The alpha 1a and alpha 1b-adrenergic receptor subtypes: molecular mechanisms of receptor activation and of drug action.
In this chapter we summarize some aspects of the structure-functional relationship of the alpha 1a and alpha 1b-adrenergic receptor subtypes related to the receptor activation process as well as the effect of different alpha-blockers on the constitutive activity of the receptor. Molecular modeling of the alpha 1a and alpha 1b-adrenergic receptor subtypes and computational simulation of receptor dynamics were useful to interpret the experimental findings derived from site directed mutagenesis studies.
Cotecchia
S
S
Institut de Pharmacologie et Toxicologie, Université de Lausanne, Faculté de Médecine, Switzerland. susanna.cotecchia@ipharm.unil.ch
Rossier
O
O
Fanelli
F
F
Leonardi
A
A
De Benedetti
P G
PG
D000818:Animals; D006801:Humans; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism
C547713:ADRA1A protein, human; C547716:ADRA1B protein, human; D018340:Receptors, Adrenergic, alpha-1