Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.Pain Perception: The process by which PAIN is recognized and interpreted by the brain.Extremities: The farthest or outermost projections of the body, such as the HAND and FOOT.Informed Consent: Voluntary authorization, by a patient or research subject, with full comprehension of the risks involved, for diagnostic or investigative procedures, and for medical and surgical treatment.Vagus Nerve: The 10th cranial nerve. The vagus is a mixed nerve which contains somatic afferents (from skin in back of the ear and the external auditory meatus), visceral afferents (from the pharynx, larynx, thorax, and abdomen), parasympathetic efferents (to the thorax and abdomen), and efferents to striated muscle (of the larynx and pharynx).Psychodrama: Primarily a technique of group psychotherapy which involves a structured, directed, and dramatized acting out of the patient's personal and emotional problems.Autonomic Nervous System: The ENTERIC NERVOUS SYSTEM; PARASYMPATHETIC NERVOUS SYSTEM; and SYMPATHETIC NERVOUS SYSTEM taken together. Generally speaking, the autonomic nervous system regulates the internal environment during both peaceful activity and physical or emotional stress. Autonomic activity is controlled and integrated by the CENTRAL NERVOUS SYSTEM, especially the HYPOTHALAMUS and the SOLITARY NUCLEUS, which receive information relayed from VISCERAL AFFERENTS.Pain: An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.Pain Threshold: Amount of stimulation required before the sensation of pain is experienced.Perception: The process by which the nature and meaning of sensory stimuli are recognized and interpreted.Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.Opiate Alkaloids: Alkaloids found in OPIUM from PAPAVER that induce analgesic and narcotic effects by action upon OPIOID RECEPTORS.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.Questionnaires: Predetermined sets of questions used to collect data - clinical data, social status, occupational group, etc. The term is often applied to a self-completed survey instrument.MichiganAnalgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Hydrocortisone: The main glucocorticoid secreted by the ADRENAL CORTEX. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions.Substance Withdrawal Syndrome: Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Antidepressive Agents, Tricyclic: Substances that contain a fused three-ring moiety and are used in the treatment of depression. These drugs block the uptake of norepinephrine and serotonin into axon terminals and may block some subtypes of serotonin, adrenergic, and histamine receptors. However the mechanism of their antidepressant effects is not clear because the therapeutic effects usually take weeks to develop and may reflect compensatory changes in the central nervous system.Physician-Patient Relations: The interactions between physician and patient.Research Personnel: Those individuals engaged in research.Anesthesia, General: Procedure in which patients are induced into an unconscious state through use of various medications so that they do not feel pain during surgery.Anesthesia: A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.Anesthesia, Local: A blocking of nerve conduction to a specific area by an injection of an anesthetic agent.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.DibenzothiazepinesAkathisia, Drug-Induced: A condition associated with the use of certain medications and characterized by an internal sense of motor restlessness often described as an inability to resist the urge to move.Databases, Factual: Extensive collections, reputedly complete, of facts and data garnered from material of a specialized subject area and made available for analysis and application. The collection can be automated by various contemporary methods for retrieval. The concept should be differentiated from DATABASES, BIBLIOGRAPHIC which is restricted to collections of bibliographic references.ThiazolesSoftware: Sequential operating programs and data which instruct the functioning of a digital computer.Terminology as Topic: The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.Fonofos: An organothiophosphorus cholinesterase inhibitor that is used as an insecticide.Antipsychotic Agents: Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Drug Discovery: The process of finding chemicals for potential therapeutic use.Parkinson Disease: A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)North AmericaAlzheimer Disease: A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)Low Back Pain: Acute or chronic pain in the lumbar or sacral regions, which may be associated with musculo-ligamentous SPRAINS AND STRAINS; INTERVERTEBRAL DISK DISPLACEMENT; and other conditions.Back Pain: Acute or chronic pain located in the posterior regions of the THORAX; LUMBOSACRAL REGION; or the adjacent regions.Antiparkinson Agents: Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.French Guiana: A French overseas department on the northeast coast of South America. Its capital is Cayenne. It was first settled by the French in 1604. Early development was hindered because of the presence of a penal colony. The name of the country and the capital are variants of Guyana, possibly from the native Indian Guarani guai (born) + ana (kin), implying a united and interrelated race of people. (From Webster's New Geographical Dictionary, 1988, p418 & Room, Brewer's Dictionary of Names, 1992, p195)Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.Back: The rear surface of an upright primate from the shoulders to the hip, or the dorsal surface of tetrapods.Pausinystalia: A plant genus of the family RUBIACEAE. Members produce YOHIMBINE.Integrative Medicine: The discipline concerned with using the combination of conventional ALLOPATHIC MEDICINE and ALTERNATIVE MEDICINE to address the biological, psychological, social, and spiritual aspects of health and illness.Evidence-Based Medicine: An approach of practicing medicine with the goal to improve and evaluate patient care. It requires the judicious integration of best research evidence with the patient's values to make decisions about medical care. This method is to help physicians make proper diagnosis, devise best testing plan, choose best treatment and methods of disease prevention, as well as develop guidelines for large groups of patients with the same disease. (from JAMA 296 (9), 2006)HistoryPlant Bark: The outer layer of the woody parts of plants.Plants, Genetically Modified: PLANTS, or their progeny, whose GENOME has been altered by GENETIC ENGINEERING.Plant Leaves: Expanded structures, usually green, of vascular plants, characteristically consisting of a bladelike expansion attached to a stem, and functioning as the principal organ of photosynthesis and transpiration. (American Heritage Dictionary, 2d ed)Plant Proteins: Proteins found in plants (flowers, herbs, shrubs, trees, etc.). The concept does not include proteins found in vegetables for which VEGETABLE PROTEINS is available.User-Computer Interface: The portion of an interactive computer program that issues messages to and receives commands from a user.Apiaceae: A large plant family in the order Apiales, also known as Umbelliferae. Most are aromatic herbs with alternate, feather-divided leaves that are sheathed at the base. The flowers often form a conspicuous flat-topped umbel. Each small individual flower is usually bisexual, with five sepals, five petals, and an enlarged disk at the base of the style. The fruits are ridged and are composed of two parts that split open at maturity.Acorus: A plant genus of the family ACORACEAE, order Arales, subclass Arecidae most notable for Acorus calamus L. root which contains asarone and has been used in TRADITIONAL MEDICINE.Pimenta: A plant genus in the family MYRTACEAE, order Myrtales, subclass Rosidae. It is best known for allspice from the dried berry of Pimenta diocia.Piper nigrum: A plant species in the PIPERACEAE plant family. It is a common spice on foods and is used medicinally to increase gastrointestinal assimilation of other supplements and drugs. Piperine is a key component. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water.Myrtaceae: The myrtle plant family of the order Myrtales. It includes several aromatic medicinal plants such as EUCALYPTUS.Acoraceae: A plant family of the order Arales, subclass Arecidae, class Liliopsida (monocot).Black Pepper: A common spice from fruit of PIPER NIGRUM. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water. Piperine is a key component used medicinally to increase gastrointestinal assimilation of other supplements and drugs.Spices: The dried seeds, bark, root, stems, buds, leaves, or fruit of aromatic plants used to season food.Cuscuta: A plant genus of the family Cuscutaceae. It is a threadlike climbing parasitic plant that is used in DRUGS, CHINESE HERBAL.Asteraceae: A large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of "daisy" refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.Oxymetazoline: A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)Opossums: New World marsupials of the family Didelphidae. Opossums are omnivorous, largely nocturnal and arboreal MAMMALS, grow to about three feet in length, including the scaly prehensile tail, and have an abdominal pouch in which the young are carried at birth.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Nasal Decongestants: Drugs designed to treat inflammation of the nasal passages, generally the result of an infection (more often than not the common cold) or an allergy related condition, e.g., hay fever. The inflammation involves swelling of the mucous membrane that lines the nasal passages and results in inordinate mucus production. The primary class of nasal decongestants are vasoconstrictor agents. (From PharmAssist, The Family Guide to Health and Medicine, 1993)Parathyroid Hormone: A polypeptide hormone (84 amino acid residues) secreted by the PARATHYROID GLANDS which performs the essential role of maintaining intracellular CALCIUM levels in the body. Parathyroid hormone increases intracellular calcium by promoting the release of CALCIUM from BONE, increases the intestinal absorption of calcium, increases the renal tubular reabsorption of calcium, and increases the renal excretion of phosphates.Virulence Factors, Bordetella: A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.Adenylate Cyclase Toxin: One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.GTP-Binding Proteins: 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.-.Marsupialia: An infraclass of MAMMALS, also called Metatheria, where the young are born at an early stage of development and continue to develop in a pouch (marsupium). In contrast to Eutheria (placentals), marsupials have an incomplete PLACENTA.Aporphines: Dibenzoquinolines derived in plants from (S)-reticuline (BENZYLISOQUINOLINES).Peumus: A plant genus of the family MONIMIACEAE. Members contain boldine ALKALOIDS. Some PEUMUS species have been reclassified as CRYPTOCARYA.OxathiinsPhenalenes: A group of AROMATIC HYDROCARBONS that have three rings joined as a triad around a single carbon atom so all three are conjoined, in contrast to a linear arrangement (ANTHRACENES) or angular arrangement (PHENANTHRENES).Lauraceae: A family of mainly aromatic evergreen plants in the order Laurales. The laurel family includes 2,200 species in 45 genera and from these are derived medicinal extracts, essential oils, camphor and other products.Compulsive Behavior: The behavior of performing an act persistently and repetitively without it leading to reward or pleasure. The act is usually a small, circumscribed behavior, almost ritualistic, yet not pathologically disturbing. Examples of compulsive behavior include twirling of hair, checking something constantly, not wanting pennies in change, straightening tilted pictures, etc.Weight Lifting: A sport in which weights are lifted competitively or as an exercise.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Dietary Supplements: Products in capsule, tablet or liquid form that provide dietary ingredients, and that are intended to be taken by mouth to increase the intake of nutrients. Dietary supplements can include macronutrients, such as proteins, carbohydrates, and fats; and/or MICRONUTRIENTS, such as VITAMINS; MINERALS; and PHYTOCHEMICALS.Sexual Dysfunctions, Psychological: Disturbances in sexual desire and the psychophysiologic changes that characterize the sexual response cycle and cause marked distress and interpersonal difficulty. (APA, DSM-IV, 1994)Libido: The psychic drive or energy associated with sexual instinct in the broad sense (pleasure and love-object seeking). It may also connote the psychic energy associated with instincts in general that motivate behavior.Testosterone: A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.Dydrogesterone: A synthetic progestational hormone with no androgenic or estrogenic properties. Unlike many other progestational compounds, dydrogesterone produces no increase in temperature and does not inhibit OVULATION.Sexual Dysfunction, Physiological: Physiological disturbances in normal sexual performance in either the male or the female.Immediate Dental Implant Loading: Endosseous dental implantation where implants are fitted with an abutment or where an implant with a transmucosal coronal portion is used immediately (within 1 week) after the initial extraction. Conventionally, the implantation is performed in two stages with more than two months in between the stages.Endocrinology: A subspecialty of internal medicine concerned with the metabolism, physiology, and disorders of the ENDOCRINE SYSTEM.Postmenopause: The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life.Orgasm: The climax of sexual excitement in either humans or animals.Menopause: The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.Brain Ischemia: Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.Hypoglycemia: A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.Ubiquitination: The act of ligating UBIQUITINS to PROTEINS to form ubiquitin-protein ligase complexes to label proteins for transport to the PROTEASOME ENDOPEPTIDASE COMPLEX where proteolysis occurs.Neuroprotective Agents: Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.Infarction, Middle Cerebral Artery: NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.Ischemic Attack, Transient: Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Neurons: 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.Ubiquitin: A highly conserved 76-amino acid peptide universally found in eukaryotic cells that functions as a marker for intracellular PROTEIN TRANSPORT and degradation. Ubiquitin becomes activated through a series of complicated steps and forms an isopeptide bond to lysine residues of specific proteins within the cell. These "ubiquitinated" proteins can be recognized and degraded by proteosomes or be transported to specific compartments within the cell.Rats, Sprague-Dawley: 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.Weight Loss: Decrease in existing BODY WEIGHT.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Body Weight: The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.Receptors, Adrenergic, alpha: One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.Diet, Reducing: A diet designed to cause an individual to lose weight.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Legislation, Veterinary: Laws and regulations, pertaining to the field of veterinary medicine, proposed for enactment or enacted by a legislative body.Paranoid Personality Disorder: A personality disorder characterized by the avoidance of accepting deserved blame and an unwarranted view of others as malevolent. The latter is expressed as suspiciousness, hypersensitivity, and mistrust.Trichiasis: A disease of the eye in which the eyelashes abnormally turn inwards toward the eyeball producing constant irritation caused by motion of the lids.Animal Rights: The moral and ethical bases of the protection of animals from cruelty and abuse. The rights are extended to domestic animals, laboratory animals, and wild animals.Cartoons as Topic: Images used to comment on such things as contemporary events, social habits, or political trends; usually executed in a broad or abbreviated manner.American Heart Association: A voluntary organization concerned with the prevention and treatment of heart and vascular diseases.Analgesia: Methods of PAIN relief that may be used with or in place of ANALGESICS.Repression, Psychology: The active mental process of keeping out and ejecting, banishing from consciousness, ideas or impulses that are unacceptable to it.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
(1/222) Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors.

The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors.  (+info)

(2/222) G-protein activation by putative antagonists at mutant Thr373Lys alpha2A adrenergic receptors.

1. Replacement of a threonine by a lysine at position 373 in the C-terminal portion of the third intracellular loop of the human alpha2A-adrenergic receptor (alpha2A AR) has been reported to generate a constitutively active mutant receptor in analogy with similar mutations in the alpha1B and beta2 AR (Ren et al., 1993). In the present study, the mutant Thr373Lys alpha2A AR receptor was investigated by measuring the formation of inositol phosphates in either the absence or presence of mouse G(alpha)15 protein in Cos-7 cells. 2. Increased affinity, potency and/or efficacy for the agonists [(-)-adrenaline, UK 14304, clonidine, guanabenz and oxymetazoline] was observed, consistent with a precoupled mutant alpha2A AR: G-protein state. The basal inositol phosphates response was similar at the wild-type (wt) and mutant alpha2A AR, but was enhanced at the mutant alpha2A AR upon co-expression with the mouse G(alpha)15 protein. This enhanced response could not be attenuated in the presence of any of the tested alpha2 AR antagonists (10 microM), suggesting that inverse agonist activity did not occur at the mutant alpha2A AR. 3. Ligands that so far have been identified as antagonists at the wt alpha2A AR demonstrated either no intrinsic activity (MK 912, WB 4101, RS 15385, RX 811059 and RX 821002) or positive efficacy [Emax, % vs. 1 microM UK 14304: dexefaroxan (27+/-7), idazoxan (34+/-9), atipamezole (27+/-4), BRL 44408 (59+/-5) and SKF 86466 (54+/-9)] at the mutant alpha2A AR, but only in the presence of the mouse G(alpha)15 protein. The ligand potencies corresponded with their respective pKi values at the mutant alpha2A AR receptor. 4. The partial agonist effect of SKF 86466 was resistant to pertussis toxin treatment (100 ng ml(-1)) and not affected by co-expression of the rat G(alpha)i1 protein. It was virtually absent in the presence of 10 microM RS 15385. SKF 86466 was without intrinsic activity upon co-expression of the mouse G(alpha)q protein. 5. Some putative alpha2 AR antagonists exerted a partial agonist activity that was highly dependent on the presence of specific G-protein alpha-subunits, suggesting that these ligands cause selective G-protein activation at the mutant alpha2A AR.  (+info)

(3/222) Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation.

The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory.  (+info)

(4/222) Effects of GABA on noradrenaline release and vasoconstriction induced by renal nerve stimulation in isolated perfused rat kidney.

We examined effects of gamma-aminobutyric acid (GABA) on vasoconstriction and noradrenaline (NA) release induced by electrical renal nerve stimulation (RNS) in the isolated pump-perfused rat kidney. RNS (1 and 2 Hz for 2.5 min each, 0.5-ms duration, supramaximal voltage) increased renal perfusion pressure (PP) and renal NA efflux. GABA (3, 10 and 100 microM) attenuated the RNS-induced increases in PP by 10-40% (P<0.01) and NA efflux by 10-30% (P<0.01). GABA did not affect exogenous NA (40 and 60 nM)-induced increases in PP. The selective GABA(B) agonist baclofen (3, 10 and 100 microM) also attenuated the RNS-induced increases in PP and NA efflux, whereas the RNS-induced responses were relatively resistant to the selective GABA(A) agonist muscimol (3, 10 and 100 microM). The selective GABA(B) antagonist 2-hydroxysaclofen (50 microM), but not the selective GABA(A) antagonist bicuculline (50 microM), abolished the inhibitory effects of GABA (10 microM) on the RNS-induced responses. The selective alpha2-adrenoceptor antagonist rauwolscine (10 nM) enhanced the RNS-induced responses. GABA (3, 10 and 100 microM) potently attenuated the RNS-induced increases in PP by 40-60% (P<0.01) and NA efflux by 20-50% (P<0.01) in the presence of rauwolscine. Prazosin (10 and 30 nM) suppressed the RNS-induced increases in PP by about 70-80%. Neither rauwolscine (10 nM) nor GABA (10 microM) suppressed the residual prazosin-resistant PP response. These results suggest that GABA suppresses sympathetic neurotransmitter release via presynaptic GABA(B) receptors, and thereby attenuates adrenergically induced vasoconstriction in the rat kidney.  (+info)

(5/222) Blocking effects of phentolamine on L-type calcium current and ATP-sensitive potassium current in guinea pig ventricular myocytes.

AIM: To study the effect of phentolamine on L-type calcium currents (ICa) and ATP-sensitive K+ currents (IK,ATP) in ventricular myocytes. METHODS: ICa and IK,ATP were observed using patch clamp techniques in whole-cell recording configuration. RESULTS: Phentolamine reduced ICa of ventricular myocytes in concentration-dependent and voltage-independent manners. Phentolamine 5, 25, and 100 mumol.L-1 decreased ICa from 370 +/- 99 nA to 310 +/- 95 nA (17% block, n = 6, P < 0.01), from 230 +/- 98 nA to 180 +/- 73 nA (23% block, n = 5, P < 0.05), and from 293 +/- 66 nA to 206 +/- 44 nA (30% block, n = 5, P < 0.01), respectively, without affecting the current-voltage relationship. Prazosin 100 mumol.L-1 and yohimbine 100 mumol.L-1, which were specific blockers of alpha 1 and alpha 2 adrenoceptors respectively, did not show the inhibitory effect on ICa. Phentolamine 100 mumol.L-1 also inhibited the IK,ATP induced by 2, 4-dinitrophenol (DNP) at 0 mV from 3.2 +/- 0.6 nA to 0.8 +/- 0.5 nA (75% block, n = 4, P < 0.01). CONCLUSION: Phentolamine directly inhibits ICa and IK,ATP in guinea pig ventricular myocytes.  (+info)

(6/222) Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors.

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters.  (+info)

(7/222) Electrochemical and electrophysiological characterization of neurotransmitter release from sympathetic nerves supplying rat mesenteric arteries.

1. Characteristic features of noradrenaline (NA) and adenosine 5'-triphosphate (ATP) release from postganglionic sympathetic nerves in rat small mesenteric arteries in vitro have been investigated on an impulse-by-impulse basis. NA release was measured using continuous amperometry and ATP release was monitored by intracellular recording of excitatory junction potentials (e.j.ps). 2. Electrical stimuli evoked transient increases in oxidation current. During trains of ten stimuli at 0.5 - 4 Hz there was a depression in the amplitude of oxidation currents evoked following the first stimulus in the train. 3. The neuronal NA uptake inhibitor, desmethylimipramine (1 microM), increased the amplitude of the summed oxidation current evoked by ten stimuli at 1 Hz and slowed the decay of oxidation currents evoked by trains of ten stimuli at 1 and 10 Hz. 4. The alpha2-adrenoceptor antagonist, idazoxan (1 microM), increased the amplitudes of the oxidation currents evoked during trains of ten stimuli at 0.5 - 10 Hz but had no effect on the oxidation currents evoked by the first stimulus in the train. 5. Idazoxan (1 microM) increased the amplitude of all e.j.ps evoked during trains of stimuli at 0.5 and 1 Hz. In addition, the facilitatory effect of idazoxan on e.j.ps was significantly greater than that on oxidation currents. 6. The findings indicate that NA release from sympathetic nerves supplying small mesenteric arteries is regulated by activation of presynaptic alpha2-adrenoceptors and that clearance of released NA in this tissue depends, in part, upon neuronal uptake. The different effects of idazoxan on the oxidation currents and e.j.ps may indicate that the release of NA and ATP is differentially modulated.  (+info)

(8/222) Enhanced cortical dopamine output and antipsychotic-like effects of raclopride by alpha2 adrenoceptor blockade.

Clozapine exerts superior clinical efficacy and markedly enhances cortical dopamine output compared with classical antipsychotic drugs. Here the alpha2 adrenoceptor antagonist idazoxan was administered to rats alone or in combination with the D2/3 dopamine receptor antagonist raclopride. Dopamine efflux in the medial prefrontal cortex and conditioned avoidance responding were analyzed. Idazoxan selectively potentiated the cortical output of dopamine and augmented the suppression of conditioned avoidance responding induced by raclopride. These results challenge basic assumptions underlying the dopamine hypothesis of schizophrenia and provide insight into clozapine's mode of action.  (+info)

*  Rauwolscine
... acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ...
*  List of veterinary drugs
... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists benazepril ... Crosses blood-brain barrier, useful in treatment of meningitis cimetidine - H2 antagonist used to reduce GI acid production ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses carprofen - COX-2 ... α2-adrenergic agonist (used to temporarily sedate animals) yohimbine - used to reverse effects of xylazine, also called an " ...
*  Olney's lesions
In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are ... Conversely, coadministration of NMDA-antagonists with alpha-2 adrenergic antagonists, like yohimbine could theoretically ... Jansen writes: Neuroscience portal NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J, Labruyere J, ... Olney's lesions, also known as NMDA receptor antagonist neurotoxicity (NAN), are a potential form of brain damage. They are ...
*  Yohimbine
... and D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... Yohimbine blocks the pre- and post-synaptic α2 receptors. Blockade of post-synaptic α2 receptors causes only minor corpus ...
*  Alpha-2A adrenergic receptor
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... ADRA2A adrenergic, alpha-2A-, receptor". "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union ... Handy DE, Gavras H (Nov 1992). "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological ...
*  Alpha-1 adrenergic receptor
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... Adrenergic receptor Graham, Robert (May 1, 1996). "α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling ...
*  Adrenergic antagonist
This drug is a non-selective α-adrenergic antagonist, which means it binds to both alpha receptors. There are few if any ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Adrenergic competitive antagonists are shorter lasting than the other two types of antagonists. While the antagonists for alpha ... There are few non-cardiovascular uses for adrenergic antagonists. Alpha-adrenergic antagonists are also used for treatment of ...
*  Alpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
*  Alpha-2 adrenergic receptor
... presumptively also mediated by α2 adrenergic receptors because it is reversed by yohimbine, an α2 antagonist. α2A selective ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ... adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. ...
*  Primary polydipsia
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ...
*  Alpha-1D adrenergic receptor
Antagonists A-315456 BMY 7378 (also α2C antagonist) Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000171873 - Ensembl, ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ...
*  Alpha-2C adrenergic receptor
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (1997). "A novel interaction between adrenergic receptors and the alpha-subunit ... Preferential coupling of the alpha 2C-adrenergic receptor to the guanine nucleotide-binding protein, Go". J. Biol. Chem. 267 ( ...
*  WB-4101
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H]WB4104 and [3H]prazosin binding. ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ... Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? Farmaco. 1998 Apr;53(4):278-86. ...
*  Beta-2 adrenergic receptor
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... denotes selective antagonist to the receptor. Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...
*  Beta-3 adrenergic receptor
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta Blocker GRCh38: Ensembl release 89: ...
*  Vascular smooth muscle
Antagonists of α 1 {\displaystyle \alpha _{1}} receptors (doxazosin, prazosin) cause vasodilation (i.e. decrease in vascular ... The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... receptors. Under NE binding α 1 {\displaystyle \alpha _{1}} receptors cause vasoconstriction (i.e. contraction of the vascular ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ...
*  Alpha-2 blocker
α2-blockers are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly ... Increases the noradrenaline release due to blockade of alpha-2 receptors. Historically, yohimbine was used as an aphrodisiac, ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ...
*  Niguldipine
... is a calcium channel blocker and a1-adrenergic receptor antagonist. Boer R, Grassegger A, Schudt C, Glossmann H ( ... May 1989). "(+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors". European ...
*  Glaucoma medication
Adrenergic antagonists (nonselective and selective Beta1-antagonists) Alpha 2 agonists Hyperosmotic agents Fotil is a ... a beta-adrenergic receptor antagonist Glaucoma Basic and clinical science course (2011-2012). Glaucoma. American Academy of ...
*  Beta-1 adrenergic receptor
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... β1-selective antagonists include: Acebutolol (in hypertension, angina pectoris and arrhythmias) Atenolol (in hypertension, ... The beta-1 adrenergic receptor (β1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the ... "GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation". The Journal ...
*  BMY-7,378
... is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ...
*  Efaroxan
... is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor. Fluparoxan Idazoxan Chopin P, ... "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions ...
*  Tetrahydropalmatine
... including alpha-1 adrenergic receptors, at which it functions as an antagonist, and GABA-A receptors, through positive ... alpha adrenergic and serotonin receptors. The Ki values for l-THP at D1 and D2 dopamine receptors are approximately 124 nM (D1 ... Along with dopamine receptors, l-THP has been reported to interact with a number of other receptor types, ... In the case of 5-HT1A receptors, l-THP binds with a Ki of approximately 340 nM. Animal experiments have shown that the sedative ...
*  Alpha blocker
However, the most common type of alpha blocker is usually an α1 blocker. Non-selective α-adrenergic receptor antagonists ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... "Alpha-Adrenoceptor Antagonists (Alpha-Blockers)" (PDF). British Hypertension Society. "CV Pharmacology , Alpha-Adrenoceptor ... Tamsulosin Terazosin Silodosin Selective α2-adrenergic receptor antagonists include: Atipamezole Idazoxan Mirtazapine Yohimbine ...
*  Pelanserin
... is an antagonist of the 5-HT2 and α1-adrenergic receptors. Villalobos-Molina, R; Ibarra, M; Hong, E (1995). "The 5- ... HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro". European Journal of ...
*  Cannabigerol
CBG has been found to act as a high affinity α2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and ... "Evidence that the plant cannabinoid cannabigerol is a highly potent alpha(2)-adrenoceptor agonist and moderately potent 5HT ... low affinity CB1 receptor antagonist. It also binds to the CB2 receptor as an antagonist. CBG does not trigger THC-like ... receptor antagonist". British Journal of Pharmacology. 159 (1): 129-141. doi:10.1111/j.1476-5381.2009.00515.x. PMC 2823359 . ...
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.  - PubMed - NCBI  3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. - PubMed - NCBI
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/6276200
The Role of Sympatho-vagal Balance on Different Limbs of Pain Perception in Healthy Subjects - Full Text View - ClinicalTrials...  The Role of Sympatho-vagal Balance on Different Limbs of Pain Perception in Healthy Subjects - Full Text View - ClinicalTrials...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Every subject will be invited to 2 separate sessions. At least 24 hours will apart the two sessions. The test in each session ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01621620?recr=Open&cond=%22Pain+Perception%22&rank=10
Studies of Opioid Seeking Behavior: Yohimbine and Hydrocortisone Effects - Full Text View - ClinicalTrials.gov  Studies of Opioid Seeking Behavior: Yohimbine and Hydrocortisone Effects - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Phase 2: Participants will then live on an inpatient research unit (located in Detroit Michigan) for at least 16 consecutive ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01536925?recr=Open&cond=%22Opioid-Related+Disorders%22&rank=3
Prophylactic Mirtazapine or Clonidine for Post-spinal Anesthesia Shivering - Full Text View - ClinicalTrials.gov  Prophylactic Mirtazapine or Clonidine for Post-spinal Anesthesia Shivering - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin ... Histamine H1 Antagonists. Histamine Antagonists. Histamine Agents. Anti-Anxiety Agents. Tranquilizing Agents. Adrenergic alpha- ... Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Each patient received 30 mg mirtazapine tablet and a placebo tablet for clonidine orally with sips of water 2 h preoperatively. ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT03679052?term=clonidine&rank=75
Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks.  Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks.
Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...
more infohttp://www.biomedsearch.com/nih/Role-adrenergic-alpha-2-receptors/19233186.html
US Neuropathic Pain Market Value Doubles to $5 Billion by 2018 - MASSAGE Magazine  US Neuropathic Pain Market Value Doubles to $5 Billion by 2018 - MASSAGE Magazine
... an opioid receptor agonist/norepinephrine reuptake inhibitor tapentadol (Ortho-McNeil); a dopamine receptor agonist sodium ... a sodium channel antagonist mexiletine (Boehringer Ingelheim); three glutamate / NMDA antagonists ketamine intranasal (Javelin ... an alpha-2 adrenergic receptor antagonist/norepinehrine reuptake inhibitor reboxetine (Pfizer); ... Eighteen drugs are in Phase III development in the US including two GABA receptor agonists pregabalin (Pfizer) and gabapentin ...
more infohttps://www.massagemag.com/us-neuropathic-pain-market-value-doubles-to-5-billion-by-2018-2299/
Yohimbe bark extract (Pausinystalia johimbe) | Plant Profiler | Sigma-Aldrich  Yohimbe bark extract (Pausinystalia johimbe) | Plant Profiler | Sigma-Aldrich
Assessment of alpha 2 adrenergic autoreceptor function in humans: effects of oral yohimbine. Life Sci 1982;30(23):2033-2041. ... It is significantly more active at presynaptic adrenoceptors than postsynaptic receptors. This action blocks the decrease in ... and peripherally to increase the release of norepinephrine from adrenergic nerve terminals. This increases the plasma ... Alpha 2-antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male ...
more infohttps://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/pausinystalia-johimbe.html
ChemIDplus - 367514-88-3 - NEKCRUIRPWNMLK-SCIYSFAVSA-N - Lurasidone hydrochloride [USAN] - Similar structures search, synonyms,...  ChemIDplus - 367514-88-3 - NEKCRUIRPWNMLK-SCIYSFAVSA-N - Lurasidone hydrochloride [USAN] - Similar structures search, synonyms,...
SEROTONIN 5-HT2 RECEPTOR ANTAGONIST, serotonin 5-HT7 receptor antagonist, and antagonist of the adrenergic ?2A and ?2C ... A thiazole derivative and atypical ANTIPSYCHOTIC AGENT that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST; ... and 5-HT7 Receptors as Well as Dopamine D2 Receptors) ... Adrenergic alpha-2 Receptor Antagonists. *. Adrenergic alpha- ... receptors, as well as a partial SEROTONIN 5-HT1A RECEPTOR AGONIST. It is used in the treatment of SCHIZOPHRENIA and BIPOLAR ...
more infohttps://chem.nlm.nih.gov/chemidplus/rn/367514-88-3
Evidence for the Role of Membrane Receptor Lateral Movement in GTP-Binding Protein-Mediated Signal Transduction | SpringerLink  Evidence for the Role of Membrane Receptor Lateral Movement in GTP-Binding Protein-Mediated Signal Transduction | SpringerLink
... direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified mem branes from human platelets. Implications of ... Role of fry subunits of G proteins in targeting the (3-adrenergic receptor kinase to membrane-bound receptors. Science 1992; ... multiple sites of regulation by 3-adrenergic receptor and Mg-' studied in reconstituted receptor-G, vesicles. J Biol Chem 1986 ...
more infohttps://link.springer.com/chapter/10.1007/978-1-4757-0680-2_5
A Category Names List - Drug Information Portal - U.S. National Library of Medicine  A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Adrenergic alpha-1 Receptor Antagonists (16) • Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. ... Adrenergic alpha-Antagonists (65) • Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the ... Adrenergic alpha-1 Receptor Agonists (7) • Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS. MeSH ... Adrenergic Antagonists (132) • Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the ...
more infohttps://druginfo.nlm.nih.gov/drugportal/drug/categories
A Category Names List - Drug Information Portal - U.S. National Library of Medicine  A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Adrenergic alpha-1 Receptor Antagonists (16) • Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. ... Adrenergic alpha-Antagonists (65) • Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the ... Adrenergic alpha-1 Receptor Agonists (7) • Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS. MeSH ... Adrenergic Antagonists (132) • Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the ...
more infohttps://druginfo.nlm.nih.gov/drugportal/jsp/drugportal/drugNamesAndCategories.jsp
Plus it  Plus it
The 5HT1 receptor-selective antagonist methiothepin, but not ketanserin (5HT2-selective) or ICS-205,930 (5HT3-selective), ... The nonselective alpha-adrenergic agonist oxymetazoline inhibits parathyroid hormone (PTH)-stimulated cAMP production in intact ... Desensitization of alpha 2-receptor-mediated inhibition of cAMP production by epinephrine did not alter the response to either ... a receptor in OK cells that is negatively coupled to adenylate cyclase but distinct from the alpha 2-adrenergic receptor. Prior ...
more infohttp://molpharm.aspetjournals.org/content/34/1/1
Boldine - Mr Supplement Australia  Boldine - Mr Supplement Australia
"Adrenergic Receptor Function in Fat Cells." Am J Clin Nutr. 55.1 (1992): 228S-36S.. (3) O'Brien P, Carrasco-Pozo C, Speisky H. ... 1)Eltze M, Grebe T, Michel MC, Czyborra P, Ullrich B. Affinity profile at alpha(1)- and alpha(2)-adrenoceptor subtypes and in ... Boldine has been shown to act as an alpha-2 adrenergic receptor antagonist. In English it's not that much simpler - boldine ... Furthermore, it is believed that the inactivation of these receptors, which are highly concentrated on fat cells, is something ...
more infohttps://www.mrsupplement.com.au/boldine-boldo-lindera
Rauvolscin - Википедија, слободна енциклопедија  Rauvolscin - Википедија, слободна енциклопедија
Perry BD, U'Prichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2- ... adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. PMID 6276200. doi:10.1016/0014-2999(81)90123-0.. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (1998). „[3H]Rauwolscine: an antagonist radioligand for the ...
more infohttps://sr.wikipedia.org/wiki/Rauvolscin
Table of Contents - August 01, 1990, 254 (2) | Journal of Pharmacology and Experimental Therapeutics  Table of Contents - August 01, 1990, 254 (2) | Journal of Pharmacology and Experimental Therapeutics
Prostaglandin synthesis elicited by adrenergic stimuli in rabbit aorta is mediated via alpha-1 and alpha-2 adrenergic receptors ... Adaptation of brain 5HT2 receptors after mianserin treatment: receptor sensitivity, not receptor binding, more accurately ... RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in ... Endothelin receptor-coupling mechanisms in vascular smooth muscle: a role for protein kinase C. N R Danthuluri and T A Brock ...
more infohttp://jpet.aspetjournals.org/content/254/2
Internet Scientific Publications  Internet Scientific Publications
It is a competitive selective Alpha-2 adrenergic receptor antagonist, which readily enters CNS, and has peripheral and central ... 2. Whereas both groups acknowledge that at least in the short term (6 months), testosterone therapy is safe, with only ... 2. Basson R. Women's Sexuality and Sexual Dysfunction. In: Gibbs RS, Karlan BY, Haney AF, Nygaard IE. Eds. Danforth's ... Menopause is associated with a variety of endocrine changes (1). These lead to a reduction in sexuality and well-being (2). The ...
more infohttp://ispub.com/IJGO/12/2/6043
Neurotransmitter Modulation of Neuronal Damage Following Cerebral Ischemia: Effects on Protein Ubiquitination | SpringerLink  Neurotransmitter Modulation of Neuronal Damage Following Cerebral Ischemia: Effects on Protein Ubiquitination | SpringerLink
Block, G.A., Pulsinelli, W.A. (1987) Excitatory amino acid receptor antagonists: Failure to prevent ischemic neuronal damage. J ... or post-treated with the non-competitive NMDA antagonist MK-801. In contrast, using an alpha 2-adrenergic receptor antagonist, ... using antagonist against the N-methyl-d-aspartate (NMDA) receptor. However, we have not been able to demonstrate a decrease in ... which cannot be blocked by noncompetitive NMDA receptor antagonist. This enhanced calcium entry can possibly be inhibited by ...
more infohttps://link.springer.com/chapter/10.1007/978-1-4684-5562-5_34
Rauwolscine - Wikipedia  Rauwolscine - Wikipedia
Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ...
more infohttps://en.wikipedia.org/wiki/Rauwolscine
Ipsen gives back rights to Santheras PD drug - PharmaTimes  Ipsen gives back rights to Santhera's PD drug - PharmaTimes
Santhera has regained the rights to fipamezole, its first-in-class selective adrenergic alpha-2 receptor antagonist for the ...
more infohttp://www.pharmatimes.com/news/ipsen_gives_back_rights_to_santheras_pd_drug_975846
Yohimbine - The Ultimate Guide: Dosage, Benefits & For Weight Loss  Yohimbine - The Ultimate Guide: Dosage, Benefits & For Weight Loss
1] Yohimbine is a powerful stimulant and alpha-2 adrenergic receptor antagonist. [2]. Yohimbine increases adrenaline levels in ... the blood and blocks these alpha-2 receptors, which turns the fat-burning switch from off' to on'. [3] Moderate doses of ... 2016. 2) Drug Record - Yohimbine (PAUSINYSTALIA YOHIMBE). LiverTox, United States National Library of Medicine, Sept. 2016, ... Muscletech Hydroxycut Hardcore Elite 28mg of yohimbine extract per 2 capsule serving ...
more infohttps://www.tigerfitness.com/articles/post/yohimbine-ultimate-guide
  • In June of that year, Raymond Ahlquist, Professor of Pharmacology at Medical College of Georgia, published a paper concerning adrenergic nervous transmission. (wikipedia.org)
  • In 1954, he was able to incorporate his findings in a textbook, Drill's Pharmacology in Medicine, and thereby promulgate the role played by α and β receptor sites in the adrenaline/noradrenaline cellular mechanism. (wikipedia.org)
  • PMID 3010073 Melchiorre C, Bolognesi ML, Budriesi R, Chiarini A, Giardinà D, Minarini A, Quaglia W, Leonardi A. Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? (wikipedia.org)
  • The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
  • Jans DA, Peters R, Fahrenholz F. Lateral mobility of the phospholipase-C-activating vasopressin V,-type receptor in A7r5 smooth muscle cells: a comparison with the adenylate cyclase-coupled V2-receptor. (springer.com)
  • Vasopressin V2-receptor mobile fraction and ligand-dependent adenylate cyclase-activity are directly correlated in LLC-PK, renal epithelial cells. (springer.com)
  • Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (springer.com)
  • Tolkovsky AM, Levitzki A. Coupling of a single adenylate cyclase to two receptors: adenosine and catecholamine. (springer.com)
  • Tolkovsky A, Braun S, Levitzki A. Kinetics of interaction between 3-receptors, GTP-proteins and the catalytic subunit of turkey erythrocyte adenylate cyclase. (springer.com)
  • Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)
  • Oxymetazoline inhibits adenylate cyclase by activation of serotonin-1 receptors in the OK cell, an established renal epithelial cell line. (aspetjournals.org)
  • After excluding several alternate hypotheses to explain this anomalous activity of oxymetazoline, we hypothesized that oxymetazoline activates a receptor in OK cells that is negatively coupled to adenylate cyclase but distinct from the alpha 2-adrenergic receptor. (aspetjournals.org)
  • These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (wikipedia.org)
  • Alpha blockers work by blocking the effect of nerves in the sympathetic nervous system. (wikipedia.org)
  • Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. (wikipedia.org)
  • In it, he explicitly named the different responses as due to what he called α receptors and β receptors, and that the only sympathetic transmitter was adrenaline. (wikipedia.org)
  • In the normal eye, beta-2 stimulation by salbutamol increases intraocular pressure via net: Increase in production of aqueous humour by the ciliary process, Subsequent increased pressure-dependent uveoscleral outflow of humour, despite reduced drainage of humour via the Canal of Schlemm. (wikipedia.org)
  • The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
  • Two yet to be launched products, Forest Laboratories/Cypress Biosciences's antidepressant milnacipran and Schwarz Pharma's sodium ion channel antagonist/CRMP2 modulator lacosamide (Vimpat), will compete for market share as well as provide the benefit of an additional mechanism of action. (massagemag.com)
  • Beta-2 adrenergic receptors have also been found to couple with Gi, possibly providing a mechanism by which response to ligand is highly localized within cells. (wikipedia.org)
  • Although both of the α receptors are GPCRs, there are large differences in their mechanism of action. (wikipedia.org)
  • Just as in A1 receptors, this normally serves as a protective mechanism, but may be destructive in altered cardiac function. (wikipedia.org)
  • Involvement of spinal kappa opioid receptors in the antinociception produced by intrathecally administered corticotropin-releasing factor in mice. (aspetjournals.org)
  • Reduced microcirculation together with adrenaline supersensitivity in organs such as liver can also be difficult problem when withdrawing from adrenergic blockers. (wikipedia.org)
  • However the development of more highly selective A2A ligands has led towards other applications, with the most significant focus of research currently being the potential therapeutic role for A2A antagonists in the treatment of Parkinson's disease. (wikipedia.org)
  • We envisage that the combination of glutamate and alpha-2 adrenergic antagonists could be potent therapies against neuronal damage following stroke and cardiac arrest. (springer.com)
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, drug addiction and Parkinson's disease. (wikipedia.org)
  • In such cases, beta-2 stimulation with its consequent increase in humour production is highly contra-indicated, and conversely, a topical beta-2 antagonist such as timolol may be employed. (wikipedia.org)