Receptors, Serotonin, 5-HT1
Receptor, Serotonin, 5-HT1A
A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.
Serotonin Receptor Agonists
Serotonin 5-HT1 Receptor Agonists
Receptors, Dopamine D2
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.
Receptor, Serotonin, 5-HT1B
A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.
Receptor, Muscarinic M2
Medial Forebrain Bundle
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
Receptors, Dopamine D3
GABA-B Receptor Antagonists
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
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.
Serotonin 5-HT1 Receptor Antagonists
Receptor, Serotonin, 5-HT2B
Serotonin Uptake Inhibitors
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.
Receptors, Histamine H3
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Adrenergic alpha-2 Receptor Antagonists
Lysergic Acid Diethylamide
Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.
The middle of the three primitive cerebral vesicles of the embryonic brain. Without further subdivision, midbrain develops into a short, constricted portion connecting the PONS and the DIENCEPHALON. Midbrain contains two major parts, the dorsal TECTUM MESENCEPHALI and the ventral TEGMENTUM MESENCEPHALI, housing components of auditory, visual, and other sensorimoter systems.
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
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.
Norepinephrine Plasma Membrane Transport Proteins
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of noradrenergic neurons. They remove NOREPINEPHRINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. It regulates signal amplitude and duration at noradrenergic synapses and is the target of ADRENERGIC UPTAKE INHIBITORS.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
Receptor, Muscarinic M4
Dopamine Uptake Inhibitors
Receptors, Metabotropic Glutamate
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Dopamine Plasma Membrane Transport Proteins
Excitatory Amino Acid Antagonists
Excitatory Postsynaptic Potentials
Serotonin Plasma Membrane Transport Proteins
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SEROTONIN UPTAKE INHIBITORS.
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.
A furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.
Dose-Response Relationship, Drug
GABA-A Receptor Antagonists
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.
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.
Ovoid body resting on the CRIBRIFORM PLATE of the ethmoid bone where the OLFACTORY NERVE terminates. The olfactory bulb contains several types of nerve cells including the mitral cells, on whose DENDRITES the olfactory nerve synapses, forming the olfactory glomeruli. The accessory olfactory bulb, which receives the projection from the VOMERONASAL ORGAN via the vomeronasal nerve, is also included here.
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.
Receptors, Kainic Acid
Collection of pleomorphic cells in the caudal part of the anterior horn of the LATERAL VENTRICLE, in the region of the OLFACTORY TUBERCLE, lying between the head of the CAUDATE NUCLEUS and the ANTERIOR PERFORATED SUBSTANCE. It is part of the so-called VENTRAL STRIATUM, a composite structure considered part of the BASAL GANGLIA.
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.
Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (1/158)Patch-clamp recordings were performed from stellate and basket cells in rat cerebellar slices. Under somatic voltage clamp, short depolarizing pulses were applied to elicit action potentials in the axon. After the action potential, a bicuculline- and Cd2+-sensitive current transient was observed. A similar response was obtained when eliciting axonal firing by extracellular stimulation. With an isotonic internal Cl- solution, the peak amplitude of this current varied linearly with the holding potential, yielding an extrapolated reversal potential of -20 to 0 mV. Unlike synaptic or autaptic GABAergic currents obtained in the same preparation, the current transient had a slow rise-time and a low variability between trials. This current was blocked when 10 mM BAPTA was included in the recording solution. In some experiments, the current transient elicited axonal action potentials. The current transient was reliably observed in animals aged 12-15 d, with a mean amplitude of 82 pA at -70 mV, but was small and rare in the age group 29-49 d. Numerical simulations could account for all properties of the current transient by assuming that an action potential activates a distributed GABAergic conductance in the axon. The actual conductance is probably restricted to release sites, with an estimated mean presynaptic current response of 10 pA per site (-70 mV, age 12-15 d). We conclude that in developing rats, stellate and basket cell axons have a high density of GABAergic autoreceptors and that a sizable fraction of the corresponding current can be measured from the soma. (+info)
S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. (2/158)S-16924 is a potential antipsychotic that displays agonist and antagonist properties at serotonin (5-HT)1A and 5-HT2A/2C receptors, respectively. In a pigeon conflict procedure, the benzodiazepine clorazepate (CLZ) increased punished responses, an action mimicked by S-16924, whereas the atypical antipsychotic clozapine and the neuroleptic haloperidol were inactive. Similarly, in a Vogel conflict paradigm in rats, CLZ increased punished responses, an action shared by S-16924 but not by clozapine or haloperidol. This action of S-16924 was abolished by the 5-HT1A antagonist WAY-100,635. Ultrasonic vocalizations in rats were inhibited by CLZ, S-16924, clozapine, and haloperidol. However, although WAY-100,635 abolished the action of S-16924, it did not affect clozapine and haloperidol. In a rat elevated plus-maze, CLZ, but not S-16924, clozapine, and haloperidol, increased open-arm entries. Like CLZ, S-16924 increased social interaction in rats, whereas clozapine and haloperidol were inactive. WAY-100,635 abolished this action of S-16924. CLZ, S-16924, clozapine, and haloperidol decreased aggressive interactions in isolated mice, but this effect of S-16924 was not blocked by WAY-100, 635. All drugs inhibited motor behavior, but the separation to anxiolytic doses was more pronounced for S-16924 than for CLZ. Finally, in freely moving rats, CLZ and S-16924, but not clozapine and haloperidol, decreased dialysis levels of 5-HT in the nucleus accumbens: this action of S-16924 was blocked by WAY-100,165. In conclusion, in contrast to haloperidol and clozapine, S-16924 possessed a broad-based profile of anxiolytic activity at doses lower than those provoking motor disruption. Its principal mechanism of action was activation of 5-HT1A (auto)receptors. (+info)
In vivo assessment of the midbrain raphe nuclear regulation of serotonin release in the hamster suprachiasmatic nucleus. (3/158)Serotonin (5-HT) plays important regulatory roles in mammalian circadian timekeeping; however, little is known concerning the regulation of serotonergic activity in the circadian clock located in the suprachiasmatic nuclei (SCN). By using in vivo microdialysis to measure 5-HT release we demonstrated that electrical or pharmacological stimulations of the dorsal or median raphe nuclei (DRN and MRN, respectively) can alter basal release of 5-HT in the hamster SCN. There were similar increases in SCN 5-HT release after electrical stimulation of either the MRN or DRN, indicating that both could contribute to the serotonergic activity in the SCN. Systemic pretreatment with the 5-HT antagonist metergoline abolished DRN-induced SCN 5-HT release but had little effect on MRN-induced SCN 5-HT release, suggesting different pathways for these nuclei in regulating 5-HT output in the SCN. Microinjections of the 5-HT1A autoreceptor agonist 8-OH-DPAT or antagonist WAY 100635 into the MRN caused significant inhibition and stimulation of SCN 5-HT release, respectively. Both drugs had substantially less effect in the DRN. These differential drug actions indicate that somatodendritic 5-HT1A autoreceptors on MRN neurons provide the prominent raphe autoregulation of 5-HT output in the SCN. Collectively the current results are evidence that DRN as well as MRN neurons can contribute to the regulation of 5-HT release in the hamster SCN. On the basis of the current observations and those from recent anatomic tracing studies of serotonergic projections to SCN it is hypothesized that DRN input to the SCN could be mediated by a DRN --> MRN --> SCN pathway involving a 5-HT-sensitive multisynaptic interaction between the DRN and MRN neurons. (+info)
Comparison of antagonist potencies at pre- and post-synaptic GABA(B) receptors at inhibitory synapses in the CA1 region of the rat hippocampus. (4/158)Synaptic activation of gamma-aminobutyric acid (GABA)B receptors at GABA synapses causes (a) postsynaptic hyperpolarization mediating a slow inhibitory postsynaptic potential/current (IPSP/C) and (b) presynaptic inhibition of GABA release which depresses IPSPs and leads to paired-pulse widening of excitatory postsynaptic potentials (EPSPs). To address whether these effects are mediated by pharmacologically identical receptors the effects of six GABA(B) receptor antagonists of widely ranging potencies were tested against each response. Monosynaptic IPSP(B)s were recorded in the presence of GABA(A), AMPA/kainate and NMDA receptor antagonists. All GABA(B) receptor antagonists tested depressed the IPSP(B) with an IC50 based rank order of potency of CGP55679> or =CGP56433 = CGP55845A = CGP52432>CGP51176>CGP36742. Paired-pulse EPSP widening was recorded as an index of paired-pulse depression of GABA-mediated IPSP/Cs. A similar rank order of potency of antagonism of paired-pulse widening was observed to that for IPSP(B) inhibition. Comparison of the IC50 values for IPSP(B) inhibition and paired-pulse EPSP widening revealed a close correlation between the two effects in that their IC50s lay within the 95% confidence limits of a correlation line that described IC50 values for inhibition of paired-pulse EPSP widening that were 7.3 times higher than those for IPSP(B) inhibition. Using the compounds tested here it is not possible to assign different subtypes of GABA(B) receptor to pre- and post-synaptic loci at GABAergic synapses. However, 5-10 fold higher concentrations of antagonist are required to block presynaptic as opposed to postsynaptic receptors when these are activated by synaptically released GABA. (+info)
Diurnal variation in 5-HT1B autoreceptor function in the anterior hypothalamus in vivo: effect of chronic antidepressant drug treatment. (5/158)1. Intracerebral microdialysis was used to examine the function of the terminal 5-hydroxytryptamine (5-HT) autoreceptor in the anterior hypothalamus of anaesthetized rats at two points in the light phase of the light-dark cycle. 2. Infusion of the 5-HT1A/1B agonist 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridyl)-1H-indole (RU24969) 0.1, 1.0 and 10 microM through the microdialysis probe led to a concentration-dependent decrease (49, 56 and 65% respectively) in 5-HT output. The effect of RU24969 (1 and 5 microM) was prevented by concurrent infusion of methiothepin (1 and 10 microM) into the anterior hypothalamus via the microdialysis probe. Infusion of methiothepin alone (1.0 and 10 microM) increased (15 and 142% respectively) 5-HT output. 3. Infusion of RU24969 (5 microM) through the probe at mid-light and end-light resulted in a quantitatively greater decrease in 5-HT output at end-light compared with mid-light. 4. Following treatment with either paroxetine hydrochloride (10 mg kg(-1) i.p.) or desipramine hydrochloride (10 mg kg)(-1) i.p.) for 21 days the function of the terminal 5-HT1B autoreceptor was more markedly attenuated at end-light. 5. The data show that, as defined by the response to RU24969, the function of the 5-HT1B receptors that control 5-HT output in the anterior hypothalamus is attenuated following chronic desipramine or paroxetine treatment in a time-of-day-dependent manner. (+info)
Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (6/158)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)
Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. (7/158)alpha2-Adrenergic receptor (AR)-selective compounds produce antihypertensive and antinociceptive effects. Moxonidine alleviates hypertension in multiple species, including humans. This study demonstrates that intrathecally administered moxonidine produces antinociception in mice. Antinociception was detected via the (52.5 degrees C) tail-flick and Substance P (SP) nociceptive tests. Moxonidine was intrathecally administered to ICR, mixed C57BL/6 x 129/Sv [wild type (WT)], or C57BL/6 x 129/Sv mice with dysfunctional alpha2aARs (D79N-alpha2a). The alpha2AR-selective antagonist SK&F 86466 and the mixed I1/alpha2AR-selective antagonist efaroxan were tested for inhibition of moxonidine-induced antinociception. Moxonidine prolonged tail-flick latencies in ICR (ED50 = 0.5 nmol; 0. 3-0.7), WT (0.17 nmol; 0.09-0.32), and D79N-alpha2a (0.32 nmol; 0. 074-1.6) mice. Moxonidine inhibited SP-elicited behavior in ICR (0. 04 nmol; 0.03-0.07), WT (0.4 nmol; 0.3-0.5), and D79N-alpha2a (1.1 nmol; 0.7-1.7) mice. Clonidine produced antinociception in WT but not D79N-alpha2a mice. SK&F 86466 and efaroxan both antagonized moxonidine-induced inhibition of SP-elicited behavior in all mouse lines. SK&F 86466 antagonism of moxonidine-induced antinociception implicates the participation of alpha2ARs. The comparable moxonidine potency between D79N-alpha2a and WT mice suggests that receptors other than alpha2a mediate moxonidine-induced antinociception. Conversely, absence of clonidine efficacy in D79N-alpha2a mice implies that alpha2aAR activation enables clonidine-induced antinociception. When clinically administered, moxonidine induces fewer side effects relative to clonidine; moxonidine-induced antinociception appears to involve a different alpha2AR subtype than clonidine-induced antinociception. Therefore, moxonidine may prove to be an effective treatment for pain with an improved side effect profile. (+info)
Characterization of binding sequences for butyrolactone autoregulator receptors in streptomycetes. (8/158)BarA of Streptomyces virginiae is a specific receptor protein for a member of butyrolactone autoregulators which binds to an upstream region of target genes to control transcription, leading to the production of the antibiotic virginiamycin M(1) and S. BarA-binding DNA sequences (BarA-responsive elements [BAREs]), to which BarA binds for transcriptional control, were restricted to 26 to 29-nucleotide (nt) sequences on barA and barB upstream regions by the surface plasmon resonance technique, gel shift assay, and DNase I footprint analysis. Two BAREs (BARE-1 and BARE-2) on the barB upstream region were located 57 to 29 bp (BARE-1) and 268 to 241 bp (BARE-2) upstream from the barB translational start codon. The BARE located on the barA upstream region (BARE-3) was found 101 to 76 bp upstream of the barA start codon. High-resolution S1 nuclease mapping analysis revealed that BARE-1 covered the barB transcription start site and BARE-3 covered an autoregulator-dependent transcription start site of the barA gene. Deletion and mutation analysis of BARE-2 demonstrated that at least a 19-nt sequence was required for sufficient BarA binding, and A or T residues at the edge as well as internal conserved nucleotides were indispensable. The identified binding sequences for autoregulator receptor proteins were found to be highly conserved among Streptomyces species. (+info)
An autoreceptor is a type of receptor located in the membranes of nerve cells. It serves as part of a negative feedback loop in ... Autoreceptors may be located in any part of the cell membrane: in the dendrites, the cell body, the axon, or the axon terminals ... The D2sh autoreceptor has been shown recently to interact with the trace amine-assorted receptor 1 (TAAR1), a G-Coupled Protein ... Autoreceptors are usually G protein-coupled receptors (rather than transmitter-gated ion channels) and act via a second ...
Monoamine autoreceptors (e.g., D2 short, presynaptic α2, and presynaptic 5-HT1A) have the opposite effect of TAAR1, and ... TAAR1 forms GPCR oligomers with monoamine autoreceptors in neurons in vivo. These and other reported TAAR1 hetero-oligomers ... Notably, amphetamine and trace amines possess high binding affinities for TAAR1, but not for monoamine autoreceptors. The ... enhancement by monoamine transporters and attenuation by the D2 autoreceptor in vitro". The Journal of Pharmacology and ...
Monoamine autoreceptors (e.g., D2 short, presynaptic α2, and presynaptic 5-HT1A) have the opposite effect of TAAR1, and ... Notably, amphetamine and trace amines possess high binding affinities for TAAR1, but not for monoamine autoreceptors. Imaging ...
Muscarinic acetylcholine receptor M2
They appear to serve as autoreceptors. In addition, they modulate muscarinic potassium channels. In the heart, this contributes ... Douglas CL, Baghdoyan HA, Lydic R (December 2001). "M2 muscarinic autoreceptors modulate acetylcholine release in prefrontal ...
... stimulating autoreceptors, inhibiting neurotransmitter release; 7) blocking autoreceptors, increasing neurotransmitter release ...
... an autoreceptor heteromer) D4-adrenoceptor α1B D4-adrenoceptor β1 Dopamine receptor D1 and Dopamine receptor D5 are Gs coupled ... autoreceptors, which regulate neurotransmission via feedback mechanisms. It affects synthesis, storage, and release of dopamine ...
Muscarinic acetylcholine receptor M4
They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the ... The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit ...
Autoreceptor Millan, M. J.; Lejeune, F.; Gobert, A. (2000). "Reciprocal autoreceptor and heteroreceptor control of serotonergic ... they are opposite to autoreceptors, which are sensitive only to neurotransmitters or hormones released by the cell in whose ...
List of Japanese inventions and discoveries
Bennett M (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clin Auton Res. 9 (3): 145-59. doi:10.1007 ...
List of multiple discoveries
Bennett MR (June 1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): ...
Bennett MR (June 1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): ...
Waters N, Lagerkvist S, Löfberg L, Piercey M, Carlsson A (September 1993). "The dopamine D3 receptor and autoreceptor ... Aretha CW, Sinha A, Galloway MP (August 1995). "Dopamine D3-preferring ligands act at synthesis modulating autoreceptors". The ... Lahti AC, Weiler M, Carlsson A, Tamminga CA (1998). "Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)- ... and an antagonist at D2Sh autoreceptors on dopaminergic nerve terminals. This causes dopamine release in the brain and has a ...
1900 in science
Bennett, M. (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): 145- ...
ISBN 978-0-19-828802-2. Bennett M (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clin Auton Res. 9 ...
Bennett MR (June 1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic Research. 9 (3): ...
History of catecholamine research
ISBN 0-444-80493-5. M. R. Bennett (1999). "One hundred years of adrenaline: the discovery of autoreceptors". Clinical Autonomic ... Klaus Starke (2001). "Presynaptic autoreceptors in the third decade: focus on α2-adrenoceptors". Journal of Neurochemistry. 78 ... presynaptic α-autoreceptors. Their existence was initially combated but is now established, for example by the demonstration of ...
Histamine H3 receptor
H3 receptors function as presynaptic autoreceptors on histamine-containing neurons. The diverse expression of H3 receptors ... where they act as autoreceptors in presynaptic histaminergic neurons and control histamine turnover by feedback inhibition of ...
Biology of depression
One possible explanation for this lag is that the neurotransmitter activity enhancement is the result of auto receptor ... Hjorth, S; Bengtsson, HJ; Kullberg, A; Carlzon, D; Peilot, H; Auerbach, SB (June 2000). "Serotonin autoreceptor function and ... The therapeutic effect of antidepressants is thought to arise from autoreceptor desensitization over a period of time, ... as firing of serotonergic neurons in the dorsal raphe adapt via the activity of 5-HT1A autoreceptors. ...
... while SRAs will initially bypass autoreceptors, the increase in serotonin they induce will then agonise autoreceptors.] In ... This autoreceptor-mediated inhibition of serotonin release has been theorized to be a major factor in the therapeutic lag that ... The autoreceptors must first desensitize before the concentration of extracellular serotonin in the synapse can become elevated ... 5-HT1A autoreceptor desensitization and increased 5-HT1A receptor postsynaptic activation via general increases in serotonin ...
This is likely due to preferential activation of D2/D3 autoreceptors versus postsynaptic receptors, the latter of which ... an extremely potent stimulant of dopamine autoreceptors". Brain Research. 231 (1): 109-16. doi:10.1016/0006-8993(82)90011-7. ...
Zoe R. Donaldson
In Hen's lab, Donaldson probed the role of the Serotonin 1A autoreceptor in behavior. She first examined how suppression of 5- ... "Developmental Effects of Serotonin 1A Autoreceptors on Anxiety and Social Behavior". Neuropsychopharmacology. 39 (2): 291-302. ...
Agonist Receptor antagonist Autoreceptor Kenakin T (April 2004). "Principles: receptor theory in pharmacology". Trends in ...
Adrenergic nerve fibre
In the brain, all autoreceptors appear to be of the α2 type. (The drug idazoxan blocks α2 autoreceptors and hence acts as an ... Adrenergic neurons, in particular the α2 autoreceptors found in the brain, are also involved in sexual behavior and in the ...
Ford, CP (Jan 23, 2004). "The role of D2-autoreceptors in regulating dopamine neuron activity and transmission". Neuroscience. ... considered to be mostly present at inhibitory D2 autoreceptor locatations) relative to the D2L form, sufficiently low partial ...
Gründer G, Wetzel H, Hammes E, Benkert O (1993). "Roxindole, a dopamine autoreceptor agonist, in the treatment of major ... Maj J, Kołodziejczyk K, Rogóz Z, Skuza G (March 1997). "Roxindole, a dopamine autoreceptor agonist with a potential ... Klimke A, Klieser E (July 1991). "Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results ... Bartoszyk GD, Harting J, Minck KO (January 1996). "Roxindole: psychopharmacological profile of a dopamine D2 autoreceptor ...
The latter was thus demonstrated to be an autoreceptor on cells that release dopamine. TAAR1 is a presynaptic intracellular ... Dopamine autoreceptors also regulate DAT by directly opposing the effect of TAAR1 activation. The human dopamine transporter ( ... receptor that is also colocalized with DAT and which has the opposite effect of the D2 autoreceptor when activated; i.e., it ...
Development and discovery of SSRI drugs
This delay is caused by the time it takes 5-HT to downregulate 5-HT1A autoreceptors and turn on the neuro impulse flow of the 5 ... When these 5-HT1A autoreceptors have been downregulated, they will no longer restrict the impulse flow of the 5-HT neuron. The ... desensitized somatodendritic 5-HT1A autoreceptors, (4) turned on the impulse flow and (5) increased the release of 5-HT from ... This increase in 5-HT concentration causes desensitization of somatodendritic 5-HT1A autoreceptors. ...
They function as autoreceptors in the brain and decrease the release of serotonin. The anxiolytic drug Buspirone acts as ...
It also appears to serve as a presynaptic serotonin autoreceptor. The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) ... Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566-577. doi:10.1016 ...
Dopamine receptor D2
The short form (D2Sh) is pre-synaptic and functions as an autoreceptor that regulates the levels of dopamine in the synaptic ... In flies, activation of the D2 autoreceptor protected dopamine neurons from cell death induced by MPP+, a toxin mimicking ... OSU-6162 - also 5-HT2A partial agonist, acts as "dopamine stabilizer" Roxindole (only at the D2 autoreceptors) RP5063 ... presynaptic autoreceptors) Amisulpride (low doses) UH-232 Homocysteine - negative allosteric modulator PAOPA SB-269,652 SB- ...
Autoreceptors | Harvard Catalyst Profiles | Harvard Catalyst
"Autoreceptors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Autoreceptors" by people in Harvard Catalyst Profiles by year ... Loss of feedback inhibition via D2 autoreceptors enhances acquisition of cocaine taking and reactivity to drug-paired cues. ... ß-adrenoceptor blockers increase cardiac sympathetic innervation by inhibiting autoreceptor suppression of axon growth. J ...
Sex-dependent adaptive changes in serotonin-1A autoreceptor function and anxiety in Deaf1-deficient mice | Molecular Brain |...
Despite a sustained increase in 5-HT1A autoreceptor binding levels, the amplitude of the 5-HT1A autoreceptor-mediated current ... The sex dependence of Deaf1 function in mice is consistent with a greater role for 5-HT1A autoreceptors in sensitivity to ... These data show that altered 5-HT1A autoreceptor regulation in male Deaf1-/- mice can be compensated for by generational ... Consistent with increased 5-HT1A autoreceptor function in vivo, hypothermia induced by the 5-HT1A agonist DPAT was augmented in ...
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Fluoxetine alone induced a trend towards desensitization of 5-HT1A autoreceptors as shown by a reduction in the effect of 8-OH- ... Effects of triiodothyronine and fluoxetine on 5-HT1A and 5-HT1B autoreceptor activity in rat brain: regional differences.. ... The combination of fluoxetine and T3 induced desensitization of 5-HT1B autoreceptors in hypothalamus. Since there is evidence ... DPAT to lower 5-HT levels in frontal cortex, and desensitized 5-HT1B autoreceptors in frontal cortex. ...
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Over the course of a month, it stops producing more autoreceptors, the existing autoreceptors gradually degrade, and ... the cell notices there is way more autoreceptor activity than expected and assumes it is producing too many autoreceptors. ... Why dont the autoreceptors notice the original problem - that you have too little serotonin and are depressed - and work their ... Maybe after a month, the cells have lost some confidence in the autoreceptors, but theyre still keeping serotonin somewhere ...
Yawning Induced by the Selective Dopamine D2 Agonist N-0437 is Blocked by the Selective Dopanrine Autoreceptor Antagonist (+)- ... autoreceptor sensitivity would be expected to decline. As a result, behavioral responses mediated by dopamine autoreceptors ... In small doses, it has been reported to act preferentially at dopamine autoreceptors. We have observed that at 0.3 mg/kg IP, N- ... The responses were blocked by the highly selective dopamine autoreceptor antagonist, (+)-UH 232 (3.0 mg/kg), but not by ...
Dopamine D2 Receptors in Dopaminergic Neurons Modulate Performance in a Reversal Learning Task in Mice | eNeuro
To clarify the role of the latter pool, namely, D2 autoreceptors, we studied mice carrying a conditional DRD2 gene, with or ... Together, these findings confirm the role of D2 autoreceptors in reversal learning and suggest a broader involvement in ... The present work provides evidence that D2 autoreceptors alone influence the performance in a task measuring impulsivity in ... We found that autoDrd2-KO mice lacking D2 autoreceptors tend to display relatively poorer reversal learning capacities, ...
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- However, identifying the role of these receptors is complicated by the existence of both postsynaptic D2 receptors and presynaptic autoreceptors, which inhibit dopamine release. (nih.gov)
- The action of N-0437 to elicit yawning is therefore stereoselective, and requires agonis t activity at presynaptic autoreceptors involved in the control of dopamine release to induce the behavioral effect. (baillement.com)
- Stimulation of midbrain M4 autoreceptors are thought to decrease the activity of dopaminergic neurons in ventral tegmental area neurons, leading to reduced dopamine release in the nucleus accumbens. (nih.gov)
- IRP researchers led by Veronica A. Alvarez, Ph.D. , addressed the challenge using a newly available transgenic mouse model with selective deletion of dopamine D2 receptors in the same neurons that release dopamine into the forebrain-autoreceptors that provide negative feedback regulation over dopamine release. (nih.gov)
- This, and other preclinical pharmacology work, shows that autoreceptor and heteroreceptor populations of these receptors have divergent roles in modulating depression-related behavior as well as responses to antidepressants and also have different functions during early postnatal development compared to during adulthood. (nih.gov)
- The responses were blocked by the highly selective dopamine autoreceptor antagonist, (+)-UH 232 (3.0 mg/kg), but not by raclopride at a dose which selectively blocks postsynaptic D2 receptors. (baillement.com)
- N-0437 acts as an agonist at both pre- and postsynaptic dopamine receptors, while (+)N-0437 behaves as an antagonist at autoreceptors involved in the release of dopamine, and as a weak antagonist at postsynaptic dopamine receptors. (baillement.com)
- Researchers from McMaster University, Dalhousie University, and the University of Toronto conducted a systematic review and meta-analysis of 14 trials enrolling 3,085 patients and included the use of armodafinil, modafinil, solriamfetol, and pitolisant-H3-autoreceptor antagonist. (eurekalert.org)
- Hence, in the present report, we examined the effectiveness of one dopamine autoreceptor antagonist, (+)-UH 232, in blocking the responses to a small dose of a selective dopamipe agonist. (baillement.com)
- Using a novel, selective dopamine autoreceptor antagonist, (+ )-UH 232, the present results provide strong confirmation of the view that yawning and stretching responses elicited by N-0437 are mediated by dopamine autoreceptors. (baillement.com)
- Despite a sustained increase in 5-HT1A autoreceptor binding levels, the amplitude of the 5-HT1A autoreceptor-mediated current in 5-HT neurons was unaltered in Deaf1-/- mice, suggesting compensatory changes in receptor function. (biomedcentral.com)
- In addition, presynaptic GABA(B) autoreceptors are present on the terminals of spiny projection neurons and/or striatal GABAergic interneurons. (ox.ac.uk)
- The present work provides evidence that D2 autoreceptors alone influence the performance in a task measuring impulsivity in mice, suggesting that impulsivity is not only resulting from dysfunctional striato-pallidal neurons but also might also be modulated by upstream, presynaptic events. (eneuro.org)
- We have observed that at 0.3 mg/kg IP, N-0437 induced hypomotility, which is indicative of autoreceptor activation, whilst at 1.0 and 3.0 mg/kg it produced mild forms of behavioral stereotypy (sniffing, oral activity) which denote postsynaptic receptor-mediated effects. (baillement.com)
- 11. Acute 5-HT₁A autoreceptor knockdown increases antidepressant responses and serotonin release in stressful conditions. (nih.gov)
- In this study, Deaf1-/- mice bred on a mixed C57BL6-BALB/c background were compared to wild-type littermates for 5-HT1A autoreceptor function and behavior in males and females. (biomedcentral.com)
- Consistent with increased 5-HT1A autoreceptor function in vivo , hypothermia induced by the 5-HT1A agonist DPAT was augmented in early generation male but not female Deaf1-/- mice, but was reduced with succeeding generations. (biomedcentral.com)
- These data show that altered 5-HT1A autoreceptor regulation in male Deaf1-/- mice can be compensated for by generational adaptation of receptor response that may help to normalize behavior. (biomedcentral.com)
- The sex dependence of Deaf1 function in mice is consistent with a greater role for 5-HT1A autoreceptors in sensitivity to depression in men. (biomedcentral.com)
- Littermate wild type and D2 autoreceptor knockout mice (autoD2 KO) were trained for 15 days on a cued-operant task in which one nose poke earned an intravenous infusion of cocaine. (nih.gov)
- They discovered that a reduction in D2 autoreceptors enhanced the likelihood that mice would engage in cocaine use, which also made them more vulnerable to cocaine in an animal model of relapse. (nih.gov)
- To clarify the role of the latter pool, namely, D2 autoreceptors, we studied mice carrying a conditional DRD2 gene, with or without Cre-recombinase expressed under the transcriptional control of the dopamine transporter gene locus (autoDrd2-KO, n = 19 and controls, n = 21). (eneuro.org)
- Rhesus monkey trace amine-associated receptor 1 signaling: enhancement by monoamine transporters and attenuation by the D2 autoreceptor in vitro. (harvard.edu)
- Autoreceptors" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
- Distinct regulation of dopamine D2S and D2L autoreceptor signaling by calcium. (harvard.edu)
- Loss of feedback inhibition via D2 autoreceptors enhances acquisition of cocaine taking and reactivity to drug-paired cues. (harvard.edu)
- The NIH writes, "(the study's) findings will provide a detailed understanding of the relationship between neurotensin, DA neuron activity and meth self-administration and will lay the foundation for therapeutics targeting neurotensinand autoreceptor-mediated signaling. (paisano-online.com)
- Together, these findings confirm the role of D2 autoreceptors in reversal learning and suggest a broader involvement in behavioral inhibition mechanisms. (eneuro.org)
- One means to determine the mechanism by which dopamine agonists elicit yawning and the other responses would be to use selective dopamine autoreceptor antagonists to see if the response to the agonists could be blocked. (baillement.com)
- In addition, the inhibition of stimulation-dependent release may occur because of D2 autoreceptor activation by DA that is released via reverse transport. (amphetamines.com)
- When D2 autoreceptor activation was minimal, the combined effects of AMPH on DA release and uptake resulted in an enhanced overflow of exocytically released DA. (amphetamines.com)
- Differential effects of GABAB autoreceptor activation on ethanol potentiation of local and lateral paracapsular GABAergic synapses in the rat basolateral amygdala. (bvsalud.org)
- The rs6295 risk allele prevents binding of the repressor Deaf1 increasing 5-HT1A receptor gene transcription, and the Deaf1-/- mouse model shows an increase in 5-HT1A autoreceptor expression. (biomedcentral.com)
- 9. Loss of Adult 5-HT1A Autoreceptors Results in a Paradoxical Anxiogenic Response to Antidepressant Treatment. (nih.gov)
- Furthermore, these illnesses are treated with antidepressant drugs that enhance 5-HT neurotransmission, but chronic treatment is required despite their rapid entry in the brain, suggesting a role for adaptive changes in 5-HT1A autoreceptor function in antidepressant response [ 20 ]. (biomedcentral.com)
- This graph shows the total number of publications written about "Autoreceptors" by people in Harvard Catalyst Profiles by year, and whether "Autoreceptors" was a major or minor topic of these publication. (harvard.edu)
- RGS4-dependent attenuation of M4 autoreceptor function in striatal cholinergic interneurons following dopamine depletion. (harvard.edu)
- It has been proposed that these effects are due to selective agonist activity at dopamine autoreceptors , although evidence against this view has also been put forward. (baillement.com)
- 12. 5-HT1A autoreceptor levels determine vulnerability to stress and response to antidepressants. (nih.gov)
- Conversely, an increase in 5-HT1A autoreceptors would lead to increased susceptibility to depression by reducing serotonergic activity [ 3 - 6 ]. (biomedcentral.com)
- Solanto instructed that stimulants may activate uational cues and to modulate the depth of their behav- presynaptic inhibitory autoreceptors and should lead to re- ior. (ehd.org)
- Rate of learning of the initial discrimination and latencies to collect rewards, to initiate trials and to produce a response were unaffected by genetic deletion of D2 autoreceptors, discarding possible motor and motivational factors. (eneuro.org)
- The researchers involved in the UTHSC study hoped to identify the cellular mechanisms involved in methamphetamine addiction, including autoreceptor signaling, which decreases as a result of methamphetamine addiction. (paisano-online.com)
- ß-adrenoceptor blockers increase cardiac sympathetic innervation by inhibiting autoreceptor suppression of axon growth. (harvard.edu)
- Although many investigators have proposed that small doses of dopamine agonïsts elicit yawning through a selective action at dopamine autoreceptors, there has been dissent from this view. (baillement.com)