  or  more  of  the  subtypes  of  5HT  or  DA  receptors  or  that  act  on  a  combination  of  both  5HT  and  DA  receptors.