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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-334370
LY-334370 is a selective 5-HT1F receptor agonist which was under development by Eli Lilly and Company for the treatment of migraine headaches. The drug showed efficacy in a phase II clinical trial but further development was halted due to toxicity detected in animals. See also * CP-135807 * Lasmiditan Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute (active but short-term) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not useful for prevention. It is ... * SN-22 References External links * 5-HT1F agonists Abandoned drugs Benzamides Drugs developed by Eli Lilly and Company 4-Fluorophenyl compounds Piperidinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and Signal_transduction, transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrophysiology, electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptor, GABA receptors. 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 (biochemistry), ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G prote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-HO-MPMI
4-HO-MPMI (also known as 4-Hydroxy-''N''-methyl-(α,''N''-trimethylene)-tryptamine or lucigenol) is a tryptamine derivative that is a psychedelic drug. It was developed by the team led by David Nichols from Purdue University in the late 1990s. This compound produces hallucinogen-appropriate responding in animal tests with a similar potency to the amphetamine- derived psychedelic DOI, and has two enantiomer In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities whi ...s, with only the (''R'')-enantiomer being active. The binding affinity for 5-HT2A receptor is 13 ± 2 nM (Ki 25IOI). It is reported at doses starting at 0.5 mg and 1.0-1.5 mg seem to be psychedelic doses. The duration it is reported between six and eight hours. Available (anecdotal) data on subjective effects report ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-MeO-MPMI
5-MeO-MPMI (also known as 5-Methoxy-''N''-methyl-(α,''N''-trimethylene)tryptamine) is a tryptamine derivative that is a psychedelic drug. It was first developed by the team led by JE Macor in 1992, and subsequently investigated by the team led by David Nichols from Purdue University in the late 1990s. This compound produces psychedelic-appropriate responding in animal tests with a similar potency to the amphetamine- derived psychedelic DOI, and has two enantiomer In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities whi ...s, with only the (''R'')-enantiomer being active. See also * 5-MeO-pyr-T * 5F-MPMI * 4-HO-MPMI * 4-HO-pyr-T * CP-135,807 * MPMI References {{Tryptamines Alpha-Alkyltryptamines Designer drugs N,N-Dialkyltryptamines 5-Methoxytryptamines Pyrrolidinylmethyli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 attack which is already in progress. Eletriptan is marketed and manufactured by Pfizer Inc. Approval and availability Eletriptan was approved by the US Food and Drug Administration (FDA) in December 2002, for the acute treatment of migraine with or without aura in adults. It is available only by prescription in the United States, Canada and Australia. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. It is available in 20 mg and 40 mg strengths. Eletriptan was covered by and ; both now expired. Mechanism of action Eletriptan is believed to reduce swelling of the blood vessels surrounding the brain. This swelling is associated with the head pain of a m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-Alkyltryptamines
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino group, amino (NH2) group via an ethyl (−CH2–CH2−) side chain, sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and dimethyltryptamine, DMT. In South America, dimethyltryptamine is obtained f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
