TY - JOUR
T1 - 5-hydroxytryptamine
T2 - Considerations about discovery, receptor classification and relevance to medical research
AU - Villalon, C. M.
AU - Terron, J. A.
AU - Ramirez-San Juan, E.
AU - Saxena, P. R.
PY - 1995
Y1 - 1995
N2 - Serotonin (5-hydroxytryptamine; 5-HT), an endogenous and ubiquitous monoamine, has become a subject of 'explosive' research. Though its vasoconstrictor properties were first noticed in defibrinated or clotted blood, 5-HT was discovered 75 years later going through several denominations such as 'enteramine, serotonin or 5-HT'. Once confirmed that serotonin, enteramine and 5-HT were the same substance, the compound was synthesized and efforts with a view to analyze 5-HT receptors were performed. On the basis of the actions of 5-HT and other drugs on several smooth muscle experimental preparations, it was originally suggested that 5-HT could act via different receptors. Thus, Gaddum and Picarelli proposed the 'D' and 'M' classification based on the differential sensitivity of guinea pig ileum 5-HT-induced contraction to some drugs. Later on, this classification was confronted with the new Peroutka's 5-HT1 and 5-HT2 classification derived from radioligand binding studies. Since these 5-HT receptors were being referred to by many names, an international committee formulated some criteria for the characterization and a framework for-the nomenclature of 5-HT receptors into 5-HT1, 5-HT2 and 5-HT3 categories. More recently, functional evidence unrelated to activation of the above 5-HT receptor types was given and a new 5-HT (5-HT4) receptor was proposed to exist. From this stage, molecular biologists have been cloning several 5-HT receptors which are different from the various receptors (sub)types characterized thus far. This review is focused on the discovery of 5-HT and the evolution of the classification of 5-HT receptors, from historical remarks to the modern concepts about receptor characterization; furthermore, the relevance of this development to medical research is considered.
AB - Serotonin (5-hydroxytryptamine; 5-HT), an endogenous and ubiquitous monoamine, has become a subject of 'explosive' research. Though its vasoconstrictor properties were first noticed in defibrinated or clotted blood, 5-HT was discovered 75 years later going through several denominations such as 'enteramine, serotonin or 5-HT'. Once confirmed that serotonin, enteramine and 5-HT were the same substance, the compound was synthesized and efforts with a view to analyze 5-HT receptors were performed. On the basis of the actions of 5-HT and other drugs on several smooth muscle experimental preparations, it was originally suggested that 5-HT could act via different receptors. Thus, Gaddum and Picarelli proposed the 'D' and 'M' classification based on the differential sensitivity of guinea pig ileum 5-HT-induced contraction to some drugs. Later on, this classification was confronted with the new Peroutka's 5-HT1 and 5-HT2 classification derived from radioligand binding studies. Since these 5-HT receptors were being referred to by many names, an international committee formulated some criteria for the characterization and a framework for-the nomenclature of 5-HT receptors into 5-HT1, 5-HT2 and 5-HT3 categories. More recently, functional evidence unrelated to activation of the above 5-HT receptor types was given and a new 5-HT (5-HT4) receptor was proposed to exist. From this stage, molecular biologists have been cloning several 5-HT receptors which are different from the various receptors (sub)types characterized thus far. This review is focused on the discovery of 5-HT and the evolution of the classification of 5-HT receptors, from historical remarks to the modern concepts about receptor characterization; furthermore, the relevance of this development to medical research is considered.
KW - 5-HT receptors
KW - Classification
KW - Serotonin (5-hydroxytryptamine; 5-HT)
UR - http://www.scopus.com/inward/record.url?scp=0029618232&partnerID=8YFLogxK
M3 - Artículo de revisión
SN - 0188-0128
VL - 26
SP - 331
EP - 344
JO - Archives of Medical Research
JF - Archives of Medical Research
IS - 4
ER -