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Aporphine
Aporphine is an alkaloid with the chemical formula . The IUPAC (International Union of Pure and Applied Chemistry) name of aporphine is ''6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo e,guinoline.'' It is the core chemical substructure of the aporphine alkaloids, a subclass of quinoline alkaloids. It can exist in either of two enantiomeric forms, (''R'')-aporphine and (''S'')-aporphine. Derivatives Many different derivatives have been isolated from plants. For example, many water-lilies (''Nymphaea'' species) produce aporphine alkaloids such as nymphaeine, nymphaline, nupharine, α- and β- nupharidine. ''In vitro'' tests of some aporphine derivatives isolated from ''Cassytha filiformis'', namely actinodaphnine, cassythine, and dicentrine, showed antiparasitic activity against ''Trypanosoma brucei''. Investigation of possible mechanisms revealed that the compounds bind to DNA and act as intercalating agents, besides inhibiting topoisomerase activity. Aporphine natural products ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aporphine Alkaloids
Aporphine alkaloids are naturally occurring chemical compounds from the group of alkaloids. After the benzylisoquinoline alkaloids they are the second largest group of isoquinoline alkaloids. At least 85 aporphine alkaloids have been isolated from plants of 15 families. The best known representative is apomorphine. The aporphine alkaloids are of interest mainly because of their similarity to morphine. Occurrence The aporphine alkaloids are most commonly found in plants. For example, isoboldine can be found in the plants in the genera ''Beilschmiedia'', '' Nandina'' (''Nandina domestica''), ''Glaucium'' (horn poppy), and other plants. As the name suggests, glaucine was first found in the horn poppy and usually the name of the alkaloids is derived from the plants in which they were first found. Corydin as a further representative of the aporphine alkaloids is found in ''Corydalis'' (larkspurs) '' Dicentra'' (heart flowers), and also in the horn poppy. Examples Apoglazio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Propylnorapomorphine
N-n-Propylnorapomorphine (NPA) is an aporphine derivative dopamine agonist closely related to apomorphine. In rodents it has been shown to produce hyperactivity, stereotypy, hypothermia, antinociception, and penile erection, among other effects. Notably, its effects on locomotion are biphasic, with low doses producing inhibition and catalepsy and high doses resulting in enhancement of activity. This is likely due to preferential activation of D2/ D3 autoreceptors versus postsynaptic receptors, the latter of which overcomes the former to increase postsynaptic dopaminergic signaling only with high doses. See also * Apomorphine Apomorphine, sold under the brand name Apokyn among others, is a type of aporphine having activity as a non- selective dopamine agonist which activates both D2-like and, to a much lesser extent, D1-like receptors. It also acts as an antago ... References Dopamine agonists Catechols Dibenzoquinolines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dicentrine
Dicentrine is an aporphinic alkaloid found in several plant species, mainly from family Lauraceae, including '' Lindera megaphylla''. At high doses, dicentrine shows antinociceptive activity in a mouse model of pain. It probably acts via a TRPA1 Transient receptor potential cation channel, subfamily A, member 1, also known as transient receptor potential ankyrin 1, TRPA1, or The Wasabi Receptor, is a protein that in humans is encoded by the ''TRPA1'' (and in mice and rats by the ''Trpa1' ...-dependent mechanism. References Aporphine alkaloids Lindera {{alkaloid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glaucine
Glaucine is an aporphine alkaloid found in several different plant species in the family Papaveraceae such as ''Glaucium flavum'', '' Glaucium oxylobum'' and '' Corydalis yanhusuo'', and in other plants like ''Croton lechleri'' in the family Euphorbiaceae. It has bronchodilator, neuroleptic and antiinflammatory effects, acting as a PDE4 inhibitor and calcium channel blocker, and is used medically as an antitussive in some countries. TLRs plays role in its anti inflammatory effects. Glaucine may produce side effects such as sedation, fatigue, and a hallucinogenic effect characterised by colourful visual images, and has been detected as a novel psychoactive drug. In a 2019 publication,Heng, HL, Chee, CF, Thy, CK, et al. In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5‐HT2 and α1 receptors. Chem Biol Drug Des. 2019; 93: 132– 138. https://doi.org/10.1111/cbdd.13390 the isomer (R)-glaucine is reported to be a positive allosteric modulator ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Boldine
Boldine is an alkaloid of the aporphine class that can be found in the boldo tree and in ''Lindera aggregata ''Lindera aggregata'' is a plant species belonging to the genus ''Lindera''. Other names Engl.: evergreen lindera, Japanese evergreen spicebush. TCM: trad.烏藥, simpl. 乌药 or 乌乐, pinyin : wūyào. Bot. syn.: ''Benzoin strychnifolium'' ...''. References Aporphine alkaloids Phenols Phenol ethers {{alkaloid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bulbocapnine
Bulbocapnine is an alkaloid found in ''Corydalis'' (notably the European species C. cava) and '' Dicentra'', genera of the plant family Fumariaceae which have caused (notably the American species '' Corydalis caseana'') the fatal poisoning of sheep and cattle. It has been shown to act as an acetylcholinesterase inhibitor, and inhibits biosynthesis of dopamine via inhibition of the enzyme tyrosine hydroxylase. Like apomorphine, it is reported to be an inhibitor of amyloid beta protein (Aβ) fiber formation, whose presence is a hallmark of Alzheimer's disease (AD). Bulbocapnine is thus a potential therapeutic under the amyloid hypothesis. According to the ''Dorlands Medical Dictionary'', it "inhibits the reflex and motor activities of striated muscle. It has been used in the treatment of muscular tremors and vestibular nystagmus". A psychiatrist at Tulane University named Robert Heath carried out experiments on prisoners at the Louisiana State Penitentiary using bulbocapnine t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloid
Alkaloids are a class of basic BASIC (Beginners' All-purpose Symbolic Instruction Code) is a family of general-purpose, high-level programming languages designed for ease of use. The original version was created by John G. Kemeny and Thomas E. Kurtz at Dartmouth College ..., natural product, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of similar structure may also be termed alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and, more rarely, other elements such as chlorine, bromine, and phosphorus.Chemical Encyclopedia: alkaloids xumuk.ru Alkaloids are produced by a large variety of organisms includi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Receptor D2
Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the ''DRD2'' gene. After work from Paul Greengard's lab had suggested that dopamine receptors were the site of action of antipsychotic drugs, several groups, including those of Solomon Snyder and Philip Seeman used a radiolabeled antipsychotic drug to identify what is now known as the dopamine D2 receptor. The dopamine D2 receptor is the main receptor for most antipsychotic drugs. The structure of DRD2 in complex with the atypical antipsychotic risperidone has been determined. Function D2 receptors are coupled to Gi subtype of G protein. This G protein-coupled receptor inhibits adenylyl cyclase activity. In mice, regulation of D2R surface expression by the neuronal calcium sensor-1 (NCS-1) in the dentate gyrus is involved in exploration, synaptic plasticity and memory formation. Studies have shown potential roles for D2R in retrieval of fear memories in the prelimbic cortex and in disc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nociception
Nociception (also nocioception, from Latin ''nocere'' 'to harm or hurt') is the sensory nervous system's process of encoding noxious stimuli. It deals with a series of events and processes required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal in order to trigger an appropriate defense response. In nociception, intense chemical (e.g., capsaicin present in Chili pepper or Cayenne pepper), mechanical (e.g., cutting, crushing), or thermal (heat and cold) stimulation of sensory neurons called nociceptors produces a signal that travels along a chain of nerve fibers via the spinal cord to the brain. Nociception triggers a variety of physiological and behavioral responses to protect the organism against an aggression and usually results in a subjective experience, or perception, of pain in sentient beings. Detection of noxious stimuli Potentially damaging mechanical, thermal, and chemical stimuli are det ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naloxone
Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter decreased breathing in opioid overdose. Effects begin within two minutes when given intravenously, and within five minutes when injected into a muscle. The medicine can also be administered by spraying it into a person's nose. Naloxone commonly blocks the effects of opioids for 30 to 90 minutes. Multiple doses may be required, as the duration of action of some opioids is greater than that of naloxone. Administration to opioid-dependent individuals may cause symptoms of opioid withdrawal, including restlessness, agitation, nausea, vomiting, a fast heart rate, and sweating. To prevent this, small doses every few minutes can be given until the desired effect is reached. In those with previous heart disease or taking medications that negatively affect the heart, further heart problems have occu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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