Drugs that bind to and activate cholinergic receptors.
Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.
Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.
Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of ACETYLCHOLINE, and drugs that affect the survival of cholinergic neurons. The term cholinergic agents is sometimes still used in the narrower sense of MUSCARINIC AGONISTS, although most modern texts discourage that usage.
One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.
A non-hydrolyzed muscarinic agonist used as a research tool.
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
An alkaloid obtained from the betel nut (Areca catechu), fruit of a palm tree. It is an agonist at both muscarinic and nicotinic acetylcholine receptors. It is used in the form of various salts as a ganglionic stimulant, a parasympathomimetic, and a vermifuge, especially in veterinary practice. It has been used as a euphoriant in the Pacific Islands.
A toxic alkaloid found in Amanita muscaria (fly fungus) and other fungi of the Inocybe species. It is the first parasympathomimetic substance ever studied and causes profound parasympathetic activation that may end in convulsions and death. The specific antidote is atropine.
Compounds containing the PhCH= radical.
Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.
A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.
The tear-forming and tear-conducting system which includes the lacrimal glands, eyelid margins, conjunctival sac, and the tear drainage system.
Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.
A high-affinity muscarinic antagonist commonly used as a tool in animal and tissue studies.
A specific subtype of muscarinic receptor that has a high affinity for the drug PIRENZEPINE. It is found in the peripheral GANGLIA where it signals a variety of physiological functions such as GASTRIC ACID secretion and BRONCHOCONSTRICTION. This subtype of muscarinic receptor is also found in neuronal tissues including the CEREBRAL CORTEX and HIPPOCAMPUS where it mediates the process of MEMORY and LEARNING.
Compounds that contain the decamethylenebis(trimethyl)ammonium radical. These compounds frequently act as neuromuscular depolarizing agents.
Drugs that bind to and activate adrenergic receptors.
A selective nicotinic cholinergic agonist used as a research tool. DMPP activates nicotinic receptors in autonomic ganglia but has little effect at the neuromuscular junction.
A region extending from the PONS & MEDULLA OBLONGATA through the MESENCEPHALON, characterized by a diversity of neurons of various sizes and shapes, arranged in different aggregations and enmeshed in a complicated fiber network.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Drugs that bind to and activate dopamine receptors.
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
A group of compounds that are derivatives of beta-methylacetylcholine (methacholine).
A subclass of muscarinic receptor that mediates cholinergic-induced contraction in a variety of SMOOTH MUSCLES.
A form of phagocyte bactericidal dysfunction characterized by unusual oculocutaneous albinism, high incidence of lymphoreticular neoplasms, and recurrent pyogenic infections. In many cell types, abnormal lysosomes are present leading to defective pigment distribution and abnormal neutrophil functions. The disease is transmitted by autosomal recessive inheritance and a similar disorder occurs in the beige mouse, the Aleutian mink, and albino Hereford cattle.
The front part of the hindbrain (RHOMBENCEPHALON) that lies between the MEDULLA and the midbrain (MESENCEPHALON) ventral to the cerebellum. It is composed of two parts, the dorsal and the ventral. The pons serves as a relay station for neural pathways between the CEREBELLUM to the CEREBRUM.
The relationship between the dose of an administered drug and the response of the organism to the drug.
An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)
Agents affecting the function of, or mimicking the actions of, the autonomic nervous system and thereby having an effect on such processes as respiration, circulation, digestion, body temperature regulation, certain endocrine gland secretions, etc.
The craniosacral division of the autonomic nervous system. The cell bodies of the parasympathetic preganglionic fibers are in brain stem nuclei and in the sacral spinal cord. They synapse in cranial autonomic ganglia or in terminal ganglia near target organs. The parasympathetic nervous system generally acts to conserve resources and restore homeostasis, often with effects reciprocal to the sympathetic nervous system.
Nerve fibers liberating acetylcholine at the synapse after an impulse.
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in URINARY INCONTINENCE, in MOTION SICKNESS, as an antispasmodic, and as a mydriatic and cycloplegic.
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Use of electric potential or currents to elicit biological responses.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
A glandular epithelial cell or a unicellular gland. Goblet cells secrete MUCUS. They are scattered in the epithelial linings of many organs, especially the SMALL INTESTINE and the RESPIRATORY TRACT.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
A stage of sleep characterized by rapid movements of the eye and low voltage fast pattern EEG. It is usually associated with dreaming.
A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.
Neurotoxic proteins from the venom of the banded or Formosan krait (Bungarus multicinctus, an elapid snake). alpha-Bungarotoxin blocks nicotinic acetylcholine receptors and has been used to isolate and study them; beta- and gamma-bungarotoxins act presynaptically causing acetylcholine release and depletion. Both alpha and beta forms have been characterized, the alpha being similar to the large, long or Type II neurotoxins from other elapid venoms.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Sweat-producing structures that are embedded in the DERMIS. Each gland consists of a single tube, a coiled body, and a superficial duct.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
The discharge of saliva from the SALIVARY GLANDS that keeps the mouth tissues moist and aids in digestion.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
A group of amylolytic enzymes that cleave starch, glycogen, and related alpha-1,4-glucans. (Stedman, 25th ed) EC 3.2.1.-.
A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
The largest of the three pairs of SALIVARY GLANDS. They lie on the sides of the FACE immediately below and in front of the EAR.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
In about 250 species of electric fishes, modified muscle fibers forming disklike multinucleate plates arranged in stacks like batteries in series and embedded in a gelatinous matrix. A large torpedo ray may have half a million plates. Muscles in different parts of the body may be modified, i.e., the trunk and tail in the electric eel, the hyobranchial apparatus in the electric ray, and extrinsic eye muscles in the stargazers. Powerful electric organs emit pulses in brief bursts several times a second. They serve to stun prey and ward off predators. A large torpedo ray can produce of shock of more than 200 volts, capable of stunning a human. (Storer et al., General Zoology, 6th ed, p672)
A specific subtype of muscarinic receptor found in the lower BRAIN, the HEART and in SMOOTH MUSCLE-containing organs. Although present in smooth muscle the M2 muscarinic receptor appears not to be involved in contractile responses.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).
Therapeutic introduction of ions of soluble salts into tissues by means of electric current. In medical literature it is commonly used to indicate the process of increasing the penetration of drugs into surface tissues by the application of electric current. It has nothing to do with ION EXCHANGE; AIR IONIZATION nor PHONOPHORESIS, none of which requires current.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
A genus of the Torpedinidae family consisting of several species. Members of this family have powerful electric organs and are commonly called electric rays.
The rate dynamics in chemical or physical systems.
An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
Elements of limited time intervals, contributing to particular results or situations.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.
Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
Drugs that selectively bind to and activate beta-adrenergic receptors.
Condensed areas of cellular material that may be bounded by a membrane.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
The most common inhibitory neurotransmitter in the central nervous system.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
Refers to animals in the period of time just after birth.
Drugs that bind to and activate excitatory amino acid receptors.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
Compounds that bind to and activate PURINERGIC RECEPTORS.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.
A family of hexahydropyridines.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

Modulation of long-term synaptic depression in visual cortex by acetylcholine and norepinephrine. (1/652)

In a slice preparation of rat visual cortex, we discovered that paired-pulse stimulation (PPS) elicits a form of homosynaptic long-term depression (LTD) in the superficial layers when carbachol (CCh) or norepinephrine (NE) is applied concurrently. PPS by itself, or CCh and NE in the absence of synaptic stimulation, produced no lasting change. The LTD induced by PPS in the presence of NE or CCh is of comparable magnitude with that obtained with prolonged low-frequency stimulation (LFS) but requires far fewer stimulation pulses (40 vs 900). The cholinergic facilitation of LTD was blocked by atropine and pirenzepine, suggesting involvement of M1 receptors. The noradrenergic facilitation of LTD was blocked by urapidil and was mimicked by methoxamine, suggesting involvement of alpha1 receptors. beta receptor agonists and antagonists were without effect. Induction of LTD by PPS was inhibited by NMDA receptor blockers (completely in the case of NE; partially in the case of CCh), suggesting that one action of the modulators is to control the gain of NMDA receptor-dependent homosynaptic LTD in visual cortex. We propose that this is a mechanism by which cholinergic and noradrenergic inputs to the neocortex modulate naturally occurring receptive field plasticity.  (+info)

Metrifonate increases neuronal excitability in CA1 pyramidal neurons from both young and aging rabbit hippocampus. (2/652)

The effects of metrifonate, a second generation cholinesterase inhibitor, were examined on CA1 pyramidal neurons from hippocampal slices of young and aging rabbits using current-clamp, intracellular recording techniques. Bath perfusion of metrifonate (10-200 microM) dose-dependently decreased both postburst afterhyperpolarization (AHP) and spike frequency adaptation (accommodation) in neurons from young and aging rabbits (AHP: p < 0.002, young; p < 0.050, aging; accommodation: p < 0.024, young; p < 0.001, aging). These reductions were mediated by muscarinic cholinergic transmission, because they were blocked by addition of atropine (1 microM) to the perfusate. The effects of chronic metrifonate treatment (12 mg/kg for 3 weeks) on CA1 neurons of aging rabbits were also examined ex vivo. Neurons from aging rabbits chronically treated with metrifonate had significantly reduced spike frequency accommodation, compared with vehicle-treated rabbits. Chronic metrifonate treatment did not result in a desensitization to metrifonate ex vivo, because bath perfusion of metrifonate (50 microM) significantly decreased the AHP and accommodation in neurons from both chronically metrifonate- and vehicle-treated aging rabbits. We propose that the facilitating effect of chronic metrifonate treatment on acquisition of hippocampus-dependent tasks such as trace eyeblink conditioning by aging subjects may be caused by this increased excitability of CA1 pyramidal neurons.  (+info)

Influence of nitric oxide modulators on cholinergically stimulated hormone release from mouse islets. (3/652)

1. We have investigated, with a combined in vitro and in vivo approach, the influence on insulin and glucagon release stimulated by the cholinergic, muscarinic agonist carbachol of different NO modulators, i.e. the nitric oxide synthase (NOS) inhibitors NG-nitro-L-arginine methyl ester (L-NAME), NG-monomethyl-L-arginine (L-NMMA) and 7-nitroindazole as well as the intracellular NO donor hydroxylamine. 2. At basal glucose (7 mM) carbachol dose-dependently stimulated insulin release from isolated islets with a half-maximal response at approximately 1 microM of the agonist. In the presence of 5 mM L-NAME (a concentration that did not influence basal insulin release) the insulin response was markedly increased along the whole dose-response curve and the threshold for carbachol stimulation was significantly lowered. 3. Carbachol-stimulated islets displayed an increased insulin release and a suppressed glucagon release in the presence of L-NAME, L-NMMA or 7-nitroindazole. Significant suppression of glucagon release (except for L-NAME) was achieved at lower concentrations (approximately 0.1-0.5 mM) of the NOS inhibitors than the potentiation of insulin release (1.0-5.0 mM). The intracellular NO donor hydroxylamine dose-dependently inhibited carbachol-induced insulin release but stimulated glucagon release only at a low concentration (3 microM). 4. In islets depolarized with 30 mM K+ in the presence of the KATP channel opener diazoxide, NOS inhibition by 5 mM L-NAME still markedly potentiated carbachol-induced insulin release (although less so than in normal islets) and suppressed glucagon release. 5. In vivo pretreatment of mice with L-NAME was followed by a markedly increased insulin release and a reduced glucagon release in response to an i.v. injection of carbachol. 6. The data suggest that NO is a negative modulator of insulin release but a positive modulator of glucagon release induced by cholinergic muscarinic stimulation. These effects were also evident in K+ depolarized islets and thus NO might exert a major influence on islet hormone secretion independently of membrane depolarization events.  (+info)

Miniglucagon (glucagon 19-29), a potent and efficient inhibitor of secretagogue-induced insulin release through a Ca2+ pathway. (4/652)

Using the MIN6 B-cell line, we investigated the hypothesis that miniglucagon, the C-terminal () fragment processed from glucagon and present in pancreatic A cells, modulates insulin release, and we analyzed its cellular mode of action. We show that, at concentrations ranging from 0.01 to 1000 pM, miniglucagon dose-dependently (ID50 = 1 pM) inhibited by 80-100% the insulin release triggered by glucose, glucagon, glucagon-like peptide-1-(7-36) amide (tGLP-1), or glibenclamide, but not that induced by carbachol. Miniglucagon had no significant effects on cellular cAMP levels. The increase in 45Ca2+ uptake induced by depolarizing agents (glucose or extracellular K+), by glucagon, or by the Ca2+channel agonist Bay K-8644 was blocked by miniglucagon at the doses active on insulin release. Electrophysiological experiments indicated that miniglucagon induces membrane hyperpolarization, probably by opening potassium channels, which terminated glucose-induced electrical activity. Pretreatment with pertussis toxin abolished the effects of miniglucagon on insulin release. It is concluded that miniglucagon is a highly potent and efficient inhibitor of insulin release by closing, via hyperpolarization, voltage-dependent Ca2+ channels linked to a pathway involving a pertussis toxin-sensitive G protein.  (+info)

Cholinergic and GABAergic regulation of nitric oxide synthesis in the guinea pig ileum. (5/652)

Nitric oxide (NO) synthesis was examined in intact longitudinal muscle-myenteric plexus preparations of the guinea pig ileum by determining the formation of [3H]citrulline during incubation with [3H]arginine. Spontaneous [3H]citrulline production after 30 min was 80-90 dpm/mg, which constituted approximately 1% of the tissue radioactivity. Electrical stimulation (10 Hz) led to a threefold increase in [3H]citrulline formation. Removal of calcium from the medium or addition of NG-nitro-L-arginine strongly inhibited both spontaneous and electrically induced production of [3H]citrulline. TTX reduced the electrically induced but not spontaneous [3H]citrulline formation. The electrically induced formation of [3H]citrulline was diminished by (+)-tubocurarine and mecamylamine and enhanced by scopolamine, which suggests that endogenous ACh inhibits, via muscarinic receptors, and stimulates, via nicotinic receptors, the NO synthesis in the myenteric plexus. The GABAA receptor agonist muscimol and GABA also reduced the electrically evoked formation of [3H]citrulline, whereas baclofen was without effect. Bicuculline antagonized the inhibitory effect of GABA. It is concluded that nitrergic myenteric neurons are equipped with GABAA receptors, which mediate inhibition of NO synthesis.  (+info)

Purinergic and cholinergic agonists induce exocytosis from the same granule pool in HT29-Cl.16E monolayers. (6/652)

Several secretagogues induce mucin secretion in epithelial monolayers, as determined by measuring released granule contents. To assess whether different agonists act on the same granule pool, capacitance changes in intact monolayers of the goblet cell line HT29-Cl.16E were measured by a novel impedance method. Apical ATP (purinergic agonist) and basolateral carbachol (cholinergic agonist) induce rapid exocytosis with maximal capacitance changes within 3 min. The maximal levels of exocytosis that can be induced by optimal concentrations of either agonist are the same and produce a 30-40% increase in total monolayer capacitance. When ATP and carbachol are applied simultaneously, the magnitude of exocytosis is unchanged from the single-secretagogue level. The recovery of capacitance to baseline (endocytosis) is significantly faster after ATP stimulation than after carbachol stimulation. When ATP and carbachol are applied sequentially at doses that give maximal exocytosis, the magnitude of the capacitance increase produced by the second secretagogue is less than or equal to that of the capacitance decrease during the recovery period. Together, these data suggest that purinergic and cholinergic agonists act on the same granule pool.  (+info)

Immunolocalization of muscarinic and VIP receptor subtypes and their role in stimulating goblet cell secretion. (7/652)

PURPOSE: To determine the subtypes of cholinergic muscarinic receptors and receptors for vasoactive intestinal peptide (VIP) present in rat conjunctival goblet cells and whether cholinergic agonists and VIP stimulate goblet cell secretion. METHODS: Immunofluorescence studies were performed using antibodies against the m1, m2, and m3 muscarinic receptor subtypes and VIP receptors 1 and 2 (VIPR1 and VIPR2). The lectin Ulex europeus agglutinin I was used to measure glycoconjugate secretion, the index of secretion, from goblet cells in an enzyme-linked lectin assay. In this assay, pieces of conjunctiva were placed on filter paper and incubated for 15 to 120 minutes, with or without increasing concentrations of the cholinergic agonist carbachol or VIP. The muscarinic antagonist atropine and the muscarinic receptor-subtype-selective antagonists pirenzepine (M1), gallamine (M2), and 4-4-diphenylacetoxy-N-(2-chloroethyl)-piperidine hydrochloride (4-DAMP mustard; M3) were incubated with carbachol to determine specificity of receptor activation. RESULTS: Immunoreactivity to M2 and M3 receptors was found on goblet cell membranes subjacent to the secretory granules. Immunoreactivity to M1 receptor was not on goblet cells but was on the stratitfied squamous cells. Immunoreactivity to VIPR2 was found on goblet cells with a localization similar to that of the M2 and M3 receptors. VIPR1 was not found on goblet cells or on the stratified squamous cells. Carbachol and VIP induced a time- and concentration-dependent stimulation of glycoconjugate secretion. Carbachol, at 10(-4) M, induced a threefold increase in glycoconjugate secretion, which was completely inhibited by atropine (10(-5) M). Carbachol-induced secretion was inhibited 54% +/- 8% by pirenzepine (10(-5) M), 69% +/- 14% by gallamine (10(-5) M), and 72% +/- 11% by 4-DAMP mustard (10(-5) M). A twofold increase in glycoconjugate secretion was obtained with VIP at 10(-8) M. CONCLUSIONS: Cholinergic agonists, through M2 and/or M3 muscarinic receptors, and VIP, through VIPR2, regulate conjunctival goblet cell secretion, suggesting that goblet cell secretion in vivo is under the control of parasympathetic nerves.  (+info)

Modulation of inhibitory synaptic potentials in the piriform cortex. (8/652)

Modulation of inhibitory synaptic potentials in the piriform cortex. Intracellular recordings from pyramidal neurons in brain slice preparations of the piriform cortex were used to test results from a computational model about the effects of cholinergic agonists on inhibitory synaptic potentials induced by stimulation of afferent fibers in layer Ia and association/intrinsic fibers in layer Ib. A simple model of piriform cortex as an associative memory was used to analyze how suppression of inhibitory synaptic transmission influenced performance of the network. Levels of suppression of excitatory synaptic transmission were set at levels determined in previous experimental work. Levels of suppression of inhibitory synaptic transmission were then systematically varied within the model. This modeling work demonstrated that suppression of inhibitory synaptic transmission in layer Ib should be stronger than suppression of inhibitory synaptic transmission in layer Ia to keep activity levels high enough for effective storage. Experimental data showed that perfusion of the cholinergic agonist carbachol caused a significant suppression of inhibitory postsynaptic potentials (IPSPs) in the pyramidal neurons that were induced by stimulation of layer Ib, with a weaker effect on IPSPs induced by stimulation of layer Ia. As previously described, carbachol also selectively suppressed excitatory postsynaptic potentials (EPSPs) elicited by intrinsic but not afferent fiber stimulation. The decrease in amplitude of IPSPs induced by layer Ib stimulation did not appear to be directly related to the decrease in EPSP amplitude induced by layer Ib stimulation. The stimulation necessary to induce neuronal firing with layer Ia stimulation was reduced in the presence of carbachol, whereas that necessary to induce neuronal firing with layer Ib stimulation was increased, despite the depolarization of resting membrane potential. Thus physiological data on cholinergic modulation of inhibitory synaptic potentials in the piriform cortex is compatible with the functional requirements determined from computational models of piriform cortex associative memory function.  (+info)

The concentrations of acetylcholine and norepinephrine and acetylcholinesterase activity in the myocardium as well as chronotropic cardiac response to exogenous mediators administered in increasing...
Bicuculline, Carbachol, Cholinergic Agonist, Gaba, Hippocampal Formation, Hippocampus, Neuron, Neurons, Population, Rats, Separated, Urethane
Carbachol- యొక్క ఉపయోగాలు, మోతాదు, దుష్ప్రభావాలు, ప్రయోజనాలు, పరస్పర చర్యలు మరియు హెచ్చరికను కనుగొనండి
A reciprocal relationship exists between agrin and acetylcholine (ACh) in controlling acetylcholine receptor (AChR) clustering at the neuromuscular junction: Agrin promotes clustering, and ACh disperses clusters. Chen et al. provide insight into how these opposing signals may allow stabilization of AChR at the neuromuscular junction by differential activity of the calcium-activated proteases calpains. Exposure of C2C12 myotubes in culture to the cholinergic agonist carbachol triggered a calcium transient, activation of calpain, and stimulation of cyclin-dependent kinase 5 (CDK5) through production of the activator p25 by cleavage of the CDK5 regulatory partner p35. (CDK5 has been previously implicated in AChR dispersal, and p35 is a known substrate for calpain.) Activation of CDK5 by carbachol was blocked by pharmacological inhibition of calpain with calpeptin, and the dispersal of AChR clusters induced by agrin was also prevented if calpain activity was blocked (pharmacologically or by RNAi). ...
The pattern of results suggests cholinergically mediated psychophysiologic pathways of emotional influence in the asthmatic process for some asthmatic children. A heuristic biopsychosocial model of these pathways is presented.
The effect that several substances may have on ANF release by atrial slices and on its tissular content was investigated. alpha- and beta-adrenergic and cholinergic agonists, vasopressin, met-enkephaline, dexamethasone and DOC, in concentration ranging from 10(-4) to 10(-8) M, were added into the in …
Depolarization-induced suppression of inhibition (DSI) is a prevailing form of endocannabinoid signalling. However, several discrepancies have arisen regarding the roles played by the two major brain endocannabinoids, 2-arachidonoylglycerol (2-AG) and anandamide, in mediating DSI. Here we studied endocannabinoid signalling in the prefrontal cortex (PFC), where several components of the endocannabinoid system have been identified, but endocannabinoid signalling remains largely unexplored. In voltage clamp recordings from mouse PFC pyramidal neurons, depolarizing steps significantly suppressed IPSCs induced by application of the cholinergic agonist carbachol. DSI in PFC neurons was abolished by extra- or intracellular application of tetrahydrolipstatin (THL), an inhibitor of the 2-AG synthesis enzyme diacylglycerol lipase (DAGL). Moreover, DSI was enhanced by inhibiting 2-AG degradation, but was unaffected by inhibiting anandamide degradation. THL, however, may affect other enzymes of lipid ...
How is carbachol-induced active sleep abbreviated? c-AS stands for carbachol-induced active sleep. c-AS is defined as carbachol-induced active sleep rarely.
Spatio-temporal patterns of CCh-induced [Ca2+]i transients. The x-y confocal Ca2+ imaging was performed at 32 Hz (A and B), 40 Hz (C), 44 Hz (D) and 30 Hz
Stoelting, R.K., Anticholinesterase Drugs and Cholinergic Agonists, in Pharmacology and Physiology in Anesthetic Practice, Lippincott-Raven Publishers, 1999, 224-237; Taylor, P. Anticholinesterase Agents, In, Goodman and Gillmans The Pharmacologial Basis of Therapeutics,(Hardman, J.G, Limbird, L.E, Molinoff, P.B., Ruddon, R.W, and Gilman, A.G.,eds) TheMcGraw-Hill Companies, Inc.,1996, pp.161-174.. ...
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A Moderate Drug Interaction exists between carbachol ophthalmic and Ceron-DM Drops. View detailed information regarding this drug interaction.
In Chapter 11, we discussed the development of alpha-7-nicotinic cholinergic agonists as a novel therapeutic strategy for schizophrenia. 10.
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TY - JOUR. T1 - Cyclic nucleotides in muscarinic regulation of DNA and RNA polymerase activity in cultured corneal epithelial cells of the rabbit. AU - Colley, A. M.. AU - Cavanagh, Harrison D. AU - Drake, L. A.. AU - Law, M. L.. N1 - Funding Information: ACKNOWLEDGMENTS This work was supported by National Eye Institute Research Grant No. EY04604 and a Departmental grant from Research to Prevent Blindness. The authors gratefully acknowledge the technical assistance o f Mr. Neil Matthews i n photography and animal care and the administrative and clerical assistance of Mrs. Edith Barron, Mrs. Cynthia Hale, and Mrs. LaDonna Hampton.. PY - 1985. Y1 - 1985. N2 - DNA and RNA polymerase activities in the purified nuclear fraction from cultured rabbit corneal epithelial cells were assayed over a range of substrate (labeled dTTP or UTP) concentrations using calf thymus DNA as template. Effects of carbamylcholine on polymerase activities were evaluated over a range of drug concentrations including those ...
Therefore, it is also possible to modify our algorithm to study the coupling mechanisms between exocytosis and endocytosis in the future. Combinatorial microscopy. Google Scholar Employing FM fluorescence imaging, basolateral exocytosis was observed in dispersed rat pancreatic acini after supramaximal CCK or carbachol stimulation; and more remarkably, also after treatment with clinically-relevant concentrations of alcohol and putative alcohol metabolites followed by physiologic CCK or carbachol stimulation 8, 9, 28thus simulating alcoholic pancreatitis. AIP Conf. In summary, we have developed a software platform for the identification and spatiotemporal analysis of vesicle fusion events obtained by TIRF microscopy.. ...
Xerostomia is a subjective sensation of dry mouth, this is a common symptom particularly in older adults and has a variety of causes. Pilocarpine is a cholinergic agonist that non-selectively binds to muscarinic receptors in smooth muscles in the gastrointestinal, urinary and pulmonary systems and stimulates the production of secretions from the salivary and sweat [read the full story…]. ...
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TY - JOUR. T1 - Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine. AU - Nowak, Thomas V.. AU - Harrington, Bonnie. PY - 1985/1/1. Y1 - 1985/1/1. N2 - Proximal and distal rat small intestine was cut into strips measuring 6.0 × 10.0 mm. Strips cut along the oral-caudal axis were called longitudinal strips, whereas those cut 90° to that axis were called circular strips. Stress in circular and longitudinal muscle strips was measured continuously as they were superf used with acetylcholine, carbamylcholine, methacholine, bethanechol, or physostigmine. Resting stress during stretch, acetylcholine-stimulated active stress, and total stress were determined. Proximal circular muscle was five times as sensitive to acetylcholine as distal circular muscle (p , 0.05); proximal longitudinal muscle was 2.8 times as sensitive to bethanechol as distal muscle (p , 0.05). Resting, active, and total stress were similar in proximal and distal muscle, but circular muscle ...
The molecular identities of the pathways that mediate K+ and Cl− effluxes in serous acinar cells are unknown. CFTR mRNA is expressed in these cells, and immunocytochemistry revealed it to be present near the apical membrane. To examine the role of CFTR in Ca2+-evoked fluid secretion, we employed cells from the cftrtm1Unc−/− mouse and we pharmacologically inhibited CFTR in WT mouse cells. The results demonstrated that mouse nasal acinar cells from both WT and cftrtm1Unc−/− mice, as well as WT cells treated with CFTRinh172, all exhibited similar rates of Cl− efflux in response to muscarinic stimulation. Isolated intact submucosal glands from CF individuals that lack functional CFTR can secrete fluid in response to cholinergic agonists (Joo et al. 2002a), and it was recently shown that intact glands in WT and cftrtm1Unc−/− mice trachea secrete fluid in response to CCh at similar rates (Ianowski et al. 2007). It has remained unclear if cholinergic-induced fluid secretion in CF glands ...
For immunofluorescence microscopy, the eyes were enucleated with the lids intact and fixed in 4% formaldehyde in phosphate-buffered saline (PBS; 145 mM NaCl, 7.3 mM Na2HPO4, and 2.7 mM NaH2PO4 [pH 7.2]), for 4 hours at 4°C. The eyes were then rinsed in 5% sucrose dissolved in PBS, placed overnight in 30% sucrose dissolved in PBS at 4°C, embedded in OCT, and frozen. Cryostat sections (6 μm) were placed on slides (Colorfrost/Plus; Fisher Scientific, Pittsburgh, PA) and kept at −20°C until use. Cultured goblet cells (CGCs) grown on glass coverslips were fixed in absolute methanol. Tissue sections and CGCs were then washed in PBS and blocked in PBS containing 1% bovine serum albumin, 4% goat serum, and 0.2% to 0.3% Triton X-100. The NT antibodies (NGF, BDNF, NT3, and NT4) were used at a dilution of 1:800. The NTr antibodies (TrkA, TrkB, TrkC, and p75) were used at a dilution of 1:200. All antibodies were diluted in PBS containing 0.3% Triton X-100 and incubated for 48 hours at 4°C. The ...
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Carbachol lowers pressure in the eye by increasing the amount of fluid that drains from the eye. Carbachol ophthalmic (for the eye) is used to reduce pressure inside the eye after cataract surgery. Carbachol ophthalmic may also be used for purposes not listed in this medication guide.
The pancreas is a mixed gland secretion (external or internal or digestive and insulin) that is in the highest part of the deep abdominal cavity behind the stomach. The pancreas is located in a transverse position with a head, body and tail. Its internal structure is clustered and each of the grains corresponds to a secretory gland acinus.
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Values are means ± SE. Cholinergic responses evoked by bath application of carbachol (10 μM for 5 min) in CA3 pyramidal neurons. Boldface numbers indicate P , 0.05 for carbachol-induced effects within individual cell types (repeated-measures ANOVA with post-tests: baseline, carbachol, and wash). Asterisks indicate P , 0.01 when compared with values in wild-type neurons (one-way ANOVA with post-tests). ...
Cholinergic receptor information including symptoms, causes, diseases, symptoms, treatments, and other medical and health issues.
We studied the effects of cholinergic agonists on slow delayed-rectifier K+ current (IKs) in isolated cells from the sino-atrial node (SAN) region of guinea pig heart, using patch-clamp procedures. Carbachol (5 nM to 10 microM) inhibited IKs in guinea pig SAN cells in the absence of previous beta-adrenergic stimulation and in cells pretreated with 8-(4-chlorophenylthio)-cAMP. Neither the muscarinic antagonist atropine nor the nicotinic antagonist hexamethonium antagonized carbachol inhibition of the current. Similar results were obtained with other cholinergic agonists. Cholinergic stimulation of the muscarinic K+ current was successfully antagonized by atropine in SAN cells where inhibition of IKs persisted. Therefore, the lack of antagonist effects on inhibition of IKs cannot be attributed to either an absence of muscarinic cholinoceptors on SAN cells or a loss of antagonist activity under our experimental conditions. These data demonstrate that cholinergic agonists, including the endogenous ...
TY - JOUR. T1 - Cholinergic modulation of MEG resting-state oscillatory activity in Parkinsons disease related dementia. AU - Bosboom, J.L.W.. AU - Stoffers, D.. AU - Stam, C.J.. AU - Berendse, H.W.. AU - Wolters, E.C.. PY - 2009. Y1 - 2009. U2 - 10.1016/j.clinph.2009.03.004. DO - 10.1016/j.clinph.2009.03.004. M3 - Article. C2 - 19386543. VL - 120. SP - 910. EP - 915. JO - Clinical Neurophysiology. JF - Clinical Neurophysiology. SN - 1388-2457. IS - 5. ER - ...
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IO-CHOL(Carbachol Intraocular Solution USP 0.01% w/v) Description: IO-Chol is a sterile balanced salt solution of carbachol for intracular injection. Warnings & Precautions: Do not…. ...
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Both drugs are agonists are nicotinic cholinergic receptors ... Kishioka S, Kiguchi N, Kobayashi Y, Saika F (2014). "Nicotine ... Nicotinic agonists, Nicotinic antagonists, Plant toxin insecticides, Pregnane X receptor agonists, Pyridine alkaloids, ... Fujii T, Mashimo M, Moriwaki Y, Misawa H, Ono S, Horiguchi K, Kawashima K (2017). "Expression and Function of the Cholinergic ... Nicotine increases cholinergic signaling and adrenergic signaling in colon cancer cells, thereby impeding apoptosis (programmed ...
Fisher A (July 2008). "Cholinergic treatments with emphasis on m1 muscarinic agonists as potential disease-modifying agents for ... In the form of pilocarpine, muscarinic receptor agonists have been used medically for a short time. M3 agonists Aceclidine, for ... Muscarinic+Agonists at the US National Library of Medicine Medical Subject Headings (MeSH) (Articles to be expanded from April ... A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor ...
Contraindications include asthma and angle closure glaucoma.[citation needed] Cevimeline is a cholinergic agonist. It has a ... Muscarinic agonists, Oxathiolanes, Quinuclidines, Spiro compounds, Daiichi Sankyo). ...
Chatterjee PK, Al-Abed Y, Sherry B, Metz CN (November 2009). "Cholinergic agonists regulate JAK2/STAT3 signaling to suppress ... The cholinergic anti-inflammatory pathway provides a braking effect on the innate immune response which protects the body ... The cholinergic anti-inflammatory pathway regulates the innate immune response to injury, pathogens, and tissue ischemia. It is ... Thus, the prefrontal input to the ANS modulate the inflammatory response to psychological stress in part via the cholinergic ...
Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. Both are direct-acting ... Muscarine mimics the function of the natural neurotransmitter acetylcholine in the muscarinic part of the cholinergic nervous ... Muscarinic agonists are used as drugs in treating glaucoma, postoperative ileus, congenital megacolon, urinary retention and ... Inocybe and Clitocybe contain muscarine concentrations up to 1.6%. Muscarine is a nonselective agonist of the muscarinic ...
Thus it is classified as a cholinergic agonist. It is primarily used for various ophthalmic purposes, such as for treating ... they both act on the cholinergic system, increasing cholinergic transmission), but its toxicity is much weaker and it is easier ... Muscarinic agonists, Nicotinic agonists, Peripherally selective drugs, Quaternary ammonium compounds, Ophthalmology drugs). ... Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary ...
Stoelting RK (1999). Anticholinesterase Drugs and Cholinergic Agonists", in Pharmacology and Physiology in Anesthetic Practice ... Blumenthal D, Brunton L, Goodman LS, Parker K, Gilman A, Lazo JS, Buxton I (1996). "5: Autonomic Pharmacology: Cholinergic ... Taylor P, Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Gilman AG (1996). "5: Autonomic Pharmacology: Cholinergic Drugs". The ... ISBN 0-7167-1614-3. Whittaker VP (1990). "The Contribution of Drugs and Toxins to Understanding of Cholinergic Function" (PDF ...
Brannan SK, Sawchak S, Miller AC, Lieberman JA, Paul SM, Breier A (February 2021). "Muscarinic Cholinergic Receptor Agonist and ... May 2000). "Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity ... It has more modest partial agonist pharmacology at the M2, M3 and M5 receptors. Xanomeline regulates key dopaminergic and ... Paul, SM; Yohn, SE; Popiolek, M; Miller, AC; Felder, CC (27 June 2022). "Muscarinic Acetylcholine Receptor Agonists as Novel ...
Cholinergic Agonists and Muscarinic Receptor Antagonists. St. Louis, Missouri: Elsevier. p. 82-97. ISBN 978-0-323-39307-2. OCLC ... α-receptor agonist, α2 > α1, giving negative feedback) Methyldopa (α2 agonist, giving negative feedback) Propranolol (β- ... For a cholinergic agent, the following criteria describe the structure activity relationship: Ing's Rule of 5: there should be ... A parasympathomimetic drug, sometimes called a cholinomimetic drug or cholinergic receptor stimulating agent, is a substance ...
"Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice". Neuropharmacology. 39 (12): ... Vedaclidine (INN,: 180 codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist- ... May 1997). "Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053): a novel analgesic with mixed muscarinic receptor agonist ... May 1997). "Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic". The Journal of ...
... but there is counter-evidence suggesting some delta agonists might have weak ICSS facilitation properties. Cholinergic drugs ... Morphine, a MOR agonist, was one of the earliest studied drugs at the advent of ICSS and BSR. High potency MOR agonists like ... The effects of delta opioid receptor (DOR) agonists/antagonists on ICSS are less clear. One DOR agonist, SNC80, has been found ... GABAB receptor agonists and positive allosteric modulators have been found to result in ICSS depression and have been found to ...
... is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist (parasympathomimetic). It was the ...
The memory impairments were reversed when treated with physostigmine, a cholinergic agonist. However, reversing memory ... A receptor is cholinergic if it uses acetylcholine as its neurotransmitter. A synapse is cholinergic if it uses acetylcholine ... Thus it was proposed that degeneration of cholinergic neurons in the basal forebrain and the associated loss of cholinergic ... Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine. In general, the word "choline" ...
Pretreatment with E1R enhanced the σ1R agonist PRE-084's stimulating effect and facilitated passive avoidance retention. It ... E1R enhances cognition and has efficacy against cholinergic dysfunction in mice without affecting locomotor activity. ...
... is a partial agonist of the 5-HT6 receptor. It enhanced recognition memory and reversed the memory deficits of ... The mechanism of memory enhancement is due to a combined modulation of cholinergic and glutamatergic neurotransmission. E-6837 ... Kendall, I. (February 2011). "E-6801, a 5-HT6 receptor agonist, improves recognition memory by combined modulation of ... 5-HT6 agonists, Anorectics, Imidazoles, Chloroarenes, Sulfonamides, Thiazoles, Tryptamines). ...
Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. GABA ... reuptake inhibitor Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic Glycinergic Histaminergic Melatonergic ...
Beta1-adrenergic agonists, Beta2-adrenergic agonists, Catecholamines, Inotropic agents, TAAR1 agonists, Phenylethanolamines, ... Mehta, Akul (January 27, 2011). "Notes - Medicinal Chemistry of the Peripheral Nervous System - Adrenergics and Cholinergic". ... Isoprenaline is a β1 and β2 adrenoreceptor agonist and has almost no activity on alpha adrenergic receptors. Its agonist ... It is a non-selective β adrenoceptor agonist that is the isopropylamine analog of epinephrine (adrenaline). It is used to treat ...
Amongst the common drugs of abuse, nicotine is one of the strongest agonists at the nicotinic cholinergic synapse. Nicotine, ...
Hartzell HC, Titus L (Feb 1982). "Effects of cholinergic and adrenergic agonists on phosphorylation of a 165,000-dalton ...
... a cholinergic agonist, in the treatment of adults with attention deficit hyperactivity disorder". Am J Psychiatry. 156 (12): ... Potter A, Corwin J, Lang J, Piasecki M, Lenox R, Newhouse PA (March 1999). "Acute effects of the selective cholinergic channel ... It acts as an agonist at neural nicotinic acetylcholine receptors, subtype-selective binding with high affinity to the α4β2, α7 ... Wilens TE, Decker MW (October 2007). "Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity ...
"Focused ultrasound delivery of a selective TrkA agonist rescues cholinergic function in a mouse model of Alzheimer's disease". ... Apolipoprotein E4 allele as a predictor of cholinergic deficits and treatment outcome in Alzheimer disease. Judes Poirier, ... to cholinergic neurons (memory-related brain cells, which are vulnerable in Alzheimer's disease) into the brains of mice with ... "Apolipoprotein E4 allele as a predictor of cholinergic deficits and treatment outcome in Alzheimer disease". Proceedings of the ...
"Muscarinic Cholinergic Receptor Agonist and Peripheral Antagonist for Schizophrenia". The New England Journal of Medicine. 384 ... an M1/M4 preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice". ... However, cholinergic-mediated side effects prevented further advancement of xanomeline into phase 3 trials. Xanomeline was ... Trospium is a non-selective muscarinic antagonist that does not cross into the CNS and reduces peripheral cholinergic side ...
Muscarinic agonist Muscarinic antagonist Nicotinic acetylcholine receptor Nicotinic agonist Nicotinic antagonist Vagal escape ... Very few parts of the sympathetic system use cholinergic receptors. In sweat glands the receptors are of the muscarinic type. ... Also, only when bound with an agonist, those G proteins normally sensitive to PTX also become susceptible to CTX. The various G ... Possible bronchospasm may result if stimulated by muscarinic agonists Location of M5 receptors is not well known. Like the M1 ...
The symptoms of nicotine poisoning are caused by effects at nicotinic cholinergic receptors. Nicotine is an agonist at ... Nicotine is specific for nicotinic cholinergic receptors only and has some, but not all of the symptoms of organophosphate ... excessive stimulation of all types of cholinergic neurons, and a wide range of symptoms. ...
As all cholinergic fibers contain high concentrations of ACh and AChE at their terminals, inhibition of AChE can impair their ... This phenomenon is caused by the excess of agonists (ACh) within the synapse, ultimately leading to a down-regulation of ... Cholinergic nerves play an important role in the normal function of the central nervous, endocrine, neuromuscular, ... When patients are resistant to atropine, the patients can be treated with low doses of anisodamine, a cholinergic and alpha-1 ...
"In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro". Psychopharmacology. ... Alvameline (Lu 25-109) is a M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of ...
Karczmar demonstrated that cholinergic agonists counteract the behavior exhibited in animal models of schizophrenia; on this ... Cholinergic mechanisms, schizophrenia, and neuropsychiatric adaptive dysfunctions. In: Central Cholinergic Mechanisms and ... Cholinergic control of hypokinesia. Prog. Clin. Biol. Res. 39: 374. Karczmar, A. G. and Long, J. P. 1958. Relationship between ... He is widely recognized for his experimental research, almost all of which is devoted to the cholinergic system, both central ...
Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic GABAergic Histaminergic Melatonergic Monoaminergic ... Examples include glycine receptor agonists, glycine receptor antagonists, and glycine reuptake inhibitors. ...
One specific drug candidate is BB14, which is a nerve growth factor-like peptide that acts as a TrkA agonist. BB14 was shown to ... For example, a few studies have used nerve growth factors to regain some cholinergic function in patients with Alzheimer's. ...
Injection of a cholinergic agonist (e.g. carbachol), into the pontine tegmentum produces a state of REM sleep in cats. PET ... Woolf, NJ; Butcher, LL (2011). "Cholinergic systems mediate action from movement to higher consciousness". Behavioural Brain ... The pontine tegmentum contains two predominately cholinergic nuclei, the pedunculopontine nucleus (PPN) and the laterodorsal ... the mesopontine cholinergic system comprising the pedunculopontine nucleus and the laterodorsal tegmental nucleus, and in the ...
Stimulatory factors: Beta-adrenergic agents, cholinergic agents, gastrin-releasing peptide (GRP) Inhibitory factor: ... Cholecystokinin agonists). ...
... has been found to cause more damage to neurons in the presence of group I mGluR agonists. On the other hand, agonists of group ... 5 on mGluR1 function in striatal cholinergic interneurons". Neuropharmacology. 49. 49 Suppl 1: 104-13. doi:10.1016/j.neuropharm ... There is also growing evidence that group II metabotropic glutamate receptor agonists may play a role in the treatment of ... A dimeric organization of mGluRs is required for signaling induced by agonists. Eight different types of mGluRs, labeled mGluR1 ...
Neuronal loss in DLB leads to profound dopamine dysfunction and marked cholinergic pathology; other neurotransmitters might be ... treatment of movement symptoms with dopamine agonists may worsen neuropsychiatric symptoms; and treatment of hallucinations and ...
... 's cytoprotective actions are mediated by enhancement of GABAergic, cholinergic, and monoaminergic neuronal systems ... where it is presumed to be an agonist. It was able to potently inhibit 80% of muscimol binding to the GABAA receptor, although ...
Inverse agonist - invertebrate peptide receptor - invertebrate photoreceptor - Ion channel - ion channel gating - Ionic bond - ... cholinergic receptor - chorionic gonadotropin - chromatid - chromatin - ciclosporin - chromatography - chromosomal crossover - ... agonist - alanine - albumin - alcohol - alcoholic fermentation - alicyclic compound - aliphatic compound - alkali - allosteric ...
Stanton T, Bolden-Watson C, Cusack B, Richelson E (June 1993). "Antagonism of the five cloned human muscarinic cholinergic ... Hindmarch I, Hashimoto K (April 2010). "Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, ... Albayrak Y, Hashimoto K (2017). "Sigma-1 Receptor Agonists and Their Clinical Implications in Neuropsychiatric Disorders". ...
In addition to acting as an inverse agonist at the H1 receptor, chlorphenamine has been found to act as a serotonin reuptake ... Yamamura HI, Snyder SH (May 1974). "Muscarinic cholinergic binding in rat brain". Proceedings of the National Academy of ... It is specifically a potent inverse agonist of the histamine H1 receptor. The drug is also commonly described as possessing ... and terfenadine at the five human muscarinic cholinergic receptor subtypes". Pharmacotherapy. 19 (4): 447-451. doi:10.1592/phco ...
In addition to its actions as an acetylcholinesterase inhibitor, donepezil has been found to act as a potent agonist of the σ1 ... December 2020). "Cholinergic dysfunction in the dorsal striatum promotes habit formation and maladaptive eating". The Journal ... Certainly, Alzheimer's disease involves a substantial loss of the elements of the cholinergic system and it is generally ... Based on the physiopathology of anorexia nervosa, namely in terms of cholinergic deficiencies, the effects of donepezil and ...
Sarter M (August 2015). "Behavioral-cognitive targets for cholinergic enhancement". Current Opinion in Behavioral Sciences. 4: ... full agonist on (α4)2(β2)3, 6% efficacy on (α4)3(β2)2 N-(3-pyridinyl)-bridged bicyclic diamines NS-9283: 60-fold left-shifting ... D2R agonist and nAChR antagonist) Oxantel α3β2-Nicotinic receptor α3β4-Nicotinic receptor α6β2-Nicotinic receptor α7-Nicotinic ... exceptionally potent agonists at nicotinic acetylcholine receptors". J. Med. Chem. 50 (15): 3627-44. doi:10.1021/jm070018l. ...
Optogenetic excitation of cholinergic inputs to the hippocampus primes future contextual fear associations . Hersman S, Cushman ... Using fast-scan cyclic voltammetry, she helped discover that cannabinoid agonists lead to an increased frequency of ... Modulation of cue-triggered reward seeking by cholinergic signaling in the dorsomedial striatum. Ostlund SB, Liu AT, Wassum KM ... Nature Neuroscience (2019) Nucleus accumbens cholinergic interneurons oppose cue-motivated behavior. Collins AL, Aitken TJ, ...
"Entrez Gene: CHRNB2 cholinergic receptor, nicotinic, beta 2 (neuronal)". Skorupska E, Rózycka A, Trzeciak WH (2002). "[ ... 2003). "The calcium sensor protein visinin-like protein-1 modulates the surface expression and agonist sensitivity of the alpha ...
... cholinergic agents MeSH D27.505.519.625.120.140 - cholinergic agonists MeSH D27.505.519.625.120.140.500 - muscarinic agonists ... cholinergic agents MeSH D27.505.696.577.120.140 - cholinergic agonists MeSH D27.505.696.577.120.140.500 - muscarinic agonists ... adrenergic agonists MeSH D27.505.519.625.050.100.100 - adrenergic alpha-agonists MeSH D27.505.519.625.050.100.200 - adrenergic ... adrenergic agonists MeSH D27.505.696.577.050.100.100 - adrenergic alpha-agonists MeSH D27.505.696.577.050.100.200 - adrenergic ...
The only mention here is that there was a discussion 'anxiolytics and GABA agonists' which included BNC-210, but does not ... May 2020). Krystal JH (ed.). "Cholinergic Modulation of Disorder-Relevant Neural Circuits in Generalized Anxiety Disorder". ...
5-Alpha-reductase inhibitor Angiotensin II receptor antagonist ACE inhibitor Alpha-adrenergic agonist Beta blocker Cholinergic ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs used to treat ... PPAR agonist) and mode of action (reducing blood triglycerides), and that are used to prevent and treat the same disease ( ...
Studies have shown that long-term use of benzodiazepines and the benzodiazepine receptor agonist nonbenzodiazepine Z drugs are ... Benzodiazepines, along with antihypertensives and drugs affecting the cholinergic system, are the most common cause of drug- ... "Use of benzodiazepines and benzodiazepine receptor agonists during pregnancy: neonatal outcome and congenital malformations". ... percent reduction in binding capacity of benzodiazepines after seven days administration of high doses of the partial agonist ...
Sigma agonists, Sodium channel blockers, Tricyclic antidepressants, TrkB agonists, World Health Organization essential ... Stanton T, Bolden-Watson C, Cusack B, Richelson E (1993). "Antagonism of the five cloned human muscarinic cholinergic receptors ... Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K (June 2009). "Amitriptyline is a TrkA and TrkB receptor agonist ...
It is still a potent agonist for the UII- receptor which suggests that this acidic amino acid is not required for activation of ... It is found in many peripheral tissues, blood vessels, and also the brainstem cholinergic neurons of the laterodorsal tegmental ... UII is known as a vasoconstrictor meaning that even though both are agonists for the same receptor they can produce opposite ... The peptide sequence for URP is: Alanine-Cysteine-Phenylalanine-Tryptophan-Lysine-Tyrosine-Cysteine-Valine URP is an agonist ...
"Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro". FEBS ... "GRK5 Deficiency Leads to Selective Basal Forebrain Cholinergic Neuronal Vulnerability". Scientific Reports. 6: 26116. Bibcode: ... "A polymorphism of G-protein coupled receptor kinase5 alters agonist-promoted desensitization of beta2-adrenergic receptors". ... of human vasopressin/oxytocin receptor subtypes with G protein-coupled receptor kinases and protein kinase C after agonist ...
Data from clinical studies have shown that DA agonists, such as bromocriptine, pramipexole and ropinirole, exhibit ... "Rosmarinus officinalis polyphenols produce anti-depressant like effect through monoaminergic and cholinergic functions ... "A combined α7 nicotinic acetylcholine receptor agonist and monoamine reuptake inhibitor, NS9775, represents a novel profile ...
... is a potent α2 adrenergic agonist. When xylazine and other α2 adrenergic receptor agonists are administered, they ... Xylazine has varying affinities for cholinergic, serotonergic, dopaminergic, α1 adrenergic, H2-histaminergic and opiate ... As an agonist, xylazine leads to a decrease in neurotransmission of norepinephrine and dopamine in the central nervous system. ... It is an analog of clonidine and an agonist at the α2 class of adrenergic receptor. In veterinary anesthesia, xylazine is often ...
The muscarine cholinergic receptor activates a G-protein when bound to extracellular ACh. The alpha subunit of the G-protein ... The result of the newly introduced ARG is a 30-fold reduction of agonist affinity, 75-fold reduction of gating efficiency, and ... Nicotinic and muscarinic are two main kinds of "cholinergic" receptors. Molecular biology has shown that the nicotinic and ... Muscarinic acetylcholine receptor M5 Nicotinic agonists "Reference at image.slidesharecdn.com". Doyle DA (2004). "Structural ...
The growth hormone releasing hormone receptor agonist MK-677 has been shown to increase REM in older adults as well as stage IV ... "Odor cueing during slow-wave sleep benefits memory independently of low cholinergic tone". Psychopharmacology. 235 (1): 291-299 ...
"Cholinergic Agonists" by people in Harvard Catalyst Profiles by year, and whether "Cholinergic Agonists" was a major or minor ... The nonopioid cholinergic agonist GTS-21 mitigates morphine-induced aggravation of burn injury pain together with inhibition of ... "Cholinergic Agonists" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... Interaction of IFN-? with cholinergic agonists to modulate rat and human goblet cell function. Mucosal Immunol. 2016 Jan; 9(1): ...
Cholinergic agonist agents. Class Summary. These agents stimulate cholinergic receptors in the smooth muscle of the urinary ... Alpha-1 Agonists. Class Summary. These are used in orthostatic hypotension if simple measures yield no improvement. ... The binding domain of the type A molecule appears to be the heavy chain, which is selective for cholinergic nerve terminals. (2 ... Smooth muscle relaxing effect distal to cholinergic receptor site. Long-acting form available for qd dosing. ...
Activated Charcoal, Polyethylene Glycol, Cholinergic Agonists, and Plasmapheresis. No data exist on the effectiveness of ... Cholinergic agonists such as guanidine and 3,4-diaminopuridine have been used in attempts to stimulate acetylcholine release ... and is transported to peripheral cholinergic nerve terminals, including neuromuscular junctions, postganglionic parasympathetic ...
Cholinergic Agonists. Class Summary. Cholinergic agonist activity activates the trigeminal parasympathetic pathway resulting in ... Varenicline nasal spray is a water-soluble agonist for nicotinic cholinergic receptor. It increases lacrimal unit production of ...
Previous Next TOPICS: Acetylcholinesterase inhibitors, acetylcholine, alzheimers disease, donepezil, rivastigmine, galantamine, edrophonium, quaternary
Receptors of cholinergic systems......Muscarinic and Nicotinic receptors..... ... Cholinergic agonist, cholinergic agonist and antagonist classification, cholinergic agonist drugs list, cholinergic and ... Following is the drugs of classification of cholinergic agonists list.. cholinergic agonists is divided into Directly acting ... Cholinergic agonist and antagonist drugs classification List:. February 4, 2018. by dramjad Leave a Comment ...
Effects of cholinergic agonists on LHb neuron membrane currents. We previously reported that the muscarinic agonist Oxo-M ... Using in vitro electrophysiology, we find that LHb neurons are depolarized or hyperpolarized by the cholinergic agonists ... 1992b) Muscarinic M2 receptor mRNA expression and receptor binding in cholinergic and non-cholinergic cells in the rat brain: a ... we measured the effect of the nonselective cholinergic agonist CCh (10 µm) on LHb neuron membrane currents under voltage clamp ...
Effect of cholinergic agonists and antagonists on morphine withdrawal induced aversion to saccharin drinking in rats. Indian ... Effect of cholinergic agonists and antagonists on morphine withdrawal induced aversion to saccharin drinking in rats. ...
Cholinergic Antagonists / therapeutic use* * Clinical Trials as Topic * Dopamine Agonists / therapeutic use* ...
Pilocarpine is in a class of medications called cholinergic agonists. It works by increasing the amount of saliva in the mouth. ...
Summary of the probe development efforts to identify agonists of the human cholinergic receptor, muscarinic 1 (CHRM1). ...
Opiate agonists have cholinergic activity. Large doses and/or rapid intravenous administration may produce bradycardia and ... Opiate agonists (applies to hydrocodone) drug dependence. Major Potential Hazard, High plausibility. Applicable conditions: ... Opiate agonists should not be used in patients with suspected or known head injury or increased intracranial pressure. Also, ... Opiate agonists (applies to hydrocodone) acute alcohol intoxication. Major Potential Hazard, High plausibility. ...
Cholinergic agonists are used in patients with detrusor areflexia; these agents include bethanechol chloride, which may mimic ...
Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Anticonvulsants. Anti- ... Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. ... Need for daily controller therapy (i.e., ICS, leukotriene modifiers, and/or long-acting beta-agonists) based on one or more of ... Current options for the second medication include a long-acting beta-agonist, a leukotriene modifier, or theophylline. It is ...
2004) Cholinergic agonists inhibit HMGB1 release and improve survival in experimental sepsis Nature Medicine 10:1216-1221. ... However, such experiments with agonists/antagonists may often be tricky. We added the following sentences: "Therefore, the ... A cholinergic anti-inflammatory pathway has also been reported, in which the activation of efferent vagus nerves suppresses ... for these claims by repeating these experiments in the presence of catecholamine antagonists or a corticosterone agonist. These ...
Cholinergic Agonist. Oral. June 20, 2022 In Use. 71335-2122-01. 71335-2122 PREDNISONE. Prednisone. 10.0 mg/1. Hormonal Therapy ...
Drugs with cholinergic effects: Coadministration may increase risk of adverse cholinergic effects ... Monitor Closely (1)amifampridine and echothiophate iodide both increase cholinergic effects/transmission. Use Caution/Monitor. ... Monitor Closely (1)amifampridine and acetylcholine both increase cholinergic effects/transmission. Use Caution/Monitor. ... Monitor Closely (1)amifampridine and bethanechol both increase cholinergic effects/transmission. Use Caution/Monitor. ...
Physiology of the Peripheral Nervous System Section 2. Cholinergic Drugs 14. Muscarinic Agonists and Antagonists 15. ... Adrenergic Agonists 18. Adrenergic Antagonists 19. Indirect-Acting Antiadrenergic Agents. UNIT V: CENTRAL NERVOUS SYSTEM DRUGS ... Drugs That Block Nicotinic Cholinergic Transmission: Neuromuscular Blocking Agents Section 3. Adrenergic Drugs 17. ...
3 Potent antagonists/partial agonists: Aripiprazole, brexpiprazole, and cariprazine. All of these are extremely potent ... Muscarinic cholinergic antagonist. *Histamine 1 antagonist. *Noradrenergic alpha 1, 2 (with sub-receptors of each) antagonist ...
Third- or fourth-line treatments include cholinergic agonists, most commonly pilocarpine or carbachol. These miotic agents ... Alpha-agonists work by increasing uveoscleral outflow of aqueous humor,61 and the newer, more specific alpha2 agonists (eg, ... cholinergic agonists and oral therapy. Limitations to existing topical IOP-reducing medications include continued disease ... Epinephrine, a nonspecific adrenergic agonist, is rarely used today, although it has a long history for glaucoma use.61 ...
1991). Midlatency auditory evoked responses: differential effects of a cholinergic agonist and antagonist. Electroencephalogr ... 1990). Cholinergic neurons of the feline pontomesencephalon. Brain Res 520:43-54. ...
Dexmedetomidine is a α2-adrenoceptor agonist with anti-inflammatory effects mediated via activation of the cholinergic anti- ... Inhibition of HMGB1/RAGE-mediated endocytosis by HMGB1 antagonist box A, anti-HMGB1 antibodies, and cholinergic agonists ... Splenic nerve is required for cholinergic antiinflammatory pathway control of TNF in endotoxemia. Proc Natl Acad Sci USA. (2008 ... Splenectomy inactivates the cholinergic antiinflammatory pathway during lethal endotoxemia and polymicrobial sepsis. J Exp Med. ...
Retention is enhanced by post-training administration of cholinergic muscarinic agonists and impaired by antagonists. The ... However, cholinergic drugs can block both the memory-enhancing and the memory-impairing effects of Epi. The findings suggest ... that memory storage can be modulated by peripheral epinephrine as well as by drugs affecting the muscarinic cholinergic system ... present experiments examined the interaction of peripheral Epi and cholinergic drugs in memory modulation. Male CFW mice (60 ...
Anti-cholinergic Agents. 7.3. Anti-leukotrienes. 7.4. Antihistamines. 7.5. Beta-2 Agonists. 7.6. Combination Drugs. 7.7. ... Based on Drug Class, the market was studied across Anti-cholinergic Agents, Anti-leukotrienes, Antihistamines, Beta-2 Agonists ... GLOBAL PULMONARY DRUGS MARKET SIZE, BY BETA-2 AGONISTS, 2018-2027 (USD BILLION). TABLE 36. GLOBAL PULMONARY DRUGS MARKET SIZE, ... BY BETA-2 AGONISTS, BY REGION, 2018-2027 (USD BILLION). TABLE 37. GLOBAL PULMONARY DRUGS MARKET SIZE, BY BETA-2 AGONISTS, BY ...
cholinergic drug Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that ... cholinergic drug Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that ... rivastigmine (CHEBI:8874) has role cholinergic drug (CHEBI:38323) rivastigmine (CHEBI:8874) has role EC (cholinesterase ... affect the life cycle of acetylcholine, and drugs that affect the survival of cholinergic neurons. ...
Use of certain medications, such as cholinergic agents or alpha-agonists. Symptoms. Any loss of bladder control can be ...
... similar neuromuscular blocking agents or cholinergic agonists such as bethanechol [see Clinical Pharmacology (12.3)]. ... In addition to muscle weakness or fasciculations, some or all of the following signs of cholinergic crisis may develop: severe ... The degree of this cholinergic loss has been correlated with degree of cognitive impairment and density of amyloid plaques (a ... An increase in cholinergic tone may worsen symptoms related to extrapyramidal disorders [see Adverse Reactions (6.2)]. ...
CHOLINERGIC AGONISTS. Pilocarpine. Carbachol ADENERGIC AGONISTS. Epinephrine. Dipivefrin Back to Top. ANTIVIRALS. Used ...
Pilocarpine belongs to a group of medications called cholinergic agonists. These work by increasing the amount of saliva in the ...
  • IMSEAR at SEARO: Effect of cholinergic agonists and antagonists on morphine withdrawal induced aversion to saccharin drinking in rats. (who.int)
  • Retention is enhanced by post-training administration of cholinergic muscarinic agonists and impaired by antagonists. (semanticscholar.org)
  • Included here are agonists and antagonists, drugs that affect the life cycle of acetylcholine, and drugs that affect the survival of cholinergic neurons. (ebi.ac.uk)
  • Selective breeding for diisopropyl fluorophosphatesensitivity: Behavioural effects of cholinergic agonists and antagonists. (bvsalud.org)
  • Pilocarpine is in a class of medications called cholinergic agonists. (medlineplus.gov)
  • Pilocarpine belongs to a group of medications called cholinergic agonists. (rxwiki.com)
  • To investigate the effects of the N-methyl-D-aspartate (NMDA) antagonist MK-801 and the intravenous anaesthetic ketamine on cholinergic modulated depolarisation-induced GABA release, both drugs were coadministered with the M-cholinoceptor agonist pilocarpine in a superfusion model of rat striatal slices. (erowid.org)
  • Pilocarpine belongs to a class of drugs known as cholinergic agonists. (blinkhealth.com)
  • There are two type of cholinesterases, True cholinesterases which is present in cholinergic neurons, ganglia, RBCs and neuromuscular junction. (medicscenter.com)
  • Using in vitro electrophysiology, we find that LHb neurons are depolarized or hyperpolarized by the cholinergic agonists oxotremorine-M (Oxo-M) and carbachol (CCh), and that mAChRs inhibit synaptic GABA and glutamatergic inputs to these cells similarly in male and female rats. (jneurosci.org)
  • The cholinergic motor neurons express an ACR-2-containing pentameric acetylcholine receptor (ACR-2R) comprised of ACR-2, ACR-3, ACR-12, UNC-38, and UNC-63 subunits. (wormbase.org)
  • These two receptor subtypes regulate the coordinated activity of excitatory (cholinergic) and inhibitory (GABAergic) motor neurons. (wormbase.org)
  • We have shown that the iAChR subunit ACR-12 is differentially expressed in both cholinergic and GABAergic motor neurons within the motor circuit. (wormbase.org)
  • In cholinergic motor neurons, ACR-12 is incorporated into the previously characterized ACR-2 heteromeric receptor, which shows non-synaptic localization patterns and plays a modulatory role in controlling circuit function. (wormbase.org)
  • Cholinergic neurons in the basal forebrain project heavily to the main olfactory bulb, the first processing station in the olfactory pathway. (nature.com)
  • Here, we identify a specific basal forebrain cholinergic projection that innervates select neurons concentrated in the internal plexiform layer of the main olfactory bulb. (nature.com)
  • Cholinergic neurons within basal forebrain (BF) nuclei project to many different brain regions where they have an important role in learning and memory, attention, and cognition. (nature.com)
  • Here, we show that a similar population of VGLUT3 + cholinergic neurons is also present in the HDB of adult mice. (nature.com)
  • Further support for GABA co-transmission is provided by showing the colocalization of cholinergic and GABAergic markers within HDB neurons as well as their axonal projections to the IPL. (nature.com)
  • Vasoconstriction of the isolated rabbit ear artery caused by nicotinic agonists acting on adrenergic neurons. (aspetjournals.org)
  • Desensitization of the adrenergic neurons of the isolated rabbit ear artery to nicotinic agonists. (aspetjournals.org)
  • However, Sesack and Bunney (1989) found that iontophoretic application of a D2 agonist directly onto single PFC neurons in vivo failed to mimic the DA-mediated firing suppression. (scholarpedia.org)
  • In separate studies, the authors colocalized alpha2C adrenoceptors with cholinergic neurons. (asahq.org)
  • Alpha2C adrenoceptors colocalized with cholinergic neurons in both superficial and deep dorsal horn. (asahq.org)
  • amifampridine and carbachol both increase cholinergic effects/transmission. (medscape.com)
  • Transient infusion of the cholinergic agonist carbachol into hippocampal slices induced rhythmic activity that persisted for hours after washout. (escholarship.org)
  • Carbachol is a cholinergic agonist that binds to and activates acetylcholine receptors, affecting both the iris sphincter and the ciliary body. (ophthalmologytimes.com)
  • For example, previous evidence suggests that combining brimonidine tartrate with carbachol could have additive contributions.4-6 Brimonidine, a sympatholytic α-2 agonist, prevents pupil dilation by inhibiting the contraction of the iris dilator muscle and may also inhibit contraction of the ciliary muscle. (ophthalmologytimes.com)
  • Topical prostaglandin analogues or beta-adrenergic receptor blockers are first used, followed by alpha-agonists or topical carbonic anhydrase inhibitors, and infrequently, cholinergic agonists and oral therapy. (ajmc.com)
  • Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia: role of cyclic 3',5' - adenosine monophosphate. (aspetjournals.org)
  • α 2 -ADRENERGIC receptor (α 2 -AR) agonists produce analgesia in humans and animals, primarily by actions in the spinal cord. (asahq.org)
  • Extensive evidence indicates that memory storage can be modulated by peripheral epinephrine as well as by drugs affecting the muscarinic cholinergic system. (semanticscholar.org)
  • Drugs that bind to and activate cholinergic receptors. (harvard.edu)
  • Following is the drugs of classification of cholinergic agonists list. (medicscenter.com)
  • The present experiments examined the interaction of peripheral Epi and cholinergic drugs in memory modulation. (semanticscholar.org)
  • Effects of cholinergic and anticholinergic drugs and a partial cholinergic agonist on the development and expression of physical dependence on morphine in rat. (aspetjournals.org)
  • To determine the interaction between cannabinoid and cholinergic systems, we exposed rats treated with WIN-2 or cholinergic drugs to a hippocampal-dependent delayed nonmatch to sample (DNMS) task to study STM, and recorded hippocampal single-unit activity in vivo. (elsevier.com)
  • Little is known about the effects of drugs on cholinergic modulated GABA release in the striatum. (erowid.org)
  • This reduction of striatal GABA release may therefore contribute to the beneficial effect of both drugs in pathological situations of cholinergic overstimulation, e.g. during intoxication with acetylcholine esterase inhibitors. (erowid.org)
  • The Flinders Sensitive Line of rats (FSL) has been selectively bred to have increased sensitivity to cholinergic drugs. (duke.edu)
  • and launch of new Alzheimer`s drugs including anti-amyloid proteins, cholinergic and nicotine receptor agonists, neuro protective drugs, vaccines and GABA receptor modulators. (financialbuzz.com)
  • Previous studies suggest a shift in alpha 2 adrenoceptor subtype and the involvement of cholinergic interneurons in antinociception in the spinal cord after nerve injury. (asahq.org)
  • Physostigmine and galanthamine bind in the presence of agonist at the canonical and noncanonical subunit interfaces of a nicotinic acetylcholine receptor. (harvard.edu)
  • acetylcarnitine chloride is an agonist for cholinergic.acetylcholine receptor (achr) is an integral membrane protein receptor for acetylcholine. (chemicalbook.com)
  • Current options for the second medication include a long-acting beta-agonist, a leukotriene modifier, or theophylline. (clinicaltrials.gov)
  • This study will also examine whether the addition of tiotropium bromide to low dose ICS is as effective as the addition of a long-acting beta-agonist at maintaining asthma control. (clinicaltrials.gov)
  • There are two type of cholinergic receptor Muscarinic and nicotinic receptors. (medicscenter.com)
  • Findings suggest that the induction of amnesia of passive avoidance involves central cholinergic systems, whereas the NEO, and possibly PHYSO, reversal of the SCOP induced amnesia is mediated peripherally by both muscarinic and nicotinic receptors. (semanticscholar.org)
  • Although mediated through activation of CB1 receptors located in memory-related brain regions such as the hippocampus and prefrontal cortex, these may, in part, be due to a reduction in acetylcholine release (i.e., cholinergic hypofunction). (elsevier.com)
  • AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. (neurotree.org)
  • There are mutual interactions between glucocorticoids and the striatal cholinergic system in enhancing the consolidation of memory of inhibitory avoidance training, and this research indicates that long-term memory may be formed through interactions within the dorsal striatum of the rat. (semanticscholar.org)
  • It is found that cholinergic NBM-cortex projections are required for BLA-mediated modulation of memory consolidation and are implicated in learning, memory storage, and plasticity. (semanticscholar.org)
  • Tests were made for use-dependent plasticity in the cholinergic projections to hippocampus. (escholarship.org)
  • Despite these strong though conflicted effects of cholinergic signaling on M/TC activity, MCs strikingly exhibit no postsynaptic response to brief optogenetic stimulation of cholinergic projections in vitro 10 and show only an ~ 0.5 mV hyperpolarization with a 15 s-long stimulation 4 . (nature.com)
  • Underscoring this controversy and the lack of clarity on the functional role of cholinergic projections is the potential for more complex neurotransmitter signaling. (nature.com)
  • The purpose of this study was to examine the location and number of cells in the spinal cord activated by intrathecal clonidine in these two circumstances and to test whether one class of interneurons, cholinergic, express alpha 2 adrenoceptors. (asahq.org)
  • 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)
  • The nonopioid cholinergic agonist GTS-21 mitigates morphine-induced aggravation of burn injury pain together with inhibition of spinal microglia activation in young rats. (harvard.edu)
  • In summary, we show that a cholinergic signal to LHb and activation of M 2 Rs are critical to enable inhibition of responding for cocaine, and we define cellular mechanisms through which this may occur. (jneurosci.org)
  • Accordingly, D2 agonists were more effective than D1 agonists in replicating the DA-mediated inhibition of spontaneous firing (Thierry et al, 1998). (scholarpedia.org)
  • Striatal GABA release has been shown to be enhanced under pathological conditions of cholinergic overstimulation, e.g. inhibition of acetylcholine esterase. (erowid.org)
  • Not only are α 2 -AR agonist potency and efficacy altered by nerve injury, but the α 2 -AR subtypes involved and their interaction with cholinergic systems of inhibition are shifted as well. (asahq.org)
  • In the mid-1990s, researchers found that Fasoracetam reverses the inhibition of cyclic AMP formation produced by the GABA-B agonist, Baclofen. (newmind.com)
  • Methylatropine (2 mg kg-1 s.c.) was administered 15 min before oxotremorine to block the peripheral effects of the agonist. (duke.edu)
  • This increase in striatal GABA release during cholinergic overstimulation is mediated by M-cholinoceptors and is associated with clinical symptoms, e.g. the occurrence of seizures. (erowid.org)
  • This supports the notion that cannabinoid-modulated cholinergic activity is a mechanism underlying the performance deficits in DNMS. (elsevier.com)
  • Alpha 2 adrenoceptor agonists produce antinociception in normal animals and alleviate mechanical allodynia in animals with nerve injury, although their mechanism of action may differ in these situations. (asahq.org)
  • Any drug used for its actions on cholinergic systems. (ebi.ac.uk)
  • Cholinergic Agonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • Prodrug metabolized to desglymidodrine, a selective alpha1-adrenoreceptor agonist. (medscape.com)
  • Reactivity of isolated tracheal smooth muscle to cholinergic agonists was significantly increased after O(3) exposure, as were contractions to electrical field stimulation at 10 Hz. (cdc.gov)
  • It thus seems that activation of cholinergic synapses induces lasting changes in hippocampal physiology. (escholarship.org)
  • Typically, these rats react with twice as great a hypothermic effect to muscarinic agonists such as oxotremorine, as do similarly bred Flinders Resistant Line rats (FRL). (duke.edu)
  • abstract = "It is now well established that cannabinoid agonists such as Delta(9)-tetrahydrocannabinol (THC), anandamide, and WIN 55,212-2 (WIN-2) produce potent and specific deficits in working memory (WM)/short-term memory (STM) tasks in rodents. (elsevier.com)
  • Smooth muscle relaxing effect distal to cholinergic receptor site. (medscape.com)
  • We further defined a role for the sphingosine kinase, sphk-1 , in cholinergic neuron activity, independent of previously known signaling pathways. (wormbase.org)
  • Second, a muscarinic antagonist (atropine) completely abolished stable rhythmic activity after agonist washout. (escholarship.org)
  • This result indicates that endogenous cholinergic activity is responsible for the persistence of rhythmic oscillations. (escholarship.org)
  • These experiments suggest that short periods of intense cholinergic activity induce lasting changes in cholinergic synapses and thus extend such forms of plasticity to beyond the glutamatergic system. (escholarship.org)
  • Fasoracetam showed antiamnesiac activity in a variety of animal models of cholinergic dysfunction. (newmind.com)
  • with cholinergic agonists to modulate rat and human goblet cell function. (harvard.edu)
  • Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. (bvsalud.org)
  • Comparable effects were obtained with physostigmine, a drug that blocks acetylcholine breakdown and thereby enhances cholinergic transmission. (escholarship.org)