Neurokinin A
Neurokinin B
Receptors, Neurokinin-2
Receptors, Neurokinin-1
Tachykinins
Receptors, Neurokinin-3
Substance P
Receptors, Tachykinin
Neurokinin-1 Receptor Antagonists
Receptors, Neurotransmitter
Kisspeptins
Eledoisin
Isoindoles
Physalaemin
Quinuclidines
Pyrrolidonecarboxylic Acid
Arcuate Nucleus
Dynorphins
Guinea Pigs
Neuropeptides
Calcitonin Gene-Related Peptide
Muscle, Smooth
Bronchoconstriction
Peptide Fragments
Trachea
Muscle Contraction
Thiorphan
Atropine
Ileum
Neurogenic Inflammation
Neurons
Neprilysin
Dose-Response Relationship, Drug
Gonadotropin-Releasing Hormone
Spinal Cord
Biphenyl Compounds
Rats, Sprague-Dawley
Peptides, Cyclic
Radioligand Assay
Bethanechol Compounds
Posterior Horn Cells
Bethanechol
Rats, Wistar
Neurogenic plasma leakage in mouse airways. (1/231)
1. This study sought to determine whether neurogenic inflammation occurs in the airways by examining the effects of capsaicin or substance P on microvascular plasma leakage in the trachea and lungs of male pathogen-free C57BL/6 mice. 2. Single bolus intravenous injections of capsaicin (0.5 and 1 micromol kg(-1), i.v.) or substance P (1, 10 and 37 nmol kg(-10, i.v.) failed to induce significant leakage in the trachea, assessed as extravasation of Evans blue dye, but did induce leakage in the urinary bladder and skin. 3. Pretreatment with captopril (2.5 mg kg(-1), i.v.), a selective inhibitor of angiotensin converting enzyme (ACE), either alone or in combination with phosphoramidon (2.5 mg kg(-1), i.v.), a selective inhibitor of neutral endopeptidase (NEP), increased baseline leakage of Evans blue in the absence of any exogenous inflammatory mediator. The increase was reversed by the bradykinin B2 receptor antagonist Hoe 140 (0.1 mg kg(-1), i.v.). 4. After pretreatment with phosphoramidon and captopril, capsaicin increased the Evans blue leakage above the baseline in the trachea, but not in the lung. This increase was reversed by the tachykinin (NK1) receptor antagonist SR 140333 (0.7 mg kg(-1), i.v.), but not by the NK2 receptor antagonist SR 48968 (1 mg kg(-1), i.v.). 5. Experiments using Monastral blue pigment as a tracer localized the leakage to postcapillary venules in the trachea and intrapulmonary bronchi, although the labelled vessels were less numerous in mice than in comparably treated rats. Blood vessels of the pulmonary circulation were not labelled. 6. We conclude that neurogenic inflammation can occur in airways of pathogen-free mice, but only after the inhibition of enzymes that normally degrade inflammatory peptides. Neurogenic inflammation does not involve the pulmonary microvasculature. (+info)Conserved polar residues in the transmembrane domain of the human tachykinin NK2 receptor: functional roles and structural implications. (2/231)
We have studied the effects of agonist and antagonist binding, agonist-induced activation and agonist-induced desensitization of the human tachykinin NK2 receptor mutated at polar residues Asn-51 [in transmembrane helix 1 (TM1)], Asp-79 (TM2) and Asn-303 (TM7), which are highly conserved in the transmembrane domain in the rhodopsin family of G-protein-coupled receptors. Wild-type and mutant receptors were expressed in both COS-1 cells and Xenopus oocytes. The results show that the N51D mutation results in a receptor which, in contrast with the wild-type receptor, is desensitized by the application of a concentration of 1 microM of the partial agonist GR64349, indicating that the mutant is more sensitive to agonist activation than is the wild-type receptor. In addition, we show that, whereas the D79E mutant displayed activation properties similar to those of the wild-type receptor, the D79N and D79A mutants displayed a severely impaired ability to activate the calcium-dependent chloride current. This suggests that it is the negative charge at Asn-79, rather than the ability of this residue to hydrogen-bond, that is critical for the activity of the receptor. Interestingly, the placement of a negative charge at position 303 could compensate for the removal of the negative charge at position 79, since the double mutant D79N/N303D displayed activation properties similar to those of the wild-type receptor. This suggests that these two residues are functionally coupled, and may even be in close proximity in the three-dimensional structure of the human tachykinin NK2 receptor. A three-dimensional model of the receptor displaying this putative interaction is presented. (+info)Respiratory action of capsaicin microinjected into the nucleus of the solitary tract: involvement of vanilloid and tachykinin receptors. (3/231)
1. The respiratory response to microinjection of capsaicin into the commissural nucleus of the solitary tract (cNTS) of urethane-anaesthetized rats was investigated in the absence and presence of the competitive vanilloid (capsaicin) antagonist, capsazepine, and selective tachykinin NK1, NK2 and NK3 antagonists (RP 67580, SR 48968 and SR 142801, respectively). 2. Microinjection of capsaicin reduced respiratory frequency but not tidal volume (VT), leading to an overall reduction in minute ventilation (VE). The effect was dose-dependent between 0.5 and 2 nmol capsaicin. Doses greater than 2 nmol produced apnoea. Tachyphylaxis was observed following repeated injection of capsaicin (1 nmol, 30 min apart). 3. Capsazepine (1 nmol) had no effect on frequency or VT when injected alone but completely blocked the respiratory response to capsaicin (1 nmol). 4. RP 67580 (1 but not 5 nmol) alone depressed frequency and VT slightly. Moreover, RP 67580 appeared to potentiate the bradypnoeic effect of capsaicin. In contrast, SR 48968 and SR 142801 (1 and 5 nmol) alone had no significant effect on respiration. However, both agents significantly attenuated the reduction in frequency produced by capsaicin. 5. In conclusion, microinjection of capsaicin into the cNTS decreases overall ventilation, primarily by reducing frequency. The action of capsaicin appears from the data to be mediated by vanilloid receptors since it is blocked by the competitive vanilloid antagonist capsazepine and is subject to tachyphylaxis. However, since NK2 (SR 48968) and NK3 (SR 142801) receptor antagonists block the actions of capsaicin, we propose that capsaicin acts also by releasing tachykinins from central afferent terminals in the cNTS. (+info)Relevance of aromatic residues in transmembrane segments V to VII for binding of peptide and nonpeptide antagonists to the human tachykinin NK(2) receptor. (4/231)
We used membranes from Chinese hamster ovary cells stably transfected with the human tachykinin NK(2) receptor, either wild-type or mutated, at four aromatic residues (His(198), Tyr(266), Phe(270), Tyr(289)) located in transmembrane segments V to VII, to assess the role of these residues in the binding of natural tachykinins and peptide and nonpeptide antagonists. Three radioligands, the agonist [(125)I]neurokinin A (NKA), the peptide antagonist [(3)H]MEN 11420, and the nonpeptide antagonist [(3)H]SR 48968 bound to the wild-type receptor with high affinity (K(d) = 2.4 nM, 0.3 nM, and 4.0 nM, respectively). Four of the six mutant receptors tested retained high affinity for at least one of the radioligands. H(198)A mutation abrogated the binding of NKA but not that of MEN 11420 or SR 48968 (K(d) = 4.8 and 11.5 nM, respectively); Y(266)F mutation abrogated the binding of MEN 11420 but not that of NKA or SR 48968 (K(d) = 2.8 nM and 1.2 nM, respectively); F(270)A mutation abrogated the binding of both NKA and MEN 11420 but not that of SR 48968 (K(d) = 1.6 nM); Y(289)F mutation abrogated the binding of SR 48968 but not that of NKA and MEN 11420 (K(d) = 2.0 and 2.9 nM, respectively). Y(266)A and Y(289)A mutations abrogated the binding of all radioligands. Among the unlabeled antagonists, the affinity of the nonpeptide GR 159897, at variance with SR 48968, resulted heavily compromised by H(198)A and Y(266)F mutations; the peptide antagonists R396 and MEN 10376 essentially followed the binding profile of NKA, but R396 showed markedly increased affinity for the Y(289)F mutant receptor. Taken together, these results indicate that different, partially overlapping sets of sites may be involved in the binding of agonists and diverse antagonists to the human tachykinin NK(2) receptor. (+info)Role of tachykinin NK2-receptor activation in the allergen-induced late asthmatic reaction, airway hyperreactivity and airway inflammatory cell influx in conscious, unrestrained guinea-pigs. (5/231)
1. In a guinea-pig model of allergic asthma, we investigated the involvement of the tachykinin NK2 receptors in allergen-induced early (EAR) and late (LAR) asthmatic reactions, airway hyperreactivity (AHR) after these reactions and inflammatory cell influx in the airways, using the selective non-peptide NK2 receptor antagonist SR48968. 2. On two different occasions, separated by a 1 week interval, ovalbumin (OA)-sensitized guinea-pigs inhaled either vehicle (3 min) or SR48968 (100 nM, 3 min) at 30 min before as well as at 5.5 h after OA provocation (between the EAR and LAR) in a random crossover design. 3. SR48968 had no significant effect on the EAR, but significantly attenuated the LAR by 44.2+/-16.4% (P<0.05) compared to saline control. 4. The NK2 receptor antagonist did not affect the OA-induced AHR to histamine after the EAR at 5 h after OA challenge (3.59+/-0.59 fold increase in histamine reactivity vs 3.79+/-0.61 fold increase in the controls, NS), but significantly reduced the AHR after the LAR at 23 h after OA challenge (1.59+/-0.24 fold increase vs 1.93+/-0.15 fold increase, respectively, P<0.05). 5. Bronchoalveolar lavage studies performed at 25 h after the second OA provocation showed that SR48968 significantly inhibited the allergen-induced infiltration of neutrophils (P<0.05) and lymphocytes (P<0.01) in the airways. 6. These results indicate that NK2 receptor activation is importantly involved in the development of the allergen-induced late (but not early) asthmatic reaction and late (but not early) AHR to histamine, and that NK2 receptor-mediated infiltration of neutrophils and lymphocytes in the airways may contribute to these effects. (+info)Characterization of the [125I]-neurokinin A binding site in the circular muscle of human colon. (6/231)
Neurokinin A (NKA) is a potent contractile agonist of human colon circular muscle. These responses are mediated predominantly through tachykinin NK2 receptors. In the present study, the NK2 receptor radioligand [125I]-NKA has been used to characterize binding sites in this tissue, using tachykinin agonists and antagonists. 125INKA labelled a single, high affinity binding site. Specific binding (95% of total binding) of [125I]-NKA was saturable (K(D) 0.47+/-0.05 nM), of high capacity (Bmax 2.1+/-0.1 fmol mg(-1) wet weight tissue) and reversible (kinetically derived K(D) 0.36+/-0.07 nM). The rank order of agonists competing for the [125I]-NKA binding site was neuropeptide gamma (NPgamma) > or = NKA > or = [Lys5, MeLeu9,Nle10]NKA (4-10) (NK2 agonist) >> substance P (SP) > neurokinin B (NKB) > or = [Pro9]SP (NK1 agonist) >> senktide (NK3 agonist), indicating binding to an NK2 site. The nonpeptide selective NK2 antagonist SR48968 showed higher affinity for the [125I]-NKA site than selective peptide NK2 antagonists. The rank order of potency for NK2 antagonists was SR48968 > or = MEN11420 > GR94800 > or = MEN10627 > MEN10376 > or = R396. The NK1 antagonist SR140333 was a weak competitor. The competition curve for SP could be resolved into two sites. When experiments were repeated in the presence of SR140333 (0.1 microM), the curve for SP became monophasic and showed a significant shift to the right, whereas curves to NKA and NKB were unaffected. In conclusion, binding of the radioligand [125I]-NKA to membranes from circular muscle is predominantly to the NK2 receptor. There may be a small component of binding to the NK1 receptor. The NK2 receptor mediates circular muscle contraction, whereas the role of the NK1 receptor in circular muscle is unclear. (+info)Airway hyperresponsiveness induced by chronic exposure to cigarette smoke in guinea pigs: role of tachykinins. (7/231)
This study was carried out to determine whether tachykinins released from lung C-fiber afferents play a part in the bronchial hyperreactivity induced in guinea pigs by chronic exposure to cigarette smoke (CS). Two matching groups of young guinea pigs were exposed to either mainstream CS (CS group) or air (control group) for 20 min twice daily for 14-17 days. There was no difference in the baseline total pulmonary resistance (RL) between the two groups, but the baseline dynamic lung compliance was reduced ( approximately 19%) in CS animals. The responses of RL to intravenous injections of ACh, neurokinin (NK) A, and capsaicin were all markedly increased in CS animals; for example, ACh at the same dose of 5.06 microg/kg increased RL by 207% in the control group and by 697% (n = 8; P < 0. 001) in the CS group. The increased responsiveness was accompanied by significant increases in the numbers of neutrophils, eosinophils, and macrophages in the bronchoalveolar lavage fluid in CS animals. Pretreatment with SR-48968 and CP-99994, antagonists of NK(1) and NK(2) receptors, respectively, did not alter the response of RL to ACh in control animals, but it abolished the elevated bronchoconstrictive response in the CS animals. Furthermore, the immunoreactivities of substance P and calcitonin gene-related peptide in the bronchoalveolar lavage fluid collected after capsaicin challenge were significantly increased in CS animals. These results show that chronic exposure to CS induced airway mucosal inflammation accompanied by bronchial hyperreactivity in guinea pigs and that the tachykininergic mechanism plays an important role in this augmented responsiveness. (+info)Subcellular compartmentalization of activation and desensitization of responses mediated by NK2 neurokinin receptors. (8/231)
A functional fluorescent neurokinin NK2 receptor was constructed by joining enhanced green fluorescent protein to the amino-terminal end of the rat NK2 receptor and was expressed in human embryonic kidney cells. On cell suspensions, the binding of fluorescent Bodipy-labeled neurokinin A results in a saturatable and reversible decrease of NK2 receptor fluorescence via fluorescence resonance energy transfer. This can be quantified for nM to microM agonist concentrations and monitored in parallel with intracellular calcium responses. On single cells, receptor site occupancy and local agonist concentration can be determined in real time from the decrease in receptor fluorescence. Simultaneous measurement of intracellular calcium responses and agonist binding reveals that partial receptor site occupancy is sufficient to desensitize cellular response to a second agonist application to the same membrane area. Subsequent stimulation of a distal membrane area leads to a second response to agonist, provided that it had not been exposed to agonist during the first application. Together with persistent translocation of fluorescent protein kinase C to the membrane area exposed to agonist, the present data support that not only homologous desensitization but also heterologous desensitization of NK2 receptors is compartmentalized to discrete membrane domains. (+info)Neurokinin A (NKA) is a neuropeptide belonging to the tachykinin family, which also includes substance P and neurokinin B. It is widely distributed in the central and peripheral nervous systems and plays a role in various physiological functions such as pain transmission, smooth muscle contraction, and immune response regulation. NKA exerts its effects by binding to neurokinin 1 (NK-1) receptors, although it has lower affinity for these receptors compared to substance P. It is involved in several pathological conditions, including inflammation, neurogenic pain, and neurodegenerative disorders.
Neurokinin B is a neuropeptide belonging to the tachykinin family, which also includes substance P and neurokinin A. It is encoded by the TAC3 gene in humans and is widely distributed throughout the central and peripheral nervous systems. Neurokinin B exerts its effects by binding to the neurokinin 3 receptor (NK3R) and plays a role in various physiological processes, including the regulation of feeding behavior, reproduction, and nociception (pain perception). It has also been implicated in several pathological conditions, such as inflammatory diseases, chronic pain, and certain types of cancer.
Neurokinin-2 (NK-2) receptors are a type of G protein-coupled receptor that binds to and is activated by the neuropeptide substance P, which is a member of the tachykinin family. These receptors are widely distributed in the central and peripheral nervous systems and play important roles in various physiological functions, including pain transmission, smooth muscle contraction, and neuroinflammation.
NK-2 receptors are involved in the development of hyperalgesia (an increased sensitivity to pain) and allodynia (pain caused by a stimulus that does not normally provoke pain). They have also been implicated in several pathological conditions, such as inflammatory bowel disease, asthma, and neurodegenerative disorders.
NK-2 receptor antagonists have been developed and investigated for their potential therapeutic use in the treatment of various pain disorders, gastrointestinal diseases, and other medical conditions.
Neurokinin-1 (NK-1) receptors are a type of G protein-coupled receptor that bind to the neuropeptide substance P, which is a member of the tachykinin family. These receptors are widely distributed in the central and peripheral nervous systems and play important roles in various physiological functions, including pain transmission, neuroinflammation, and emesis (vomiting).
NK-1 receptors are activated by substance P, which binds to the receptor's extracellular domain and triggers a signaling cascade that leads to the activation of various intracellular signaling pathways. This activation can ultimately result in the modulation of neuronal excitability, neurotransmitter release, and gene expression.
In addition to their role in normal physiological processes, NK-1 receptors have also been implicated in a number of pathological conditions, including pain, inflammation, and neurodegenerative disorders. As such, NK-1 receptor antagonists have been developed as potential therapeutic agents for the treatment of these conditions.
Tachykinins are a group of neuropeptides that share a common carboxy-terminal sequence and bind to G protein-coupled receptors, called tachykinin receptors. They are widely distributed in the nervous system and play important roles as neurotransmitters or neuromodulators in various physiological functions, such as pain transmission, smooth muscle contraction, and inflammation. The most well-known tachykinins include substance P, neurokinin A, and neuropeptide K. They are involved in many pathological conditions, including chronic pain, neuroinflammation, and neurodegenerative diseases.
Neurokinin-3 (NK-3) receptors are a type of G protein-coupled receptor that binds the neuropeptide neurokinin B, which is a member of the tachykinin family. These receptors are widely distributed in the central and peripheral nervous systems and play important roles in various physiological functions, including the regulation of nociception (pain perception), inflammation, and reproduction.
NK-3 receptors have been identified as key mediators of female reproductive function, particularly in the hypothalamus where they are involved in the control of gonadotropin-releasing hormone (GnRH) secretion. Dysregulation of NK-3 receptor signaling has been implicated in several reproductive disorders, including polycystic ovary syndrome and endometriosis.
In addition to their role in reproduction, NK-3 receptors have also been implicated in various neurological and psychiatric conditions, such as anxiety, depression, and drug addiction. As a result, NK-3 receptor antagonists have emerged as potential therapeutic targets for the treatment of these disorders.
Substance P is an undecapeptide neurotransmitter and neuromodulator, belonging to the tachykinin family of peptides. It is widely distributed in the central and peripheral nervous systems and is primarily found in sensory neurons. Substance P plays a crucial role in pain transmission, inflammation, and various autonomic functions. It exerts its effects by binding to neurokinin 1 (NK-1) receptors, which are expressed on the surface of target cells. Apart from nociception and inflammation, Substance P is also involved in regulating emotional behaviors, smooth muscle contraction, and fluid balance.
Tachykinin receptors are a type of G protein-coupled receptor (GPCR) that bind and respond to tachykinins, which are neuropeptides involved in various physiological functions such as neurotransmission, smooth muscle contraction, vasodilation, and pain perception. There are three main subtypes of tachykinin receptors: NK1, NK2, and NK3.
NK1 receptors primarily bind substance P, a neuropeptide that plays a role in neurotransmission, inflammation, and pain signaling. NK2 receptors mainly bind neurokinin A (NKA) and are involved in smooth muscle contraction, particularly in the respiratory and gastrointestinal tracts. NK3 receptors primarily bind neurokinin B (NKB) and are found in the central nervous system, where they play a role in regulating body temperature, feeding behavior, and sexual function.
Tachykinin receptors have been implicated in various pathological conditions such as chronic pain, inflammation, asthma, and neurodegenerative disorders. As a result, tachykinin receptor antagonists are being developed as potential therapeutic agents for these conditions.
Neurokinin-1 (NK-1) receptor antagonists are a class of drugs that block the action of substance P, a neuropeptide involved in pain transmission and inflammation. These drugs work by binding to NK-1 receptors found on nerve cells, preventing substance P from activating them and transmitting pain signals. NK-1 receptor antagonists have been studied for their potential use in treating various conditions associated with pain and inflammation, such as migraine headaches, depression, and irritable bowel syndrome. Some examples of NK-1 receptor antagonists include aprepitant, fosaprepitant, and rolapitant.
Neurotransmitter receptors are specialized protein molecules found on the surface of neurons and other cells in the body. They play a crucial role in chemical communication within the nervous system by binding to specific neurotransmitters, which are chemicals that transmit signals across the synapse (the tiny gap between two neurons).
When a neurotransmitter binds to its corresponding receptor, it triggers a series of biochemical events that can either excite or inhibit the activity of the target neuron. This interaction helps regulate various physiological processes, including mood, cognition, movement, and sensation.
Neurotransmitter receptors can be classified into two main categories based on their mechanism of action: ionotropic and metabotropic receptors. Ionotropic receptors are ligand-gated ion channels that directly allow ions to flow through the cell membrane upon neurotransmitter binding, leading to rapid changes in neuronal excitability. In contrast, metabotropic receptors are linked to G proteins and second messenger systems, which modulate various intracellular signaling pathways more slowly.
Examples of neurotransmitters include glutamate, GABA (gamma-aminobutyric acid), dopamine, serotonin, acetylcholine, and norepinephrine, among others. Each neurotransmitter has its specific receptor types, which may have distinct functions and distributions within the nervous system. Understanding the roles of these receptors and their interactions with neurotransmitters is essential for developing therapeutic strategies to treat various neurological and psychiatric disorders.
Kisspeptins are a family of peptides that are derived from the preproprotein kisspeptin. The most well-known member of this family is kisspeptin-54, which is also known as metastin. Kisspeptins play important roles in several physiological processes, including the regulation of growth, inflammation, and energy homeostasis. However, they are perhaps best known for their role in the reproductive system.
In the reproductive system, kisspeptins act as key regulators of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for controlling reproductive function. Kisspeptins are produced by neurons in the hypothalamus and bind to receptors on other neurons that release gonadotropin-releasing hormone (GnRH). GnRH then stimulates the pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which act on the gonads to promote the production of sex steroids and eggs or sperm.
Dysregulation of the HPG axis, including abnormal kisspeptin signaling, has been implicated in a number of reproductive disorders, such as precocious puberty, delayed puberty, and infertility. As such, there is significant interest in understanding the role of kisspeptins in reproductive function and developing therapies that target this pathway.
Eledoisin is a tachykinin peptide that is found in the venom of certain marine cephalopods, such as the octopus and squid. It is a potent vasodilator and smooth muscle stimulant, and has been studied for its potential therapeutic uses in conditions such as asthma, bronchitis, and cardiovascular disease. However, it has not yet been approved for use in medical treatments.
Isoindoles are not typically considered in the context of medical definitions, as they are organic compounds that do not have direct relevance to medical terminology or human disease. However, isoindole is a heterocyclic compound that contains two nitrogen atoms in its structure and can be found in some naturally occurring substances and synthetic drugs.
Isoindoles are aromatic compounds, which means they have a stable ring structure with delocalized electrons. They can form the core structure of various bioactive molecules, including alkaloids, which are nitrogen-containing compounds that occur naturally in plants and animals and can have various pharmacological activities.
Some isoindole derivatives have been synthesized and studied for their potential medicinal properties, such as anti-inflammatory, antiviral, and anticancer activities. However, these compounds are still in the early stages of research and development and have not yet been approved for medical use.
Therefore, while isoindoles themselves do not have a specific medical definition, they can be relevant to the study of medicinal chemistry and drug discovery.
Physalaemin is defined as a polypeptide toxin that is derived from the skin of certain frog species, specifically in the genus Physalaemus. This peptide contains 24 amino acids and has been found to have various pharmacological effects, including acting as a potent vasodilator, smooth muscle relaxant, and hypotensive agent. It also interacts with opioid receptors in the brain and can produce analgesic (pain-relieving) and hyperalgesic (increased sensitivity to pain) effects. Physalaemin is primarily used in research settings for its pharmacological properties and as a tool to study the structure and function of opioid receptors.
Quinuclidines are a class of organic compounds that contain a unique cage-like structure consisting of a tetrahydrofuran ring fused to a piperidine ring. The name "quinuclidine" is derived from the Latin word "quinque," meaning five, and "clidis," meaning key or bar, which refers to the five-membered ring system that forms the core of these compounds.
Quinuclidines have a variety of biological activities and are used in pharmaceuticals as well as agrochemicals. Some quinuclidine derivatives have been found to exhibit anti-inflammatory, antiviral, and anticancer properties. They can also act as inhibitors of various enzymes and receptors, making them useful tools for studying biological systems and developing new drugs.
It is worth noting that quinuclidines are not typically used in medical diagnosis or treatment, but rather serve as building blocks for the development of new pharmaceutical compounds.
Capsaicin is defined in medical terms as the active component of chili peppers (genus Capsicum) that produces a burning sensation when it comes into contact with mucous membranes or skin. It is a potent irritant and is used topically as a counterirritant in some creams and patches to relieve pain. Capsaicin works by depleting substance P, a neurotransmitter that relays pain signals to the brain, from nerve endings.
Here is the medical definition of capsaicin from the Merriam-Webster's Medical Dictionary:
caпсаісіn : an alkaloid (C18H27NO3) that is the active principle of red peppers and is used in topical preparations as a counterirritant and analgesic.
Pyrrolidonecarboxylic acid, also known as Proline or Prolinic acid, is an organic compound with the formula N-pyrrolidinecarboxylic acid. It is a cyclic amino acid, which means that its side chain is bonded to the rest of the molecule in a ring structure.
Proline is an important constituent of many proteins and plays a crucial role in maintaining the structural integrity of the protein. It is classified as a non-essential amino acid because it can be synthesized by the human body from other amino acids, such as glutamic acid.
Pyrrolidonecarboxylic acid has a variety of uses in medicine and industry, including as a chiral auxiliary in organic synthesis, a building block for pharmaceuticals, and a component in cosmetics and personal care products. It is also used as a buffering agent and a stabilizer in various medical and industrial applications.
Piperidines are not a medical term per se, but they are a class of organic compounds that have important applications in the pharmaceutical industry. Medically relevant piperidines include various drugs such as some antihistamines, antidepressants, and muscle relaxants.
A piperidine is a heterocyclic amine with a six-membered ring containing five carbon atoms and one nitrogen atom. The structure can be described as a cyclic secondary amine. Piperidines are found in some natural alkaloids, such as those derived from the pepper plant (Piper nigrum), which gives piperidines their name.
In a medical context, it is more common to encounter specific drugs that belong to the class of piperidines rather than the term itself.
The arcuate nucleus is a part of the hypothalamus in the brain. It is involved in the regulation of various physiological functions, including appetite, satiety, and reproductive hormones. The arcuate nucleus contains two main types of neurons: those that produce neuropeptide Y and agouti-related protein, which stimulate feeding and reduce energy expenditure; and those that produce pro-opiomelanocortin and cocaine-and-amphetamine-regulated transcript, which suppress appetite and increase energy expenditure. These neurons communicate with other parts of the brain to help maintain energy balance and reproductive function.
Dynorphins are a type of opioid peptide that is naturally produced in the body. They bind to specific receptors in the brain, known as kappa-opioid receptors, and play a role in modulating pain perception, emotional response, and reward processing. Dynorphins are derived from a larger precursor protein called prodynorphin and are found throughout the nervous system, including in the spinal cord, brainstem, and limbic system. They have been implicated in various physiological processes, as well as in the development of certain neurological and psychiatric disorders, such as chronic pain, depression, and substance use disorders.
I must clarify that the term "Guinea Pigs" is not typically used in medical definitions. However, in colloquial or informal language, it may refer to people who are used as the first to try out a new medical treatment or drug. This is known as being a "test subject" or "in a clinical trial."
In the field of scientific research, particularly in studies involving animals, guinea pigs are small rodents that are often used as experimental subjects due to their size, cost-effectiveness, and ease of handling. They are not actually pigs from Guinea, despite their name's origins being unclear. However, they do not exactly fit the description of being used in human medical experiments.
Neuropeptides are small protein-like molecules that are used by neurons to communicate with each other and with other cells in the body. They are produced in the cell body of a neuron, processed from larger precursor proteins, and then transported to the nerve terminal where they are stored in secretory vesicles. When the neuron is stimulated, the vesicles fuse with the cell membrane and release their contents into the extracellular space.
Neuropeptides can act as neurotransmitters or neuromodulators, depending on their target receptors and the duration of their effects. They play important roles in a variety of physiological processes, including pain perception, appetite regulation, stress response, and social behavior. Some neuropeptides also have hormonal functions, such as oxytocin and vasopressin, which are produced in the hypothalamus and released into the bloodstream to regulate reproductive and cardiovascular function, respectively.
There are hundreds of different neuropeptides that have been identified in the nervous system, and many of them have multiple functions and interact with other signaling molecules to modulate neural activity. Dysregulation of neuropeptide systems has been implicated in various neurological and psychiatric disorders, such as chronic pain, addiction, depression, and anxiety.
Calcitonin gene-related peptide (CGRP) is a neurotransmitter and vasodilator peptide that is widely distributed in the nervous system. It is encoded by the calcitonin gene, which also encodes calcitonin and catestatin. CGRP is produced and released by sensory nerves and plays important roles in pain transmission, modulation of inflammation, and regulation of blood flow.
CGRP exists as two forms, α-CGRP and β-CGRP, which differ slightly in their amino acid sequences but have similar biological activities. α-CGRP is found primarily in the central and peripheral nervous systems, while β-CGRP is expressed mainly in the gastrointestinal tract.
CGRP exerts its effects by binding to specific G protein-coupled receptors, which are widely distributed in various tissues, including blood vessels, smooth muscles, and sensory neurons. Activation of CGRP receptors leads to increased intracellular cyclic AMP levels, activation of protein kinase A, and subsequent relaxation of vascular smooth muscle, resulting in vasodilation.
CGRP has been implicated in several clinical conditions, including migraine, cluster headache, and inflammatory pain. Inhibition of CGRP signaling has emerged as a promising therapeutic strategy for the treatment of these disorders.
Smooth muscle, also known as involuntary muscle, is a type of muscle that is controlled by the autonomic nervous system and functions without conscious effort. These muscles are found in the walls of hollow organs such as the stomach, intestines, bladder, and blood vessels, as well as in the eyes, skin, and other areas of the body.
Smooth muscle fibers are shorter and narrower than skeletal muscle fibers and do not have striations or sarcomeres, which give skeletal muscle its striped appearance. Smooth muscle is controlled by the autonomic nervous system through the release of neurotransmitters such as acetylcholine and norepinephrine, which bind to receptors on the smooth muscle cells and cause them to contract or relax.
Smooth muscle plays an important role in many physiological processes, including digestion, circulation, respiration, and elimination. It can also contribute to various medical conditions, such as hypertension, gastrointestinal disorders, and genitourinary dysfunction, when it becomes overactive or underactive.
Bronchoconstriction is a medical term that refers to the narrowing of the airways in the lungs (the bronchi and bronchioles) due to the contraction of the smooth muscles surrounding them. This constriction can cause difficulty breathing, wheezing, coughing, and shortness of breath, which are common symptoms of asthma and other respiratory conditions.
Bronchoconstriction can be triggered by a variety of factors, including allergens, irritants, cold air, exercise, and emotional stress. In some cases, it may also be caused by certain medications, such as beta-blockers or nonsteroidal anti-inflammatory drugs (NSAIDs). Treatment for bronchoconstriction typically involves the use of bronchodilators, which are medications that help to relax the smooth muscles around the airways and widen them, making it easier to breathe.
A peptide fragment is a short chain of amino acids that is derived from a larger peptide or protein through various biological or chemical processes. These fragments can result from the natural breakdown of proteins in the body during regular physiological processes, such as digestion, or they can be produced experimentally in a laboratory setting for research or therapeutic purposes.
Peptide fragments are often used in research to map the structure and function of larger peptides and proteins, as well as to study their interactions with other molecules. In some cases, peptide fragments may also have biological activity of their own and can be developed into drugs or diagnostic tools. For example, certain peptide fragments derived from hormones or neurotransmitters may bind to receptors in the body and mimic or block the effects of the full-length molecule.
The trachea, also known as the windpipe, is a tube-like structure in the respiratory system that connects the larynx (voice box) to the bronchi (the two branches leading to each lung). It is composed of several incomplete rings of cartilage and smooth muscle, which provide support and flexibility. The trachea plays a crucial role in directing incoming air to the lungs during inspiration and outgoing air to the larynx during expiration.
Muscle contraction is the physiological process in which muscle fibers shorten and generate force, leading to movement or stability of a body part. This process involves the sliding filament theory where thick and thin filaments within the sarcomeres (the functional units of muscles) slide past each other, facilitated by the interaction between myosin heads and actin filaments. The energy required for this action is provided by the hydrolysis of adenosine triphosphate (ATP). Muscle contractions can be voluntary or involuntary, and they play a crucial role in various bodily functions such as locomotion, circulation, respiration, and posture maintenance.
Thiorphan is not a medical condition or disease, but rather a synthetic medication. It is a potent inhibitor of membrane-bound metalloendopeptidases, also known as neprilysin enzymes. These enzymes are responsible for breaking down certain peptides in the body, including some hormones and neurotransmitters.
Thiorphan has been used in research to study the role of these enzymes in various physiological processes. It is also being investigated as a potential therapeutic agent for conditions such as hypertension, heart failure, and Alzheimer's disease. However, it is not currently approved for clinical use in humans.
Therefore, there is no medical definition of 'Thiorphan' as a condition or disease.
Benzamides are a class of organic compounds that consist of a benzene ring (a aromatic hydrocarbon) attached to an amide functional group. The amide group can be bound to various substituents, leading to a variety of benzamide derivatives with different biological activities.
In a medical context, some benzamides have been developed as drugs for the treatment of various conditions. For example, danzol (a benzamide derivative) is used as a hormonal therapy for endometriosis and breast cancer. Additionally, other benzamides such as sulpiride and amisulpride are used as antipsychotic medications for the treatment of schizophrenia and related disorders.
It's important to note that while some benzamides have therapeutic uses, others may be toxic or have adverse effects, so they should only be used under the supervision of a medical professional.
Atropine is an anticholinergic drug that blocks the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. It is derived from the belladonna alkaloids, which are found in plants such as deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), and Duboisia spp.
In clinical medicine, atropine is used to reduce secretions, increase heart rate, and dilate the pupils. It is often used before surgery to dry up secretions in the mouth, throat, and lungs, and to reduce salivation during the procedure. Atropine is also used to treat certain types of nerve agent and pesticide poisoning, as well as to manage bradycardia (slow heart rate) and hypotension (low blood pressure) caused by beta-blockers or calcium channel blockers.
Atropine can have several side effects, including dry mouth, blurred vision, dizziness, confusion, and difficulty urinating. In high doses, it can cause delirium, hallucinations, and seizures. Atropine should be used with caution in patients with glaucoma, prostatic hypertrophy, or other conditions that may be exacerbated by its anticholinergic effects.
The ileum is the third and final segment of the small intestine, located between the jejunum and the cecum (the beginning of the large intestine). It plays a crucial role in nutrient absorption, particularly for vitamin B12 and bile salts. The ileum is characterized by its thin, lined walls and the presence of Peyer's patches, which are part of the immune system and help surveil for pathogens.
Neurogenic inflammation is a type of inflammatory response that is initiated by the nervous system and involves the release of neurotransmitters and neuropeptides, such as substance P, calcitonin gene-related peptide (CGRP), and nitric oxide. These substances cause vasodilation, increased vascular permeability, and recruitment of immune cells to the site of injury or damage.
Neurogenic inflammation can occur in response to a variety of stimuli, including tissue injury, infection, and chemical or physical irritants. It is thought to play a role in the development and maintenance of various clinical conditions, such as migraine headaches, neuropathic pain, asthma, and allergies.
In contrast to classical inflammation, which is mediated by the immune system, neurogenic inflammation is primarily driven by the nervous system and can occur independently of traditional immune responses. However, the two processes often interact and amplify each other, leading to a more robust and prolonged inflammatory response.
Neurons, also known as nerve cells or neurocytes, are specialized cells that constitute the basic unit of the nervous system. They are responsible for receiving, processing, and transmitting information and signals within the body. Neurons have three main parts: the dendrites, the cell body (soma), and the axon. The dendrites receive signals from other neurons or sensory receptors, while the axon transmits these signals to other neurons, muscles, or glands. The junction between two neurons is called a synapse, where neurotransmitters are released to transmit the signal across the gap (synaptic cleft) to the next neuron. Neurons vary in size, shape, and structure depending on their function and location within the nervous system.
Neprilysin (NEP), also known as membrane metallo-endopeptidase or CD10, is a type II transmembrane glycoprotein that functions as a zinc-dependent metalloprotease. It is widely expressed in various tissues, including the kidney, brain, heart, and vasculature. Neprilysin plays a crucial role in the breakdown and regulation of several endogenous bioactive peptides, such as natriuretic peptides, bradykinin, substance P, and angiotensin II. By degrading these peptides, neprilysin helps maintain cardiovascular homeostasis, modulate inflammation, and regulate neurotransmission. In the context of heart failure, neprilysin inhibitors have been developed to increase natriuretic peptide levels, promoting diuresis and vasodilation, ultimately improving cardiac function.
A dose-response relationship in the context of drugs refers to the changes in the effects or symptoms that occur as the dose of a drug is increased or decreased. Generally, as the dose of a drug is increased, the severity or intensity of its effects also increases. Conversely, as the dose is decreased, the effects of the drug become less severe or may disappear altogether.
The dose-response relationship is an important concept in pharmacology and toxicology because it helps to establish the safe and effective dosage range for a drug. By understanding how changes in the dose of a drug affect its therapeutic and adverse effects, healthcare providers can optimize treatment plans for their patients while minimizing the risk of harm.
The dose-response relationship is typically depicted as a curve that shows the relationship between the dose of a drug and its effect. The shape of the curve may vary depending on the drug and the specific effect being measured. Some drugs may have a steep dose-response curve, meaning that small changes in the dose can result in large differences in the effect. Other drugs may have a more gradual dose-response curve, where larger changes in the dose are needed to produce significant effects.
In addition to helping establish safe and effective dosages, the dose-response relationship is also used to evaluate the potential therapeutic benefits and risks of new drugs during clinical trials. By systematically testing different doses of a drug in controlled studies, researchers can identify the optimal dosage range for the drug and assess its safety and efficacy.
Afferent neurons, also known as sensory neurons, are a type of nerve cell that conducts impulses or signals from peripheral receptors towards the central nervous system (CNS), which includes the brain and spinal cord. These neurons are responsible for transmitting sensory information such as touch, temperature, pain, sound, and light to the CNS for processing and interpretation. Afferent neurons have specialized receptor endings that detect changes in the environment and convert them into electrical signals, which are then transmitted to the CNS via synapses with other neurons. Once the signals reach the CNS, they are processed and integrated with other information to produce a response or reaction to the stimulus.
Gonadotropin-Releasing Hormone (GnRH), also known as Luteinizing Hormone-Releasing Hormone (LHRH), is a hormonal peptide consisting of 10 amino acids. It is produced and released by the hypothalamus, an area in the brain that links the nervous system to the endocrine system via the pituitary gland.
GnRH plays a crucial role in regulating reproduction and sexual development through its control of two gonadotropins: follicle-stimulating hormone (FSH) and luteinizing hormone (LH). These gonadotropins, in turn, stimulate the gonads (ovaries or testes) to produce sex steroids and eggs or sperm.
GnRH acts on the anterior pituitary gland by binding to its specific receptors, leading to the release of FSH and LH. The hypothalamic-pituitary-gonadal axis is under negative feedback control, meaning that when sex steroid levels are high, they inhibit the release of GnRH, which subsequently decreases FSH and LH secretion.
GnRH agonists and antagonists have clinical applications in various medical conditions, such as infertility treatments, precocious puberty, endometriosis, uterine fibroids, prostate cancer, and hormone-responsive breast cancer.
The spinal cord is a major part of the nervous system, extending from the brainstem and continuing down to the lower back. It is a slender, tubular bundle of nerve fibers (axons) and support cells (glial cells) that carries signals between the brain and the rest of the body. The spinal cord primarily serves as a conduit for motor information, which travels from the brain to the muscles, and sensory information, which travels from the body to the brain. It also contains neurons that can independently process and respond to information within the spinal cord without direct input from the brain.
The spinal cord is protected by the bony vertebral column (spine) and is divided into 31 segments: 8 cervical, 12 thoracic, 5 lumbar, 5 sacral, and 1 coccygeal. Each segment corresponds to a specific region of the body and gives rise to pairs of spinal nerves that exit through the intervertebral foramina at each level.
The spinal cord is responsible for several vital functions, including:
1. Reflexes: Simple reflex actions, such as the withdrawal reflex when touching a hot surface, are mediated by the spinal cord without involving the brain.
2. Muscle control: The spinal cord carries motor signals from the brain to the muscles, enabling voluntary movement and muscle tone regulation.
3. Sensory perception: The spinal cord transmits sensory information, such as touch, temperature, pain, and vibration, from the body to the brain for processing and awareness.
4. Autonomic functions: The sympathetic and parasympathetic divisions of the autonomic nervous system originate in the thoracolumbar and sacral regions of the spinal cord, respectively, controlling involuntary physiological responses like heart rate, blood pressure, digestion, and respiration.
Damage to the spinal cord can result in various degrees of paralysis or loss of sensation below the level of injury, depending on the severity and location of the damage.
Electric stimulation, also known as electrical nerve stimulation or neuromuscular electrical stimulation, is a therapeutic treatment that uses low-voltage electrical currents to stimulate nerves and muscles. It is often used to help manage pain, promote healing, and improve muscle strength and mobility. The electrical impulses can be delivered through electrodes placed on the skin or directly implanted into the body.
In a medical context, electric stimulation may be used for various purposes such as:
1. Pain management: Electric stimulation can help to block pain signals from reaching the brain and promote the release of endorphins, which are natural painkillers produced by the body.
2. Muscle rehabilitation: Electric stimulation can help to strengthen muscles that have become weak due to injury, illness, or surgery. It can also help to prevent muscle atrophy and improve range of motion.
3. Wound healing: Electric stimulation can promote tissue growth and help to speed up the healing process in wounds, ulcers, and other types of injuries.
4. Urinary incontinence: Electric stimulation can be used to strengthen the muscles that control urination and reduce symptoms of urinary incontinence.
5. Migraine prevention: Electric stimulation can be used as a preventive treatment for migraines by applying electrical impulses to specific nerves in the head and neck.
It is important to note that electric stimulation should only be administered under the guidance of a qualified healthcare professional, as improper use can cause harm or discomfort.
Biphenyl compounds, also known as diphenyls, are a class of organic compounds consisting of two benzene rings linked by a single carbon-carbon bond. The chemical structure of biphenyl compounds can be represented as C6H5-C6H5. These compounds are widely used in the industrial sector, including as intermediates in the synthesis of other chemicals, as solvents, and in the production of plastics and dyes. Some biphenyl compounds also have biological activity and can be found in natural products. For example, some plant-derived compounds that belong to this class have been shown to have anti-inflammatory, antioxidant, and anticancer properties.
Sprague-Dawley rats are a strain of albino laboratory rats that are widely used in scientific research. They were first developed by researchers H.H. Sprague and R.C. Dawley in the early 20th century, and have since become one of the most commonly used rat strains in biomedical research due to their relatively large size, ease of handling, and consistent genetic background.
Sprague-Dawley rats are outbred, which means that they are genetically diverse and do not suffer from the same limitations as inbred strains, which can have reduced fertility and increased susceptibility to certain diseases. They are also characterized by their docile nature and low levels of aggression, making them easier to handle and study than some other rat strains.
These rats are used in a wide variety of research areas, including toxicology, pharmacology, nutrition, cancer, and behavioral studies. Because they are genetically diverse, Sprague-Dawley rats can be used to model a range of human diseases and conditions, making them an important tool in the development of new drugs and therapies.
Cyclic peptides are a type of peptides in which the N-terminus and C-terminus of the peptide chain are linked to form a circular structure. This is in contrast to linear peptides, which have a straight peptide backbone with a free N-terminus and C-terminus. The cyclization of peptides can occur through various mechanisms, including the formation of an amide bond between the N-terminal amino group and the C-terminal carboxylic acid group (head-to-tail cyclization), or through the formation of a bond between side chain functional groups.
Cyclic peptides have unique structural and chemical properties that make them valuable in medical and therapeutic applications. For example, they are more resistant to degradation by enzymes compared to linear peptides, which can increase their stability and half-life in the body. Additionally, the cyclic structure allows for greater conformational rigidity, which can enhance their binding affinity and specificity to target molecules.
Cyclic peptides have been explored as potential therapeutics for a variety of diseases, including cancer, infectious diseases, and neurological disorders. They have also been used as tools in basic research to study protein-protein interactions and cell signaling pathways.
A radioligand assay is a type of in vitro binding assay used in molecular biology and pharmacology to measure the affinity and quantity of a ligand (such as a drug or hormone) to its specific receptor. In this technique, a small amount of a radioactively labeled ligand, also known as a radioligand, is introduced to a sample containing the receptor of interest. The radioligand binds competitively with other unlabeled ligands present in the sample for the same binding site on the receptor. After allowing sufficient time for binding, the reaction is stopped, and the amount of bound radioligand is measured using a technique such as scintillation counting. The data obtained from this assay can be used to determine the dissociation constant (Kd) and maximum binding capacity (Bmax) of the receptor-ligand interaction, which are important parameters in understanding the pharmacological properties of drugs and other ligands.
Bethanechol compounds are a type of cholinergic agent used in medical treatment. They are parasympathomimetic drugs, which means they mimic the actions of the neurotransmitter acetylcholine at muscarinic receptors. Specifically, bethanechol compounds stimulate the muscarinic receptors in the smooth muscle of the bladder and gastrointestinal tract, increasing tone and promoting contractions.
Bethanechol is primarily used to treat urinary retention and associated symptoms, such as those that can occur after certain types of surgery or with conditions like spinal cord injury or multiple sclerosis. It works by helping the bladder muscle contract, which can promote urination.
It's important to note that bethanechol should be used with caution, as it can have various side effects, including sweating, increased salivation, flushed skin, and gastrointestinal symptoms like nausea, vomiting, or diarrhea. It may also interact with other medications, so it's crucial to discuss any potential risks with a healthcare provider before starting this treatment.
Posterior horn cells refer to the neurons located in the posterior (or dorsal) horn of the gray matter in the spinal cord. These cells are primarily responsible for receiving and processing sensory information from peripheral nerves, particularly related to touch, pressure, pain, and temperature. The axons of these cells form the ascending tracts that carry this information to the brain for further processing. It's worth noting that damage to posterior horn cells can result in various sensory deficits, such as those seen in certain neurological conditions.
The kidney pelvis, also known as the renal pelvis, is the funnel-shaped part of the upper end of the ureter in the kidney. It receives urine from the minor and major calyces, which are extensions of the renal collecting tubules, and then drains it into the ureter, which carries it to the bladder for storage and eventual elimination from the body. The kidney pelvis is lined with transitional epithelium, which is designed to stretch and accommodate changes in urine volume.
Bethanechol is a parasympathomimetic drug, which means it stimulates the parasympathetic nervous system. This system is responsible for regulating many automatic functions in the body, including digestion and urination. Bethanechol works by causing the smooth muscles of the bladder to contract, which can help to promote urination in people who have difficulty emptying their bladder completely due to certain medical conditions such as surgery, spinal cord injury, or multiple sclerosis.
The medical definition of 'Bethanechol' is:
A parasympathomimetic agent that stimulates the muscarinic receptors of the autonomic nervous system, causing contraction of smooth muscle and increased secretion of exocrine glands. It is used to treat urinary retention and associated symptoms, such as those caused by bladder-neck obstruction due to prostatic hypertrophy or neurogenic bladder dysfunction. Bethanechol may also be used to diagnose urinary tract obstruction and to test the integrity of the bladder's innervation.
"Wistar rats" are a strain of albino rats that are widely used in laboratory research. They were developed at the Wistar Institute in Philadelphia, USA, and were first introduced in 1906. Wistar rats are outbred, which means that they are genetically diverse and do not have a fixed set of genetic characteristics like inbred strains.
Wistar rats are commonly used as animal models in biomedical research because of their size, ease of handling, and relatively low cost. They are used in a wide range of research areas, including toxicology, pharmacology, nutrition, cancer, cardiovascular disease, and behavioral studies. Wistar rats are also used in safety testing of drugs, medical devices, and other products.
Wistar rats are typically larger than many other rat strains, with males weighing between 500-700 grams and females weighing between 250-350 grams. They have a lifespan of approximately 2-3 years. Wistar rats are also known for their docile and friendly nature, making them easy to handle and work with in the laboratory setting.
Protein precursors, also known as proproteins or prohormones, are inactive forms of proteins that undergo post-translational modification to become active. These modifications typically include cleavage of the precursor protein by specific enzymes, resulting in the release of the active protein. This process allows for the regulation and control of protein activity within the body. Protein precursors can be found in various biological processes, including the endocrine system where they serve as inactive hormones that can be converted into their active forms when needed.
Neurokinin A
Tachykinin receptor 2
Tachykinin peptides
Tachykinin receptor 1
Trefoil factor 2
Substance P
5-HT1A receptor
Pre-Bötzinger complex
Serlopitant
Tachykinin receptor 3
Ezlopitant
Elinzanetant
Tradipitant
Lanepitant
R-type calcium channel
Meclinertant
Vofopitant
TAC3
Gerardo Turcatti
L-733,060
Mir-500 microRNA precursor family
Preprotachykinin
Vomiting
Pavinetant
Burapitant
Rhodopsin-like receptors
NK1 receptor antagonist
Sean Ekins
Vestipitant
Follower neuron
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A neurokinin 3 receptor-selective agonist accelerates pulsatile luteinizing hormone secretion in lactating cattle†
Antagonist22
- This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A. Several selective ligands for NK2 are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant. (wikipedia.org)
- The rational discovery of a high affinity NK2 receptor antagonist is described utilizing a general strategy for peptoid design. (nih.gov)
- Further exploration of structure-affinity via conformationally restricted analogues and N- and C-terminus modifications gave a selective, nanomolar affinity NK2 receptor antagonist, (2,3di-CH3OPh)CH2OCO(S)Trp(S)alpha-MePheGlyNH2, PD 147714 (19) with an K(i) = 1.4 nM (hamster urinary bladder membranes and using [125I]-iodohistidyl-NKA (0.1 nM) as the radioligand). (nih.gov)
- The aim of the present study was to investigate the effects of the non‐peptide NK‐2 receptor antagonist, SR 48968 on the responses of dorsal horn neurons to iontophoretic application of the endogenous NK‐2 receptor ligand, neurokinin A, and on synaptically elicited responses in chloralose‐anaesthetized cats. (mcmaster.ca)
- CI-1021 ([(2-benzofuran)-CH 2 OCO]-( R )-α-MeTrp-( S )-NHCH(CH 3 )Ph) is a selective and competitive neurokinin-1 (NK 1 ) receptor antagonist. (aspetjournals.org)
- PD 156982, a NK 1 receptor antagonist with poor central nervous system penetration, failed to have any effect. (aspetjournals.org)
- Phase 2 Trial of a Neurokinin-1 Receptor Antagonist for the Treatment of Chronic Itch in Epidermolysis Bullosa Patients: A Randomized Clinical Trial. (stanford.edu)
- Veozah is the first nonhormonal neurokinin 3 (NK3) receptor antagonist approved to treat VMS due to menopause. (primetherapeutics.com)
- Pretreatment with CP-99994, a neurokinin type 1 receptor antagonist, partially abolished the O(3)-induced reactivity to cholinergic agonists and electrical field stimulation. (cdc.gov)
- Halothane displayed an initial peak within 2 min which was blocked by atropine but not by the neurokinin 1 (NK1) receptor antagonist CP-99. (lu.se)
- EMEND ® is a substance P/neurokinin 1 (NK 1 ) receptor antagonist. (nih.gov)
- Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. (adooq.cn)
- Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. (adooq.cn)
- Maropitant is a neurokinin (NK1) receptor antagonist. (adooq.cn)
- Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. (adooq.cn)
- Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. (adooq.cn)
- The percentage of chemotherapy administration involving patients prescribed prophylactic antiemetic drugs, namely, a neurokinin 1 receptor antagonist, serotonin receptor antagonist, and/or dexamethasone, was calculated. (urotoday.com)
- An azido derivative of [3H2](2S, 3S)-cis-2-(diphenylmethyl)-N-((2-methoxyphenyl) methyl)-1-azabicyclo[2.2.2]octon-3-amine (CP-96,345), a potent nonpeptide antagonist of the substance P (SP) (neurokinin-1) receptor, was synthesized and shown to have an affinity for the human SP receptor similar to that of the parent compound, CP-96,345. (shengsci.com)
- Fezolinetant is an investigational nonhormonal selective neurokinin 3 (NK3) receptor antagonist. (salesandmarketingnetwork.com)
- We pooled data from two prospective observational studies in Japan and one phase III clinical trial to assess whether delayed CINV could be controlled with a combination of three antiemetics adding a neurokinin-1 receptor antagonist and identified individual risk factors, using an inverse probability treatment-weighted analysis. (biomedcentral.com)
- Cisplatin-based highly emetogenic chemotherapy (HEC) regimens, which are key treatments for some of malignant tumors, were conventionally administered after an antiemetic premedication with dexamethasone plus a 5-hydroxytryptamine 3 receptor antagonist (5-HT 3 RA) such as ondansetron or granisetron. (medscape.com)
- Aprepitant, a neurokinin-1 (NK-1) receptor antagonist, and palonosetron, a second-generation 5-HT 3 RA, are two recently introduced antiemetic agents expected to improve control of CINV. (medscape.com)
Antagonists9
- Tachykinin receptor antagonists inhibit hyperpnea-induced bronchoconstriction in guinea pigs. (mcmaster.ca)
- However, responses of wide dynamic range neurons to neurokinin A were totally blocked by i.v. administration (0.5 mg/kg) of the NK‐1 receptor antagonists CP‐96,345 ( n = 7) and CP‐99,994 ( n = 5) but not by CP‐96,344 ( n = 4), the inactive enantiomer of CP‐96,345. (mcmaster.ca)
- Two chemically unrelated NK 1 receptor antagonists, CP-99,994 (3-30 mg/kg) and SR 140333 (1-100 mg/kg), also dose dependently blocked the late phase, with respective MEDs of 3 and 10 mg/kg. (aspetjournals.org)
- It is suggested that NK 1 receptor antagonists possess a superior side effect profile to carbamazepine and morphine and may have a therapeutic use for the treatment of inflammatory and neuropathic pain. (aspetjournals.org)
- Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. (rndsystems.com)
- Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy. (rndsystems.com)
- Of these, patients who received 24 373 administrations of chemotherapy with a low emetic risk (47.8%) and 633 administrations of chemotherapy with a minimal emetic risk (2.8%) were prescribed serotonin receptor antagonists and dexamethasone. (urotoday.com)
- e.g., palonosetron) and neurokinin-1 receptor antagonists (NK1RAs). (biomedcentral.com)
- There has been no phase III study of comparing the efficacy of first- and second-generation 5-HT 3 receptor antagonists in the triplet regimen with dexamethasone and aprepitant for preventing chemotherapy-induced nausea and vomiting after highly emetogenic chemotherapy (HEC). (medscape.com)
NK1R1
- The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). (wikidoc.org)
Ligand3
- The ligand binding site of the neurokinin 2 receptor. (wikipedia.org)
- This action is mediated through conformational changes in the receptor following ligand binding. (sdbonline.org)
- Endogenous ligand for NK 3 receptor. (enzolifesciences.com)
Substance P neurokinin1
- The substance P neurokinin 1 receptor (NK 1 R) regulates motility, secretion, inflammation and pain in the intestine. (nyu.edu)
Transducing extracellular1
- G protein-coupled receptors are the largest superfamily of cell surface receptors in the Metazoa and play critical roles in transducing extracellular signals into intracellular responses. (sdbonline.org)
Selective3
- The present study aimed to clarify the role of NKB-neurokinin 3 receptor (NK3R) signaling in the pulsatile pattern of GnRH/gonadotropin secretion in postpartum lactating cattle.We examined the effects of the administration of an NK3R-selective agonist, senktide, on gonadotropin secretion in lactating cattle. (bioone.org)
- Thus, based on both their receptor potency and pharmacological potency, these peptides are potent and selective tachykinin analogs. (aspetjournals.org)
- The contraction of guinea pig ileum induced by one of the conformationally constrained analogs is attenuated by pretreatment of the tissue with atropine (2 microM), while that induced by substance P methyl ester, a selective inhibitor of 125I-labeled Bolton Hunter-conjugated substance P binding, is not. (aspetjournals.org)
Serotonin2
- MCs can secrete nociceptor sensitizing and activating agents, such as serotonin, prostaglandins, histamine, and proteolytic enzymes that can also activate the pain-mediating transient receptor potential vanilloid channels. (frontiersin.org)
- Five neurotransmitter receptors are of primary importance in PONV: acetylcholine, dopamine-2, histamine-1, serotonin-3, and neurokinin-1. (ispub.com)
Tachykinin receptors1
- Thus, the constrained analog has a higher affinity for the tachykinin receptors in the guinea pig myenteric plexus which are responsible for acetylcholine release than for the tachykinin receptors present on the smooth muscle cells. (aspetjournals.org)
Neurons14
- The effect of iontophoretic application of neurokinin A was tested on 51 dorsal horn neurons. (mcmaster.ca)
- Neurokinin A induced a slow, prolonged excitation of 25 of the wide dynamic range neurons. (mcmaster.ca)
- SR 48968 (50 pg to 1.0 mg/kg, i.v.) did not affect the on‐going basal activity ( n = 8) or the slow excitation induced by neurokinin A in any of the nine wide dynamic range neurons tested. (mcmaster.ca)
- To eliminate the possibility that systemically administered SR 48968 may not be reaching central sites, SR 48968 was also applied iontophoretically (70-120 nA) to five neurons and tested against excitatory responses to iontophoretically applied neurokinin A. The on‐going activity of these cells were unaffected by SR 48968. (mcmaster.ca)
- SR 48968 also had no effect on the excitatory responses of seven neurons to iontophoretic application of the NK‐1 receptor agonist, substance P indicating that substance P actions are not mediated via NK‐2 receptors and that SR 48968 did not react with NK‐1 receptors. (mcmaster.ca)
- Responses of the neurons to non‐noxious (hair) stimulation ( n = 10), noxious mechanical ( n = 5) and noxious thermal ( n = 8) stimulation of the receptive field were also unaffected by SR 48968, suggesting a lack of participation of NK‐2 receptors in these responses. (mcmaster.ca)
- These data suggest that neurokinin A, like substance P may be acting via NK‐1, rather than NK‐2 receptors, to produce excitation of wide dynamic range neurons in the dorsal horn of the cat spinal cord. (mcmaster.ca)
- These neurons appear to be located more superficially and are more sensitive to pruritogenic substances than pain receptors. (medscape.com)
- Here we report that TcdB induces neurogenic inflammation by targeting gut-innervating afferent neurons and pericytes through receptors, including the Frizzled receptors (FZD1, FZD2 and FZD7) in neurons and chondroitin sulfate proteoglycan 4 (CSPG4) in pericytes. (nature.com)
- Targeted delivery of the TcdB enzymatic domain, through fusion with a detoxified diphtheria toxin, into peptidergic sensory neurons that express exogeneous diphtheria toxin receptor (an approach we term toxogenetics) is sufficient to induce neurogenic inflammation and recapitulates major colonic histopathology associated with CDI. (nature.com)
- Fig. 2: TcdB targets neurons through FZD1/2/7 and pericytes through CSPG4. (nature.com)
- Neurokinin B (NKB) neurons in the arcuate nucleus of the hypothalamus are considered to play an essential role in generating the pulsatile mode of GnRH/luteinizing hormone (LH) secretion. (bioone.org)
- Its receptor - the neurokinin type 1 - is distributed over cytoplasmic membranes of many cell types (neurons, glia, endothelia of capillaries and lymphatics, fibroblasts, stem cells, white blood cells) in many tissues and organs. (wikidoc.org)
- 2006 ). The majority of CB1 receptors is localized on striatal glutamatergic and gamma-aminobutyric acid (GABA)-ergic interneurons and projection neurons. (springer.com)
Affinity2
- The results from this study indicated the primary importance of the Trp and Phe side-chain for binding and led to the observation that Z-Trp-PheNH2 (9a) is a micromolar affinity NK2 receptor dipeptide lead. (nih.gov)
- [ 5-7 ] Palonosetron has several advantageous features over first-generation 5-HT 3 RA, such as a longer plasma elimination half-life and a higher affinity for the 5-HT 3 receptor. (medscape.com)
Antibody1
- Find the TGF beta-2 antibody that fits your needs. (caslab.com)
Neurotransmitter1
- T-2 toxin mainly causes antifeedant reaction through four pathways: vagus nerve, gastrointestinal hormone, neurotransmitter and cytokine. (bvsalud.org)
Mediate2
- The responses to neurokinin A were also unaffected suggesting that neurokinin A did not mediate its effects via NK‐2 receptors. (mcmaster.ca)
- Increasing the therapeutic potential and reducing the side effects of U.S. Food and Drug Administration-approved glucagon-like peptide-1 receptor (GLP-1R) agonists used to treat obesity require complete characterization of the central mechanisms that mediate both the food intake-suppressive and illness-like effects of GLP-1R signaling. (bvsalud.org)
Stimulation1
- Stimulation of opioid mu receptors accentuates pruritus, while stimulation of kappa receptors and blockage of mu receptors suppress pruritus. (medscape.com)
GPCRs2
- G protein-coupled receptors (GPCRs) are a large family of proteins that regulate many processes in the body and are the target of one third of clinically used drugs. (sciencemission.com)
- [7] It belongs to the tachykinin receptor sub-family of GPCRs . (wikidoc.org)
Inhibitors3
- Inhibitors of IMP dehydrogenase stimulate the phosphorylation of the anti-human immunodeficiency virus nucleosides 2',3'-dideoxyadenosine and 2',3'-dideoxyinosine. (shengsci.com)
- Some glycosidic laurel compounds such as laurusides were proposed as inhibitors of important protein targets of SARS-CoV-2, which clearly recalls their potential as anti-COVID-19 drugs. (cnr.it)
- Hexapeptides containing phenylalanine, isoleucine, and valine identical with the carboxyl-terminal sequences of substance P, eledoisin, and neurokinin B, respectively, were nearly equipotent as inhibitors of 125I-labeled Bolton Hunter-conjugated eledoisin binding. (aspetjournals.org)
Acetylcholine1
- Additionally, leucine substitutions at this position caused similar signaling defects in the follicle-stimulating hormone receptor (FSHR), Galanin receptor (GALR1), AKH receptor (AKHR), corazonin receptor (CRZR), and muscarinic acetylcholine receptor (mACHR1) . (sdbonline.org)
Protein-coupled receptor1
- Interestingly, a second antiserum that was generated against the third extracellular loop of the G protein-coupled receptor no longer immunoprecipitated the receptor when covalently labeled with [3H2]azido-CP-96,345. (shengsci.com)
Palonosetron1
- Patients with a malignant solid tumor who would receive HEC containing 50 mg/m 2 or more cisplatin were randomly assigned to either palonosetron (0.75 mg) arm (Arm P) or granisetron (1 mg) arm (Arm G), on day 1, both arms with dexamethasone (12 mg on day 1 and 8 mg on days 2-4) and aprepitant (125 mg on day 1 and 80 mg on days 2-3). (medscape.com)
Tachykinins1
- This gene belongs to a family of genes that function as receptors for tachykinins. (wikipedia.org)
Mice7
- Conversely, mice lacking SP, CGRP or the SP receptor (neurokinin 1 receptor) show reduced pathology in both models of caecal TcdB injection and CDI. (nature.com)
- Studying NK1 receptors in the lab has the benefit of clinically available drugs that target the receptor, but also comes with challenges, as there are large differences between the NK1 receptor in mice and humans. (sciencemission.com)
- To overcome this, the researchers genetically modified mice to express the human NK1 receptor. (sciencemission.com)
- In another experiment, the researchers studied mice with a different type of NK1 receptor on the outer membrane of the cell, rather than inside. (sciencemission.com)
- These mice were more resistant to pain than those with human NK1 receptors inside the cell, illustrating the importance of endosomes in signaling pain and the need for treatments that can penetrate cells. (sciencemission.com)
- Our polyclonal, recombinant polyclonal and monoclonal TGF beta-2 antibodies are developed in rabbits and mice. (caslab.com)
- The consumption of T-2 toxin can cause anorexic response in mice, rats, rabbits, and other animals. (bvsalud.org)
Responses1
- The neuropeptide Leucokinin (Lk) and its receptor ( Lkr ) are essential for the reduction of responses to noxious heat. (sdbonline.org)
Agonist1
- C-terminal truncation of the neurokinin-2 receptor causes enhanced and sustained agonist-induced signaling. (wikipedia.org)
Neuropeptide substance1
- This is a receptor for the tachykinin neuropeptide substance K (neurokinin A). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. (idrblab.net)
Efficacy4
- MydCombi's application is supported by data from two Phase 3 studies, MIST-1 and MIST-2 that evaluated the efficacy and safety of MydCombi. (primetherapeutics.com)
- The approval is based on the three Phase 3 clinical trials, SKYLIGHT 1 and SKLYLIGHT 2 that demonstrated safety and efficacy, while SKYLIGHT 4 was a safety study to characterize the long-term safety profile. (primetherapeutics.com)
- Results from the SKYLIGHT 1 and SKYLIGHT 2 pivotal trials characterize the efficacy and safety of fezolinetant for the treatment of moderate to severe VMS associated with menopause. (salesandmarketingnetwork.com)
- Fezolinetant works by blocking neurokinin B (NKB) binding on the kisspeptin/neurokinin/dynorphin (KNDy) neuron to moderate neuronal activity in the thermoregulatory center of the brain (the hypothalamus) to reduce the frequency and severity of moderate to severe VMS associated with menopause.7,8,9 The safety and efficacy of fezolinetant are under investigation and have not been established. (salesandmarketingnetwork.com)
Molecular4
- The molecular underpinnings common to and connecting these disorders are not known, but may include shared genetic risk factors ( 1 , 8 ), regulation of brain cations ( 9 , 10 ), or common receptor signaling events that activate pain ( 11 ), inflammation ( 12 ), or oxidative ( 13 ) pathways. (frontiersin.org)
- When Chinese hamster ovary cells expressing the human SP receptor were photolabeled with this compound and analyzed with the use of sodium dodecyl sulfate-polyacrylamide gel electrophoresis and fluorography, several radioactive bands were observed, including a major band centered at molecular mass 80 kDa, the expected value for the SP receptor expressed in Chinese hamster ovary cells. (shengsci.com)
- Thus, we performed molecular dynamic (MD) simulations of laurusides-SARS-CoV-2 protease complexes to deepen the knowledge on the stability of the interaction and compare the effects of the targeting among the two genomic variants. (cnr.it)
- In this review, the basic information of T-2 toxin, appetite regulation mechanism and the molecular mechanism of T-2 toxin-induced anorectic response in animals are presented and discussed. (bvsalud.org)
Cannabinoid1
- antagonism or inverse agonism at the cannabinoid CB1 receptor. (bvsalud.org)
Isoform1
- Latent TGF beta 2 is the predominant isoform found in bodily fluids such as amniotic fluid, breast milk, and the aqueous and vitreous humor of the eye. (caslab.com)
Colonic1
- Functional subtyping of neurokinin receptors on canine proximal colonic mucosa. (mcmaster.ca)
Inflammation2
- In the mouse model that mimics atopic dermatitis in humans, the histamine (H4) receptor mediates both TH-2 inflammation and pruritus. (medscape.com)
- Unique among biological processes, SP release (and expression of its NK1 Receptor (through autocrine, paracrine, and endocrine-like processes)) may not naturally subside in diseases marked by chronic inflammation (including cancer). (wikidoc.org)
Biological Activity1
- TGF beta 1, TGF beta 2, and TGF beta 1.2 appear to have equivalent biological activity, although there appear to be differences in binding to certain types of receptors. (caslab.com)
Contraction3
- Receptors in the posterior pharynx are then activated to initiate the involuntary phase of deglutition, which involves carefully sequenced contraction of numerous head and neck muscles. (nature.com)
- Endothelium-dependent contraction in intrapulmonary arteries: mediation by endothelial NK 1 receptors and TXA 2 . (rndsystems.com)
- These analogs stimulate guinea pig ileum contraction (ED50 1-16 nM) and stimulate rat vas deferens contraction (ED50 2-4 microM). (aspetjournals.org)
Chemotherapy3
- Several FDA-approved drugs that target the NK1 receptor are used to prevent nausea and vomiting associated with chemotherapy or surgery. (sciencemission.com)
- Administer EMEND 1 hour prior to chemotherapy on Days 1, 2, and 3. (nih.gov)
- If no chemotherapy is given on Days 2 and 3, administer EMEND in morning. (nih.gov)
Interneurons1
- The neurokinin-1 receptor is expressed with gastrin-releasing peptide receptor in spinal interneurons and modulates itch. (rndsystems.com)
TACR21
- Substance-K receptor is a protein that in humans is encoded by the TACR2 gene. (wikipedia.org)
Gene2
- [1] [2] Substance P and its closely related neurokinin A (NKA) are produced from a polyprotein precursor after differential splicing of the preprotachykinin A gene . (wikidoc.org)
- Small Indels in the Androgen Receptor Gene: Phenotype Implications and Mechanisms of Mutagenesis. (medscape.com)
Activate1
- Some of the receptors are cation channels, which can directly depolarize the nociceptor upon activation, while other receptors activate second messenger systems to change neuronal excitability by changing expression of, or modifying the function of, other cation channels. (frontiersin.org)
19941
- 1994 Feb;2(2):101-13. (nih.gov)
Pharmacology1
- In this review, the pharmacology of central SP and its receptors are discussed, together with the exploration of the prospects and implications for future treatments of depression. (biopsychiatry.com)
Cells4
- One reason why drugs targeting the NK1 receptor may not have been effective against pain is that most drugs block receptors at the surface of cells. (sciencemission.com)
- These changes allowed the modified netupitant to readily penetrate cells to reach the endosome and block signaling of the NK1 receptor in endosomes with a much more prolonged effect in cells. (sciencemission.com)
- Although we focused on the neurokinin-1 receptor, our findings are likely applicable to many G-protein coupled receptors because many of them show sustained signaling within cells, and therefore require drugs that can enter cells and block the receptors in endosomes," said the senior author. (sciencemission.com)
- and virtually all mammalian cells possess a specific TGF receptor. (caslab.com)
Antibodies4
- Antibodies that detect TGF beta-2 can be used in several scientific applications, including Western Blot, immunohistochemistry (paraffin), ELISA, immunocytochemistry, and immunohistochemistry (frozen). (caslab.com)
- These antibodies target TGF beta-2 in human, mouse and rat samples. (caslab.com)
- These antibodies were checked by Knockdown to confirm specificity to TGF beta-2. (caslab.com)
- Choose from 1 of 15 TGF beta-2 antibodies, which have been validated in experiments with 10 publications and 36 images featured in our data gallery. (caslab.com)
Type7
- Effects of bariatric surgery on blood and vascular large extracellular vesicles according to type 2 diabetes status. (medscape.com)
- Approach to the Patient with Youth-Onset Type 2 Diabetes. (medscape.com)
- Insulin resistance is associated with the capillary permeability of thigh muscles in patients with type 2 diabetes. (medscape.com)
- Metabolites as Risk Factors for Diabetic Retinopathy in Patients with Type 2 Diabetes: a 12-year Follow-up Study. (medscape.com)
- Whole blood-based transcriptional risk score for nonobese type 2 diabetes predicts dynamic changes in glucose metabolism. (medscape.com)
- T-2 toxin is the most characteristic type A toxin in the trichothecene mycotoxins. (bvsalud.org)
- Caloric restriction that promotes weight loss is an effective strategy for treating non-alcoholic fatty liver disease and improving insulin sensitivity in people with type 2 diabetes1. (bvsalud.org)
Insulin1
- Insulin signaling through the insulin receptor increases linear growth through effects on bone and the GH-IGF-1 axis. (medscape.com)