PMID- 11723224
OWN - NLM
STAT- MEDLINE
DCOM- 20011221
LR  - 20220408
IS  - 0026-895X (Print)
IS  - 0026-895X (Linking)
VI  - 60
IP  - 6
DP  - 2001 Dec
TI  - Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and 
      metabolites of the catecholamine neurotransmitters are agonists of a rat trace 
      amine receptor.
PG  - 1181-8
AB  - The trace amine para-tyramine is structurally and functionally related to the 
      amphetamines and the biogenic amine neurotransmitters. It is currently thought 
      that the biological activities elicited by trace amines such as p-tyramine and 
      the psychostimulant amphetamines are manifestations of their ability to inhibit 
      the clearance of extracellular transmitter and/or stimulate the efflux of 
      transmitter from intracellular stores. Here we report the discovery and 
      pharmacological characterization of a rat G protein-coupled receptor that 
      stimulates the production of cAMP when exposed to the trace amines p-tyramine, 
      beta-phenethylamine, tryptamine, and octopamine. An extensive pharmacological 
      survey revealed that psychostimulant and hallucinogenic amphetamines, numerous 
      ergoline derivatives, adrenergic ligands, and 3-methylated metabolites of the 
      catecholamine neurotransmitters are also good agonists at the rat trace amine 
      receptor 1 (rTAR1). These results suggest that the trace amines and catecholamine 
      metabolites may serve as the endogenous ligands of a novel intercellular 
      signaling system found widely throughout the vertebrate brain and periphery. 
      Furthermore, the discovery that amphetamines, including 
      3,4-methylenedioxymethamphetamine (MDMA; "ecstasy"), are potent rTAR1 agonists 
      suggests that the effects of these widely used drugs may be mediated in part by 
      this receptor as well as their previously characterized targets, the 
      neurotransmitter transporter proteins.
FAU - Bunzow, J R
AU  - Bunzow JR
AD  - Department of Physiology & Pharmacology, Oregon Health & Science University, 
      Portland, Oregon 97201, USA.
FAU - Sonders, M S
AU  - Sonders MS
FAU - Arttamangkul, S
AU  - Arttamangkul S
FAU - Harrison, L M
AU  - Harrison LM
FAU - Zhang, G
AU  - Zhang G
FAU - Quigley, D I
AU  - Quigley DI
FAU - Darland, T
AU  - Darland T
FAU - Suchland, K L
AU  - Suchland KL
FAU - Pasumamula, S
AU  - Pasumamula S
FAU - Kennedy, J L
AU  - Kennedy JL
FAU - Olson, S B
AU  - Olson SB
FAU - Magenis, R E
AU  - Magenis RE
FAU - Amara, S G
AU  - Amara SG
FAU - Grandy, D K
AU  - Grandy DK
LA  - eng
GR  - DA07262-09/DA/NIDA NIH HHS/United States
GR  - DA10703/DA/NIDA NIH HHS/United States
GR  - DA12408/DA/NIDA NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Mol Pharmacol
JT  - Molecular pharmacology
JID - 0035623
RN  - 0 (Catecholamines)
RN  - 0 (Dopamine Agents)
RN  - 0 (Neurotransmitter Agents)
RN  - 0 (Receptors, Biogenic Amine)
RN  - 0 (Serotonin Agents)
RN  - 8NA5SWF92O (Lysergic Acid Diethylamide)
RN  - CK833KGX7E (Amphetamine)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
SB  - IM
CIN - Mol Pharmacol. 2001 Dec;60(6):1165-7. PMID: 11723221
MH  - Amino Acid Sequence
MH  - Amphetamine/*pharmacology
MH  - Animals
MH  - Catecholamines/metabolism/pharmacology
MH  - Chromosome Mapping
MH  - Chromosomes, Human, Pair 6
MH  - Cloning, Molecular
MH  - Dopamine Agents/pharmacology
MH  - Humans
MH  - Lysergic Acid Diethylamide/*pharmacology
MH  - Molecular Sequence Data
MH  - N-Methyl-3,4-methylenedioxyamphetamine/*pharmacology
MH  - Neurotransmitter Agents/pharmacology
MH  - Rats
MH  - Receptors, Biogenic Amine/*agonists/metabolism
MH  - Sequence Homology, Amino Acid
MH  - Serotonin Agents/pharmacology
MH  - Subcellular Fractions
MH  - Tumor Cells, Cultured
EDAT- 2001/11/28 10:00
MHDA- 2002/01/05 10:01
CRDT- 2001/11/28 10:00
PHST- 2001/11/28 10:00 [pubmed]
PHST- 2002/01/05 10:01 [medline]
PHST- 2001/11/28 10:00 [entrez]
AID - 10.1124/mol.60.6.1181 [doi]
PST - ppublish
SO  - Mol Pharmacol. 2001 Dec;60(6):1181-8. doi: 10.1124/mol.60.6.1181.