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AH-494
AH-494 is a potent and selective, water-soluble full agonist at the 5HT7 serotonin receptor. It is a close derivative of the known chemical probe 5-Carboxamidotryptamine, as well as of the more lipophilic indole-imidazoles: AGH-107 and AGH-192. It has been shown to exhibit favorable ADMET profile in in vitro assays. See also * AGH-107 * AGH-192 * Frovatriptan Frovatriptan, sold under the brand name Frova, is a triptan drug developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual migraine. The product is licensed to Endo Pharmaceuticals in North America ... References {{reflist Serotonin receptor agonists Indoles Iodoarenes Imidazoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Carboxamidotryptamine
5-Carboxamidotryptamine (5-CT) 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 negligible affinity for the 5-HT1E and 5-HT1F receptors. 5-CT binds most strongly to the 5-HT1A receptor and it was once thought to be selective for this site. Recently, a close derivative of 5-CT, AH-494 has been shown to function as an agonist of 5-HT7, although being more selective over 5-HT1A. Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family. See also * 2-Methyl-5-hydroxytryptamine * 5-Benzyloxytryptamine * 5-Methoxytryptamine * α-Methyl-5-hydroxytryptamine * Frovatriptan * AH-494 * Acetryptine Acetryptine (INN) (developmental code name W-2965-A), also known as 5-acetyltryp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT7 Receptor
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the ''HTR7'' gene, which in humans is transcribed into 3 different splice variants. Function When the 5-HT7 receptor is activated by serotonin, it sets off a cascade of events starting with release of the stimulatory G protein Gs from the GPCR complex. Gs in turn activates adenylate cyclase which increases intracellular levels of the second messenger cAMP. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AGH-107
AGH-107 is a potent, selective, water-soluble and brain penetrant full agonist at the 5HT7 serotonin receptor. AGH-107 is one of the few examples of low-basicity aminergic receptor agonists, which may underlie its high selectivity over the related central nervous system targets. AGH-107 was found to reverse the impairment in novel object recognition caused by MK-801 in mice. The relatively short half-life in rodents inhibited its use as a molecular probe. See also * AH-494 * AGH-192 AGH-192 is a potent and selective, water soluble, orally bioavailable and brain penetrant full agonist at the 5HT7 serotonin receptor, derived from the older drug AGH-107. In animal tests it showed activity indicative of potential application ... References {{reflist Serotonin receptor agonists Indoles Iodoarenes Imidazoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AGH-192
AGH-192 is a potent and selective, water soluble, orally bioavailable and brain penetrant full agonist at the 5HT7 serotonin receptor, derived from the older drug AGH-107. In animal tests it showed activity indicative of potential application in the treatment of neuropathic pain. See also * AGH-107 AGH-107 is a potent, selective, water-soluble and brain penetrant full agonist at the 5HT7 serotonin receptor. AGH-107 is one of the few examples of low-basicity aminergic receptor agonists, which may underlie its high selectivity over the relat ... * AH-494 References {{reflist Serotonin receptor agonists Indoles Iodoarenes Imidazoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Frovatriptan
Frovatriptan, sold under the brand name Frova, is a triptan drug developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual migraine. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe. Medical uses Frovatriptan is used in the treatment of migraine. Available forms It is available as 2.5 mg tablets. Contraindications Frovatriptan should not be given to patients with: * Ischemic heart disease * Cerebrovascular syndrome * Peripheral vascular disease * Uncontrolled hypertension * Hemiplegic or basilar migraine Side effects Rare, but serious cardiac events have been reported in patients with risk factors predictive of CAD. These include: coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation. Pharmacology Pharmacodynamics Frovatriptan is a serotonin receptor agonist, with high affinity for the 5-HT1B/1D receptor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonists
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indoles
Indole is an aromatic heterocyclic organic compound with the formula C8 H7 N. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indole is widely distributed in the natural environment and can be produced by a variety of bacteria. As an intercellular signal molecule, indole regulates various aspects of bacterial physiology, including spore formation, plasmid stability, resistance to drugs, biofilm formation, and virulence. The amino acid tryptophan is an indole derivative and the precursor of the neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. The corresponding substituent is called indolyl. Indole undergoes electrophilic substitution, mainly at position 3 (see diagram i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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