NEU 365D Lecture Notes - Lecture 15: Cyclic Adenosine Monophosphate, Aripiprazole, Microsecond
Document Summary
Ionotropic nt binding site is on ion channel low microsecond time scale. Responses slow onset & longer duration compared to ionotropic receptors. 1/3 all fda approved drugs act on gpcr-activation. Ex: abilify second generation antipsychotic (in top 10 drugs in us) ~1/2 used in olfaction ability to distinguish different odors, pattern of binding to which particular receptors. Sutherland & rall (1950s) experiment: epinephrine/adrenaline application to cardiac cells didn"t get inside the cell, but there were internal increases in camp (cyclic adenosine monophosphate) molecules. Cardiac cells have specific receptors for epinephrine/adrenaline (first messenger: hormone, nts, etc. Don"t cross the cell to go inside) Transmission of binding info to inside of cell. Effectors downstream of gpcr = 2 nd messengers. Multiple receptors for single nts that bind gpcrs. Ex: 5 classes of muscarinic ach receptors & 6 classes of adrenergic receptors. Consequences of activation of the different receptors differ. Some activate, others inhibit downstream effector proteins.
