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5-HT1D
5-hydroxytryptamine (serotonin) 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 vasoconstriction in the brain. Tissue distribution 5HT1D receptors are found at low levels in the basal ganglia (globus pallidus, substantia nigra, caudate putamen), the hippocampus, and in the cortex. Structure 5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory response by decreasing cellular levels of cAMP. The 5HT1D is a 7-TM receptor. A large intercellular loop between TM-5 and TM-6 is believed to be associated with coupling to a second messenger. Agonists might bind in a manner that utilizes an aspartate residue in TM-3 and residues in the TM-4, TM-5 and TM-6. A human clone containing an intronless open reading frame was found to encode 377 amino acids of the 5HT1D receptor. The ...
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5-HT Receptor
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the Central nervous system, central and peripheral nervous systems. They mediate both Neurotransmitter#Excitatory and inhibitory, excitatory and inhibitory Synaptic transmission, neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural Ligand (biochemistry), ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamic acid, glutamate, gamma-Aminobutyric acid, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cogn ...
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L-760790
L-760,790 is an experimental drug from the substituted tryptamine family, which acts as a selective agonist for the 5-HT1D serotonin receptor 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both ex ..., with around 62x selectivity for 5-HT1D over the closely related 5-HT1B receptor. References 5-HT1B agonists 5-HT1D agonists Benzylamines Indoles Pyrrolidines Triazoles Secondary amines {{nervous-system-drug-stub ...
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Sumatriptan
Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, subcutaneous Injection under the skin, injection. Therapeutic effects generally occur within three hours. Its primary effect as a serotonin 5-HT1B, 5-HT1B/5-HT1D receptor, 5-HT1D receptor agonist can create common side effects such as chest pressure, fatigue, vomiting, tingling, and vertigo. Serious side effects may include serotonin syndrome, heart attack, stroke, and seizures. With excessive use, medication overuse headaches may occur. It is unclear if use during pregnancy or breastfeeding is safe. The mechanism of action is not entirely clear. It is in the triptan class of medications. Sumatriptan was patented in 1982 and approved for medical use in 1991. It is on the WHO Model List of Essential Medicines, World Health Organization's L ...
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Zolmitriptan
Zolmitriptan, sold under the brand name Zomig among others, is a serotonergic drug, serotonergic medication which is used in the acute treatment of migraine attacks with or without aura (symptom), aura and cluster headaches. It is taken oral administration, by mouth as a swallowing, swallowed or orally disintegrating tablet, disintegrating tablet (pharmacy), tablet or as a nasal spray. Side effects include tightness in the neck or throat, Orofacial pain, jaw pain, dizziness, paresthesia, asthenia, somnolence, warm/cold sensations, nausea, chest pressure, and dry mouth. The drug acts as a binding selectivity, selective serotonin 5-HT1B receptor, 5-HT1B and 5-HT1D receptor, 5-HT1D receptor agonist. Chemical structure, Structurally, it is a triptan and a substituted tryptamine, tryptamine chemical derivative, derivative. It was patented in 1990 and was approved for medical use in 1997. Medical uses Migraine Zolmitriptan is used for the acute treatment of migraines with or witho ...
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Sumatriptan
Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, subcutaneous Injection under the skin, injection. Therapeutic effects generally occur within three hours. Its primary effect as a serotonin 5-HT1B, 5-HT1B/5-HT1D receptor, 5-HT1D receptor agonist can create common side effects such as chest pressure, fatigue, vomiting, tingling, and vertigo. Serious side effects may include serotonin syndrome, heart attack, stroke, and seizures. With excessive use, medication overuse headaches may occur. It is unclear if use during pregnancy or breastfeeding is safe. The mechanism of action is not entirely clear. It is in the triptan class of medications. Sumatriptan was patented in 1982 and approved for medical use in 1991. It is on the WHO Model List of Essential Medicines, World Health Organization's L ...
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Yohimbine
Yohimbine, also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe'' (yohimbe); also from the bark of the unrelated South American tree '' Aspidosperma quebracho-blanco''. Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug used to reverse sedation in dogs and deer. While yohimbine behaves as an aphrodisiac in some mammals, it does not do so in humans. It has been prescribed as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs. Substances that have purported to be extracts from the yohimbe tree have been marketed as dietary supplements for various purposes, but they contain highly variable amounts of yohimbine, if any; no published scientific evidence supports their efficacy. Uses Sexual dysfunction and aphrodisiac Yohimbe extracts, ...
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Ziprasidone
Ziprasidone, sold under the brand name Geodon among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It may be used by mouth and by injection into a muscle (IM). The intramuscular form may be used for acute agitation in people with schizophrenia. Common side effects include tremors, tics, dizziness, dry mouth, restlessness, nausea, and mild sedation. Although it can also cause weight gain, the risk is much lower than for other atypical antipsychotics. How it works is not entirely clear but is believed to involve effects on serotonin and dopamine in the brain. Ziprasidone was approved for medical use in the United States in 2001. The pills are made up of the hydrochloride salt, ziprasidone hydrochloride. The intramuscular form is the mesylate, ziprasidone mesylate trihydrate, and is provided as a lyophilized powder. In 2020, it was the 282nd most commonly prescribed medication in the United States, with more than 1million prescript ...
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5-(Nonyloxy)tryptamine
5-(Nonyloxy)tryptamine (5-NOT) is a tryptamine derivative which acts as a selective agonist at the 5-HT1B receptor. Increasing the O-alkoxy chain length in this series gives generally increasing potency and selectivity for 5-HT1B, with highest activity found for the nonyloxy derivative, having a 5-HT1B binding affinity of 1.0 nM, and around 300-fold selectivity over the related 5-HT1A receptor. See also * 5-Allyloxy-AMT * 5-Benzyloxytryptamine * 5-Carboxamidotryptamine * 5-Ethoxy-DMT * 5-Methyltryptamine * Sumatriptan Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, su ... References Indole ethers at the benzene ring 5-Methoxytryptamines Serotonin receptor agonists {{nervous-system-drug-stub ...
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CP-135807
CP-135807 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. See also * 4-HO-MPMI * 5-MeO-MPMI * Eletriptan Eletriptan, sold under the brand name Relpax and used in the form of eletriptan hydrobromide, is a second-generation triptan medication intended for treatment of migraine headaches. It is used as an abortive medication, blocking a migraine at ... * LY-334370 References Disubstituted pyridines Alpha-Alkyltryptamines N,N-Dialkyltryptamines Nitroarenes Pyrrolidinylmethylindoles Serotonin receptor agonists {{nervous-system-drug-stub ...
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Metergoline
Metergoline (, ), also known as methergoline and sold under the brand names Contralac (veterinary) and Liserdol (clinical), is a monoaminergic medication of the ergoline group which is used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) and to suppress lactation. Pharmacology Pharmacodynamics Metergoline is a ligand of various serotonin and dopamine receptor Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through diff ...s. References External links * {{Ergolines Antipsychotics Carbamates Dopamine agonists Ergolines Prolactin inhibitors Serotonin receptor antagonists ...
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Ergotamine
Ergotamine, sold under the brand name Ergomar among others, is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is structurally similar to several neurotransmitters, and it acts as a vasoconstrictor. It is used for acute migraines, sometimes with caffeine as the combination ergotamine/caffeine. The drug is a non-selective modulator or agonist of serotonin receptors and other receptors. It is peripherally selective and crosses into the brain in minimal amounts. Medicinal use of ergot fungus began in the 16th century, for the induction of childbirth; but dosage uncertainty discouraged its use. It has been used to prevent post-partum hemorrhage (bleeding after childbirth). It was first isolated from the ergot fungus by Arthur Stoll, at Sandoz in 1918, and was marketed as Gynergen in 1921. Medical uses Ergotamine is indicated as therapy to abort or prevent vascular headache. Available ...
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Methiothepin
Metitepine (; developmental code names Ro 8-6837 (maleate), VUFB-6276 (mesylate)), also known as methiothepin, is a drug described as a " psychotropic agent" of the tricyclic or tetracyclic group which was never marketed. It acts as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors, including of the serotonin 5-HT1, 5-HT2, 5-HT5, 5-HT6, and 5-HT7 receptors. The drug has antipsychotic properties. Pharmacology Pharmacodynamics Chemistry Analogues Metitepine is closely structurally related to certain other tetracyclic compounds including amoxapine, batelapine, clorotepine, clotiapine, clozapine, flumezapine, fluperlapine, loxapine, metiapine, olanzapine, oxyprothepin, perathiepin, perlapine, quetiapine Quetiapine ( ), sold under the brand name Seroquel among others, is an atypical antipsychotic medication used in the treatment of schizophrenia, bipolar disorder, bipolar depression, and major depressive disorder. Despite being wide ...
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