3-F-BPAP
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3-F-BPAP
3-F-BPAP is a trifluorinated derivative of benzofuranylpropylaminopentane (BPAP) and is an antagonist of the monoaminergic activity enhancer (MAE) effects of the tryptamine-related BPAP. Conversely, 3-F-BPAP does not antagonize the catecholaminergic activity enhancer (CAE) effects of the phenethylamine- derived selegiline (L-deprenyl) and phenylpropylaminopentane (PPAP). This suggests that different MAEs like BPAP and selegiline may not be identical in their actions and might be acting via different receptor subtypes. In contrast to 3-F-BPAP however, the TAAR1 antagonist EPPTB antagonizes the MAE effects of both BPAP and selegiline. 3-F-BPAP has a weak MAE effect itself but with much lower potency than BPAP. The effects of MAEs like BPAP and selegiline appear to be mediated by TAAR1 agonism, and hence 3-F-BPAP may be acting as a TAAR1 antagonist (or weak partial agonist). 3-F-BPAP was developed by József Knoll and colleagues and was first described in the scientific litera ...
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Monoaminergic Activity Enhancer
Monoaminergic activity enhancers (MAE), also known as catecholaminergic/serotonergic activity enhancers (CAE/SAE), are a class of drugs that enhance the action potential-evoked release of monoamine neurotransmitters in the nervous system. MAEs are distinct from monoamine releasing agents (MRAs) like amphetamine and fenfluramine in that they do not induce the release of monoamines from synaptic vesicles but rather potentiate only nerve impulse propagation-mediated monoamine release. That is, MAEs increase the amounts of monoamine neurotransmitters released by neurons per electrical impulse. MAEs have been shown to significantly enhance nerve impulse-mediated dopamine release in the striatum, substantia nigra, and olfactory tubercle; norepinephrine release from the locus coeruleus; and/or serotonin release from the raphe nucleus in rodent studies. Some MAEs are selective for effects on some of these neurotransmitters but not on others. The maximal impacts of MAEs on brain monoam ...
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Benzofuranylpropylaminopentane
(–)-Benzofuranylpropylaminopentane (BPAP; developmental code name FPFS-1169) is an experimental drug related to selegiline which acts as a monoaminergic activity enhancer (MAE). It is orally active in animals. BPAP is a highly potent MAE and enhances the nerve impulse propagation-mediated release of serotonin, norepinephrine, and dopamine. At much higher concentrations, BPAP is also a monoamine reuptake inhibitor, specifically of dopamine and norepinephrine and to a much lesser extent of serotonin. BPAP produces psychostimulant-like effects in animals, with these effects mediated by its MAE actions. The drug is a substituted benzofuran derivative and tryptamine relative structurally related to phenylpropylaminopentane (PPAP). BPAP was first described in 1999. There has been interest in BPAP for potential clinical use in humans, including in the treatment of Parkinson's disease, Alzheimer's disease, and depression. There has also been interest in BPAP to help slow aging. ...
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Monoaminergic Activity Enhancer
Monoaminergic activity enhancers (MAE), also known as catecholaminergic/serotonergic activity enhancers (CAE/SAE), are a class of drugs that enhance the action potential-evoked release of monoamine neurotransmitters in the nervous system. MAEs are distinct from monoamine releasing agents (MRAs) like amphetamine and fenfluramine in that they do not induce the release of monoamines from synaptic vesicles but rather potentiate only nerve impulse propagation-mediated monoamine release. That is, MAEs increase the amounts of monoamine neurotransmitters released by neurons per electrical impulse. MAEs have been shown to significantly enhance nerve impulse-mediated dopamine release in the striatum, substantia nigra, and olfactory tubercle; norepinephrine release from the locus coeruleus; and/or serotonin release from the raphe nucleus in rodent studies. Some MAEs are selective for effects on some of these neurotransmitters but not on others. The maximal impacts of MAEs on brain monoam ...
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Phenylpropylaminopentane
1-Phenyl-2-propylaminopentane (PPAP), also known as α,''N''-dipropylphenethylamine (DPPEA) and by the developmental code name MK-306, is an experimental drug related to selegiline which acts as a catecholaminergic activity enhancer (CAE). PPAP is a CAE and enhances the nerve impulse propagation-mediated release of norepinephrine and dopamine. It produces psychostimulant-like effects in animals. The drug is a phenethylamine and amphetamine derivative and was derived from selegiline. PPAP was first described in the literature in 1988 and in the first major paper in 1992. It led to the development of the improved monoaminergic activity enhancer (MAE) benzofuranylpropylaminopentane (BPAP) in 1999. PPAP was a reference compound for studying the MAE system for many years. However, it was superseded by BPAP, which is more potent, selective, and also enhances serotonin. There has been interest in PPAP for potential clinical use in humans, including in the treatment of depression, ...
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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 ...
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Monoaminergic Activity Enhancer Antagonists
Monoaminergic means "working on monoamine neurotransmitters", which include serotonin, dopamine, norepinephrine, epinephrine, and histamine. A monoaminergic, or monoaminergic drug, is a chemical, which functions to directly modulate the serotonin, dopamine, norepinephrine, epinephrine, and/or histamine neurotransmitter systems in the brain. Monoaminergics include catecholaminergics (which can be further divided into adrenergics and dopaminergics), serotonergics, and histaminergics. Examples of monoaminergic drugs include monoamine precursors, monoamine receptor modulators, monoamine reuptake inhibitors, monoamine releasing agents, and monoamine metabolism modulators such as monoamine oxidase inhibitors. See also * Adenosinergic * Adrenergic * Cannabinoidergic * Cholinergic * Dopaminergic * GABAergic * Glycinergic * Histaminergic * Melatonergic * Opioidergic An opioidergic agent (or drug) is a chemical which directly or indirectly modulate the function of opioid receptors. O ...
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Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ...
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Drugs With Unknown Mechanisms Of Action
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that have s ...
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Scientific Literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical contributions. These papers serve as essential sources of knowledge and are commonly referred to simply as "the literature" within specific research fields. The process of academic publishing involves disseminating research findings to a wider audience. Researchers submit their work to reputable journals or conferences, where it undergoes rigorous evaluation by experts in the field. This evaluation, known as peer review, ensures the quality, validity, and reliability of the research before it becomes part of the scientific literature. Peer-reviewed publications contribute significantly to advancing our understanding of the world and shaping future research endeavors. Original scientific research first published in scientific journals co ...
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József Knoll
József Knoll (May 30, 1925 – April 17, 2018), or Joseph Knoll, was a Hungarian psychopharmacologist known for developing the antiparkinsonian and antidepressant drug selegiline (L-deprenyl). He developed selegiline in the 1960s and subsequently studied the drug and related agents for many decades. Knoll also developed the concepts of monoaminergic activity enhancers (MAEs) and the mesencephalic enhancer regulation system, among other contributions. MAEs developed by Knoll and colleagues include selegiline, benzofuranylpropylaminopentane (BPAP), and phenylpropylaminopentane (PPAP), among others. During his scientific career, Knoll published 894papers and was the originator of 55patents. As of 2018, his papers had been cited more than 10,000times. He is described as one of the best-known Hungarian pharmacologists. Knoll is known for having extensively researched and promoted selegiline for claimed drive- and longevity Longevity may refer to especially long-lived members ...
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