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alpha-2 adrenergic receptor
Function:
- alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins
- rank order of potency for agonists: oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine
- rank order of potency for antagonists: yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
- presynaptic autoreceptor
- norepinephrine inhibits further release of norepinephrine
- presynaptic heteroreceptor on serotoninergic neurons
- norepinephrine interaction stimulates further release of serotonin
Interactions
molecular events
Related
alpha-2 adrenergic receptor agonist
alpha-2 adrenergic receptor gene
Specific
alpha-2A adrenergic receptor; alpha-2A adrenoreceptor; alpha-2A adrenoceptor; alpha-2AAR; alpha-2 adrenergic receptor subtype C10 (ADRA2A, ADRA2R, ADRAR)
alpha-2B adrenergic receptor; alpha-2B adrenoreceptor; alpha-2B adrenoceptor; alpha-2 adrenergic receptor subtype C2 (ADRA2B ADRA2L1 ADRA2RL1)
alpha-2C adrenergic receptor; alpha-2C adrenoreceptor; alpha-2C adrenoceptor; alpha-2 adrenergic receptor subtype C4 (ADRA2C, ADRA2L2, ADRA2RL2)
alpha-2D adrenergic receptor
General
alpha adrenergic receptor
phosphoprotein
Properties
COMPARTMENT: synaptic membrane
CELL: neuron
MOTIF: exoplasmic domain {N-TERMINAL}
ligand-binding site
SITE: WITHIN-MEMBRANE-DOMAINS
FOR-BINDING-OF: norepinephrine
epinephrine
transmembrane domain {TM1}
transmembrane domain {TM2}
transmembrane domain {TM3}
transmembrane domain {TM4}
transmembrane domain {TM5}
transmembrane domain {TM6}
transmembrane domain {TM7}
binding site
SITE: C-TERMINAL-CYS
EFFECTOR-BOUND: palmitate
BOUND-VIA: carboxylate
S/T phosphorylation site
glutamate-rich region
MOTIF: glutamate residue (12)
cytoplasmic domain {C-TERMINAL}
References
- VanDongen AM, Codina J, Olate J, Mattera R, Joho R,
Birnbaumer L, Brown AM.
Newly identified brain potassium channels gated by the guanine
nucleotide binding protein Go.
Science. 1988 Dec 9;242(4884):1433-7.
PMID: 3144040
- Sagi-Eisenberg R
GTP-binding proteins as possible targets for protein kinase C
action
TIBS 14:355 1989
PMID: 2512697
- Ross CA, McInnis MG, Margolis RL, Li SH.
Genes with triplet repeats: candidate mediators of
neuropsychiatric disorders.
Trends Neurosci. 1993 Jul;16(7):254-60. Review.
PMID: 7689767