trace-amine receptor activity
Definition
Target type: molecularfunction
Combining with a trace amine to initiate a change in cell activity. Trace amines are biogenic amines that are synthesized from aromatic amino acids and are substrates for monoamine oxidase, and are therefore detectable only at trace levels in mammals. [GOC:mah, PMID:19325074]
Trace-amine receptors (TARs) are a group of G protein-coupled receptors that are activated by trace amines, which are neurotransmitters present in the brain at low concentrations. These receptors play a role in various physiological processes, including mood regulation, sleep, appetite, and neuroprotection. The molecular function of trace-amine receptor activity involves the following steps:
1. **Ligand Binding:** Trace amines, such as tyramine, tryptamine, and β-phenylethylamine, bind to the extracellular domain of the TAR, initiating a conformational change in the receptor protein.
2. **G Protein Activation:** This conformational change triggers the activation of a G protein, which is a heterotrimeric complex consisting of alpha, beta, and gamma subunits. The activated G protein dissociates into its subunits, leading to the activation of downstream signaling pathways.
3. **Second Messenger Production:** The activated G protein can activate various effector enzymes, such as adenylyl cyclase or phospholipase C, which catalyze the production of second messengers like cyclic AMP (cAMP) or inositol triphosphate (IP3). These second messengers, in turn, regulate the activity of various intracellular proteins and pathways.
4. **Cellular Response:** The activation of downstream signaling pathways leads to a variety of cellular responses, including changes in gene expression, ion channel activity, and intracellular calcium levels. These responses are responsible for the physiological effects of trace-amine receptor activation.
In summary, trace-amine receptor activity involves a series of molecular events, starting with ligand binding, followed by G protein activation, second messenger production, and ultimately, cellular responses. These receptors are essential for regulating various physiological processes in the brain and other tissues.'
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Proteins (1)
| Protein | Definition | Taxonomy |
|---|---|---|
| Trace amine-associated receptor 1 | A trace amine-associated receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q96RJ0] | Homo sapiens (human) |
Compounds (28)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| norepinephrine, (+,-)-isomer | catecholamine | human xenobiotic metabolite | |
| phenethylamine | 2-phenylethylamine : A phenylethylamine having the phenyl substituent at the 2-position. phenethylamine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #7016 | alkaloid; aralkylamine; phenylethylamine | Escherichia coli metabolite; human metabolite; mouse metabolite |
| tryptamine | aminoalkylindole; aralkylamino compound; indole alkaloid; tryptamines | human metabolite; mouse metabolite; plant metabolite | |
| 3-methoxytyramine | 3-methoxytyramine : A monomethoxybenzene that is dopamine in which the hydroxy group at position 3 is replaced by a methoxy group. It is a metabolite of the neurotransmitter dopamine and considered a potential biomarker of pheochromocytomas and paragangliomas. 3-methoxytyramine: RN given refers to parent cpd | monomethoxybenzene; phenols; phenylethylamine; primary amino compound | biomarker; human blood serum metabolite; human urinary metabolite |
| o-methyltyramine | 4-methoxyphenylethylamine : A primary amino compound consisting of ethylamine having a 4-methoxyphenyl substituent at the 2-position. O-methyltyramine: RN given refers to parent cpd | primary amino compound | |
| phentermine | Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity. | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| tolazoline | tolazoline : A member of the class of imidazoles that is 4,5-dihydro-1H-imidazole substituted by a benzyl group. Tolazoline: A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. | imidazoles | alpha-adrenergic antagonist; antihypertensive agent; vasodilator agent |
| tyramine | monoamine molecular messenger; primary amino compound; tyramines | EC 3.1.1.8 (cholinesterase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter | |
| dextroamphetamine | (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic. | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| methamphetamine | methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed. | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| 3-tyramine | 3-tyramine: MH Tyramine refers to 4-tyramine; RN given refers to parent cpd m-tyramine : A primary amino compound that is 2-phenylethanamine substituted by a hydroxy group at position 3. | primary amino compound; tyramines | human urinary metabolite; neurotransmitter |
| n-methylphenethylamine | N-methylphenethylamine: substrate for type A & B monoamine oxidase; RN given refers to parent cpd | ||
| tranylcypromine | (1R,2S)-tranylcypromine : A 2-phenylcyclopropan-1-amine that is the (1R,2S)-enantiomer of tranylcypromine. tranylcypromine : A racemate comprising equal amounts of (1R,2S)- and (1S,2R)-2-phenylcyclopropan-1-amine. An irreversible monoamine oxidase inhibitor that is used as an antidepressant (INN tranylcypromine). Tranylcypromine: A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders. (From AMA Drug Evaluations Annual, 1994, p311) | 2-phenylcyclopropan-1-amine | |
| 4-chlorophenylbiguanide | |||
| n,n-dimethylphenylethylamine | N,N-dimethylphenylethylamine: RN given refers to parent cpd | primary amine | |
| l-amphetamine | (R)-amphetamine : A 1-phenylpropan-2-amine that has R configuration. | 1-phenylpropan-2-amine | |
| 4-chlorophenethylamine | 4-chlorophenethylamine: RN given refers to parent cpd | ||
| 3,4-methylenedioxyphenethylamine | 3,4-methylenedioxyphenethylamine: RN given refers to parent cpd | ||
| 3-methoxy-4-hydroxyphenylethylamine | 3-methoxy-4-hydroxyphenylethylamine: a metabolite of dopamine and 5-hydroxytryptamine | ||
| 2-(2,5-dimethoxyphenyl)ethanamine | dimethoxybenzene | ||
| 2-chloro-2-phenethylamine | 2-chloro-2-phenethylamine: RN given refers to parent cpd | ||
| 2-(4-bromo-2,5-dimethoxyphenyl)ethylamine | 2-(4-bromo-2,5-dimethoxyphenyl)ethylamine: behaves as a partial agonist toward both alpha1-adrenergic & 5-HT(2) serotonergic receptors 2,5-dimethoxy-4-bromophenethylamine : A 2-arylethylamine compound where the aryl moiety is 4-bromo-2,5-dimethoxyphenyl. | 2-arylethylamine | |
| st 1913 | St 1913: methylene bridged clonidine analog; RN given refers to parent cpd | ||
| proguanil | proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells. Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent. | biguanides; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| 3-iodothyronamine | 3-iodothyronamine: a thyroid hormone derivative that may be involved in a fast response signaling pathway; structure in first source | aromatic ether | |
| 2,5-dimethoxy-4-bromoamphetamine, (r)-isomer | |||
| 2,5-dimethoxy-4-bromoamphetamine, (s)-isomer | |||
| ro5166017 | RO5166017: structure in first source |