5-HT1D receptor
Encyclopedia
5-hydroxytryptamine receptor 1D, also known as HTR1D, is a 5-HT receptor
, but also denotes the human gene
encoding it. 5-HT1D acts on the central nervous system
, and affects locomotion
and anxiety
. It also induces vascular vasoconstriction
in the brain.
5-HT receptor
The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission...
, but also denotes the human gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
encoding it. 5-HT1D acts on the central nervous system
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
, and affects locomotion
Animal locomotion
Animal locomotion, which is the act of self-propulsion by an animal, has many manifestations, including running, swimming, jumping and flying. Animals move for a variety of reasons, such as to find food, a mate, or a suitable microhabitat, and to escape predators...
and anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
. It also induces vascular vasoconstriction
Vasoconstriction
Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, small arterioles and veins. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in...
in the brain.
Agonists
- 5-(Nonyloxy)tryptamine5-(Nonyloxy)tryptamine5-tryptamine is a tryptamine derivative which acts as a selective agonist at the 5-HT1D serotonin receptor. Increasing the O-alkoxy chain length in this series gives generally increasing potency and selectivity for 5-HT1D, with highest activity found for the nonyloxy derivative, having a 5-HT1D...
, - sumatriptanSumatriptanSumatriptan is a triptan sulfa drug containing a sulfonamide group. It is used for the treatment of migraine headaches. Sumatriptan is produced and marketed by various drug manufacturers with many different trade names such as Sumatriptan, Imitrex, Imigran, Imigran recovery.-Approval and...
(vasoconstrictor in migraineMigraineMigraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
) - 5-Carboxamidotryptamine5-Carboxamidotryptamine5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has...
(5-CT) - 5-(t-Butyl)-N-methyltryptamine
- CP-135,807CP-135,807CP-135,807 is a drug which acts as a potent and selective agonist for the 5-HT1D serotonin receptor, and is used to study the function of this receptor subtype....
- CP-286,601
- PNU-109,291 ((S)-3,4-Dihydro-1-[2-[4-(4-methoxyphenyl)-1-piperazinyl]ethyl]-N-methyl-1H-2-benzopyran-6-carboxamide)
- PNU-142,633 ((1S)-1-[2-[4-[4-(Aminocarbonyl)phenyl]-1-piperazinyl]ethyl]-3,4-dihydro-N-methyl-1H-2-benzopyran-6-carboxamide)
- GR-46611 (3-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide)
- L-694,247 (2-[5-[3-(4-Methylsulfonylamino)benzyl-1,2,4-oxadiazol-5-yl]-1H-indol-3-yl]ethanamine)
- L-772,405
Antagonists
- ZiprasidoneZiprasidoneZiprasidone was the fifth atypical antipsychotic to gain FDA approval . In the United States, Ziprasidone is Food and Drug Administration approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients...
(atypical antipsychoticAtypical antipsychoticThe atypical antipsychotics are a group of antipsychotic tranquilizing drugs used to treat psychiatric conditions. Some atypical antipsychotics are FDA approved for use in the treatment of schizophrenia...
) http://books.google.com/books?id=HkA0Q31YDhAC&pg=PA438&lpg=PA438&dq=antipsychotics+5ht1d&source=web&ots=dSBm26DKPf&sig=3GtDECBspZW7_O1y6zJHd04BFo8#PPA438,M1 - methiothepin (antipsychoticAntipsychoticAn antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...
) - yohimbineYohimbineYohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids...
(aphrodisiacAphrodisiacAn aphrodisiac is a substance that increases sexual desire. The name comes from Aphrodite, the Greek goddess of sexuality and love. Throughout history, many foods, drinks, and behaviors have had a reputation for making sex more attainable and/or pleasurable...
) - metergolineMetergolineMetergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors....
- ergotamine (vasoconstrictor in migraineMigraineMigraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
) - BRL-15572BRL-15572BRL-15,572 is a drug which acts as a selective antagonist for the serotonin receptor subtype 5-HT1D, with around 60x selectivity over other related receptors...
- GR-127,935 (mixed 5-HT1B/1D antagonist)
- LY-310,762LY-310,762LY-310,762 is a drug which acts as a potent and selective antagonist for the 5-HT1D serotonin receptor, with reasonable selectivity over the closely related 5-HT1B subtype....
- LY-367,642
- LY-456,219
- LY-456,220