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Preclamol
3-PPP (''N''-''n''-propyl-3-(3-hydroxyphenyl)piperidine) is a mixed sigma σ1 and σ2 receptor agonist (with similar affinity for both subtypes, though slightly higher affinity for the latter) and D2 receptor partial agonist which is used in scientific research. It shows stereoselectivity in its pharmacodynamics. (+)-3-PPP is the enantiomer that acts as an agonist of the sigma receptors; it is also an agonist of both D2 presynaptic and postsynaptic receptors. Conversely, (−)-3-PPP, also known as preclamol (), acts as an agonist of presynaptic D2 receptors but as an antagonist of postsynaptic D2 receptors, and has antipsychotic effects. 3-PPP has also been reported to be a monoamine reuptake inhibitor and possibly to act at adrenergic receptors or some other non-sigma receptor. Synthesis The Grignard reagent was prepared for 3-Bromoanisole 398-37-0(1) and this was reacted with 3-Bromopyridine 26-55-1(2) to give 3-(3-methoxyphenyl)pyridine 373-67-5(3). Reaction with 1-bromo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Reuptake Inhibitor
A monoamine reuptake inhibitor (MRI) is a drug that acts as a reuptake inhibitor of one or more of the three major monoamine neurotransmitters serotonin, norepinephrine, and dopamine by blocking the action of one or more of the respective monoamine transporters (MATs), which include the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). This in turn results in an increase in the synaptic concentrations of one or more of these neurotransmitters and therefore an increase in monoaminergic neurotransmission. Uses The majority of currently approved antidepressants act predominantly or exclusively as MRIs, including the selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs), and almost all of the tricyclic antidepressants (TCAs). Many psychostimulants used either in the treatment of or as appetite suppressants in the treatment of obesity also behave as MRIs, although notably amphetamine (and m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D2 Antagonists
D, or d, is the fourth letter of the Latin alphabet, used in the modern English alphabet, the alphabets of other western European languages and others worldwide. Its name in English is ''dee'' (pronounced ), plural ''dees''. History The Semitic letter Dāleth may have developed from the logogram for a fish or a door. There are many different Egyptian hieroglyphs that might have inspired this. In Semitic, Ancient Greek and Latin, the letter represented ; in the Etruscan alphabet the letter was archaic but still retained. The equivalent Greek letter is delta, Δ. The minuscule (lower-case) form of 'd' consists of a lower-story left bowl and a stem ascender. It most likely developed by gradual variations on the majuscule (capital) form 'D', and is now composed as a stem with a full lobe to the right. In handwriting, it was common to start the arc to the left of the vertical stroke, resulting in a serif at the top of the arc. This serif was extended while the rest of t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay, together with mood stabilizers, in the treatment of bipolar disorder. Moreover, they are also used as adjuncts in the treatment of treatment-resistant major depressive disorder. The use of antipsychotics may result in many unwanted side effects such as involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. Long-term use can produce adverse effects such as tardive dyskinesia, tardive dystonia, tardive akathisia, and brain tissue volume reduction. The long term use of antipsychotics often changes the brain both structurally and chemically in a way that can be difficult or impossible to reverse. This can lead ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-Phenylpiperidines
3-Phenylpiperidine is a chemical compound and cyclized phenethylamine. It can be thought of as β-phenethylamine with a propyl group connecting the amine and the β position. 3-Phenylpiperidine is a parent compound of several drugs such as the psychedelic and related drugs LPH-5 and Z3517967757 (Z7757), the antipsychotic OSU-6162, and the sigma receptor agonist 3-PPP. According to Daniel Trachsel and colleagues in 2013, the pharmacology of 3-phenylpiperidine itself has not been reported, only its chemical synthesis has been described. 3-Phenylpiperidine was first described in the scientific literature by 1933. See also * Phenylpiperidines * 4-Phenylpiperidine * 2-Methyl-3-phenylpiperidine * Phenmetrazine * Substituted phenylmorpholine * 1-Phenylpiperazine * Partial ergoline Partial or simplified ergolines and lysergamides are structural analog, analogues of ergolines and substituted lysergamide, lysergamides like LSD in which one or more atoms or covalent bond, bonds, for in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PF-219,061
PF-219,061 is a drug that was under development by Pfizer which acts as a potent and highly selective agonist for the dopamine D3 receptor. It was under development as a potential medication for the treatment of female sexual dysfunction. It did not advance into clinical trials. See also * ABT-670 * ABT-724 * Cabergoline * Bremelanotide * Flibanserin * Intrinsa * Melanotan II * OSU-6162 * PF-592,379 PF-592,379 is a drug developed by Pfizer which acts as a potent, functional_selectivity, selective and orally active agonist for the dopamine D3_receptor, D3 Receptor (biochemistry), receptor, which was under development as a potential medication ... * Pramipexole * Tibolone * UK-414,495 References {{Dopaminergics Dopamine agonists Female sexual dysfunction drugs Phenylmorpholines 3-Hydroxyphenyl compounds Drugs developed by Pfizer Abandoned drugs Aphrodisiacs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
OSU-6162
OSU-6162 (PNU-96391) is a compound which acts as a partial agonist at both dopamine D2 receptors and 5-HT2A receptors. It acts as a dopamine stabilizer in a similar manner to the closely related drug pridopidine, and has antipsychotic, anti- addictive and anti-Parkinsonian effects in animal studies. Both enantiomers show similar activity but with different ratios of effects, with the (S) enantiomer (–)-OSU-6162 that is more commonly used in research, having higher binding affinity to D2 but is a weaker partial agonist at 5-HT2A, while the (R) enantiomer (+)-OSU-6162 has higher efficacy at 5-HT2A but lower D2 affinity. See also * Flumexadol * LPH-5 * PF-219,061 PF-219,061 is a drug that was under development by Pfizer which acts as a potent and highly selective agonist for the dopamine D3 receptor. It was under development as a potential medication for the treatment of female sexual dysfunction. It d ... References {{Serotonergics Benzosulfones Dopamine agon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alazocine
Alazocine (developmental code name -10047), also known more commonly as ''N''-allylnormetazocine (NANM), is a synthetic opioid analgesic of the benzomorphan family related to metazocine, which was never marketed. In addition to its opioid activity, the drug is a sigma receptor agonist, and has been used widely in scientific research in studies of this receptor. Alazocine is described as a potent analgesic, psychotomimetic or hallucinogen, and opioid antagonist. Moreover, one of its enantiomers was the first compound that was found to selectively label the σ1 receptor, and led to the discovery and characterization of the receptor. Pharmacology Pharmacodynamics Alazocine shows stereoselectivity in its pharmacodynamics. The (−)-enantiomer is a non-selective and high-affinity ligand of the μ-, κ-, and δ-opioid receptors (Ki = 3.0, 4.7, and 15 nM in guinea pig brain membranes) with very low affinity for the sigma σ1 receptor (Ki = 1,800–4,657 nM in gui ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-PPBP
4-PPBP is a neuroprotective cyclic amine which binds to sigma receptors. 4-PPBP decreases neuronal nitric oxide synthase (nNOS) activity and ischemia-evoked nitric oxide (NO) production. 4-PPBP provides neuroprotection; this involves the prevention of ischemia-induced intracellular Ca2+ dysregulation. 4-PPBP protects neurons using a mechanism that activates the transcription factor cyclic adenosine monophosphate response element-binding protein (CREB). Neuroprotection that is associated with 4-PPBP increases Bcl-2 expression; Bcl-2 expression is regulated by CREB. See also * 3-PPP 3-PPP (''N''-''n''-propyl-3-(3-hydroxyphenyl)piperidine) is a mixed sigma σ1 and σ2 receptor agonist (with similar affinity for both subtypes, though slightly higher affinity for the latter) and D2 receptor partial agonist which is used in ... References 4-Phenylpiperidines Sigma agonists {{biochem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-Phenylpiperidine
3-Phenylpiperidine is a chemical compound and cyclized phenethylamine. It can be thought of as β-phenethylamine with a propyl group connecting the amine and the β position. 3-Phenylpiperidine is a parent compound of several drugs such as the psychedelic drug, psychedelic and related drugs LPH-5 (drug), LPH-5 and Z3517967757 (Z7757), the antipsychotic OSU-6162, and the sigma receptor agonist 3-PPP. According to Daniel Trachsel and colleagues in 2013, the pharmacology of 3-phenylpiperidine itself has not been reported, only its chemical synthesis has been described. 3-Phenylpiperidine was first described in the scientific literature by 1933. See also * Phenylpiperidines * 4-Phenylpiperidine * 2-Methyl-3-phenylpiperidine * Phenmetrazine * Substituted phenylmorpholine * 1-Phenylpiperazine * Partial ergoline References External links 3-Phenylpiperidine - Isomer Design 3-Phenylpiperidines {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
