*  Substituted pyrazoles - Patent # 7417046 - PatentGenius
... s and 1H-indazoles and their affinity for benzodiazepine receptors," Chemical Abstracts No. (CAN) 122:314528 (1994) 8:126-131. ... Fce Receptor I on Dendritic Cells Delivers IgE-Bound Multivalent Antigens into a Cathepsin S-Dependent Pathway of MHC Class II ... Nerenberg, J.B. et al., "Design and Synthesis of N-Alkylated Saccharins as Selective .alpha.-1A Adrenergic Receptor Antagonists ... Andronati, "Synthesis of 3-aryl-1-[4-phenyl-1-piperazinyl)butyl]iondazole derivatives and their affinity to 5-HT1A serotonin ...
  http://www.patentgenius.com/patent/7417046.html
*  Bifeprunox - Wikipedia
... piperazines as potential atypical antipsychotics sharing dopamine D2-receptor and serotonin 5-HT1A-receptor affinities". Bioorg ... Bifeprunox and other novel atypical antipsychotics will instead of antagonizing D2 receptors, will act as partial agonists, as ... combines minimal D2 receptor agonism with serotonin receptor agonism. It was under development for the treatment of ... 2007). "Pharmacological profiles in rats of novel antipsychotics with combined dopamine D2/serotonin 5-HT1A activity: ...
  https://en.wikipedia.org/wiki/Bifeprunox
*  Aripiprazole | SpringerLink
Aripiprazole is a quinolinone derivative with a high affinity for dopamine D2 and D3 receptors, and serotonin 5-HT1a, 5-HT2A ... Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. ... Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther ... The main active metabolite, dehydro-aripiprazole, has affinity for dopamine D2 receptors and thus has some pharmacological ...
  https://link.springer.com/article/10.2165%2F00003495-200464150-00010
*  Plus it
Binding affinities (pKi) for serotonin receptor agonists and antagonists at different receptors involved in gastrointestinal ... which included various serotonin receptors and dopamine D2 receptor, by radioligand competition binding assays, according to ... receptors but moderate to no affinity for other relevant serotonin receptors (i.e., 5-HT1B, 5-HT1D, 5-HT3, and 5-HT4; pKi , ... We found that a compound known as SF-2 has micromolar affinities for dopamine D2 receptor (pKi = 6.08) and 5-HT1A receptor (pKi ...
  http://jpet.aspetjournals.org/content/338/3/917
*  Citric acid Mediated One-pot Regioselective Synthesis of N-Alkylated Indazoles: An Efficient Green Strategy
2005) Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists. Bioorganic ... a Norepinephrine/Serotonin reuptake inhibitor for the treatment of Fibromyalgia. Organic Process Research & Development 12: 877 ... indazole derivatives and their affinity to 5-HT1A serotonin and dopamine D1 receptors. Die Pharmazie 54: 99-101. ... 3. Ethyl 2-(5-chloro-1H-indazol-1-yl)acetate (4c): Colourless oil, Yield=94%, 1H NMR (300 MHz): δ 8.05 (s, 1H, arom H), 7.72 (d ...
  http://green-chemistry.imedpub.com/citric-acid-mediated-onepot-regioselectivesynthesis-of-nalkylated-indazoles-anefficient-green-strategy.php?aid=20672
*  Full text] Profile of aripiprazole in the treatment of bipolar disorder in childr | AHMT
... as well as a partial agonist of the serotonin 5-HT1A and dopamine D2 receptors. It can be safely used in children and ... Aripiprazole acts as a serotonin 5-HT2A receptor antagonist, ... Affinity for dopamine D2 receptors and intrinsic activity. ... that block histamine and serotonin 5HT receptors. It has also been suggested that the 5HT2C receptor agonist m-chlorophenyl ... Aripiprazole affinity at serotonin 5HT receptors. Aripiprazole also demonstrates high affinity at serotonin 5-HT1A and 5-HT2A ...
  https://www.dovepress.com/profile-of-aripiprazole-in-the-treatment-of-bipolar-disorder-in-childr-peer-reviewed-fulltext-article-AHMT
*  Lisuride - Wikipedia
It has a high affinity for the dopamine D2, D3 and D4 receptors, as well as serotonin 5-HT1A and 5-HT2A/C receptors. While ... 2008). "Identification of a serotonin/glutamate receptor complex implicated in psychosis". Nature. 452 (7183): 93-7. doi: ... Lisuride is a dopamine and a partial agonist for several serotonin receptors. It is an antagonist at the serotonin 5-HT2B ... a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction ...
  https://en.wikipedia.org/wiki/Lisuride
*  Archiv der Pharmazie - organic-reaction.com
... both p-xylyl and benzyl derivatives had the highest affinity for the dopamine D2 receptor (i.e., 16 out of 24 compounds ... of Carboxamide/Sulfonamide Replacement in Arylpiperazinylalkyl Derivatives on Activity to Serotonin and Dopamine Receptors () A ... analogs were prepared and tested for their affinity to bind to serotonin 5-HT1A/5-HT6/5-HT7 and dopamine D2 receptors. This ... piperazine analogs were tested for their affinity to the serotonin 5-HT1A/5-HT6/5-HT7 and dopamine D2 receptors, allowing ...
  https://www.organic-reaction.com/organic-and-medicinal-chemistry-news/archiv-der-pharmazie/
*  ChemIDplus - 367514-88-3 - NEKCRUIRPWNMLK-SCIYSFAVSA-N - Lurasidone hydrochloride [USAN] - Similar structures search, synonyms,...
A thiazole derivative and atypical ANTIPSYCHOTIC AGENT that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST; SEROTONIN 5-HT2 ... Treatment of Schizophrenia (High-Affinity Agonist of Serotonin 5-HT1A, 5-HT2, and 5-HT7 Receptors as Well as Dopamine D2 ... 2C receptors, as well as a partial SEROTONIN 5-HT1A RECEPTOR AGONIST. It is used in the treatment of SCHIZOPHRENIA and BIPOLAR ... RECEPTOR ANTAGONIST, serotonin 5-HT7 receptor antagonist, and antagonist of the adrenergic ?2A and ? ...
  https://chem.nlm.nih.gov/chemidplus/rn/367514-88-3
*  Mazapertine - Wikipedia
It exerts its pharmacological effect through affinity for dopamine D2, serotonin 5-HT1A, and α1-adrenergic receptors. ... "Orally Active Benzamide Antipsychotic Agents with Affinity for Dopamine D2, Serotonin 5-HT1A, and Adrenergic α1Receptors". ... Baxter, Ellen W.; Reitz, Allen B. (1997). "Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A ... receptor". Bioorganic & Medicinal Chemistry Letters. 7 (7): 763. doi:10.1016/S0960-894X(97)00074-7. ...
  https://en.wikipedia.org/wiki/Mazapertine
*  Amesergide - Wikipedia
... and dopamine D1 and D2 receptors (Ki = 150-730 nM). It has negligible affinity for the histamine H1 and muscarinic ... Amesergide (INN, USAN; developmental code name LY-237733) is a serotonin receptor antagonist of the ergoline and lysergamide ... Leopoldo M (2004). "Serotonin(7) receptors (5-HT(7)Rs) and their ligands". Curr. Med. Chem. 11 (5): 629-61. PMID 15032609. Marc ... Amesergide also has affinity for the serotonin 5-HT1D receptor (Ki = 57.9 nM) and lower affinity for the serotonin 5-HT1A, α1- ...
  https://en.wikipedia.org/wiki/Amesergide
*  Amphetamine - Wikipedia
Amphetamine addiction is largely mediated through increased activation of dopamine receptors and co-localized NMDA receptors in ... inhibits dopamine reuptake and amplifies amphetamine-induced dopamine efflux in vitro. The human serotonin transporter and ... The human dopamine transporter (hDAT) contains an endogenous high affinity Zn2+ binding site with three coordinating residues ... and induces increased dopamine receptor D2 (DRD2) density in the striatum. This is the opposite of pathological stimulant use, ...
  https://en.wikipedia.org/wiki/Amphetamine
*  "Synthesis of Novel Aporphine-Inspired Neuroreceptor Ligands" by Nirav R. Kapadia
... serotonin receptors (5-HT1A and 5-HT7) and α adrenergic receptors. Aporphines are also inhibitors of the acetylcholinesterase ... Considering the diverse profile of aporphine alkaloids at CNS receptors they can be considered as ... Within the Central Nervous Systems (CNS), aporphine alkaloids are known to possess high affinity for several clinically ... valuable targets including dopamine receptors (predominantly D1 and D2), ...
  https://academicworks.cuny.edu/gc_etds/792/
*  Vilazodone (Professional Patient Advice) - Drugs.com
Vilazodone inhibits CNS neuron serotonin uptake; minimal or no effect on reuptake of norepinephrine or dopamine. It also binds ... selectively with high affinity to 5-HT1A receptors and is a 5-HT1A receptor partial agonist. 5-HT1A receptor activity may be ... Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome ... Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant ...
  https://www.drugs.com/ppa/vilazodone.html
*  Use of atypical antipsychotic drugs in old age psychiatry | BJPsych Advances
It has stronger dopamine antagonism at the D1 and D4 receptors relative to its affinity for the D2 receptor, which may explain ... Quetiapine acts as an antagonist at multiple neurotransmitter receptors in the brain, including dopamine D1 and D2, serotonin 5 ... HT1A and 5-HT2, histaminic H1 and α1- and α2-adrenergic receptors. Quetiapine exhibits a lower binding affinity to D2 than to 5 ... It also has affinity for α1-adenergic receptors and lower affinity for α2-adrenergic and H1-histaminergic receptors. Unlike ...
  http://apt.rcpsych.org/content/8/1/49.full
*  Osemozotan - Wikipedia
1-(2-pyrimidinyl)-piperazine has affinity for receptors other than 5-HT1A, decreasing its specificity and increasing the risk ... Ago, Y.; Nakamura, S.; Baba, A.; Matsuda, T. (2008). "Neuropsychotoxicity of abused drugs: effects of serotonin receptor ... dopamine, or adrenergic receptors. With repeated exposure of Osemozotan at the 5-HT1A receptors, there seems to be no change in ... a serotonin 1A-receptor agonist, on methamphetamine-induced c-Fos expression in prefrontal cortical neurons". Biological & ...
  https://en.wikipedia.org/wiki/Osemozotan
*  3H-spiroperidol binding in human temporal cortex (brodmann areas 41-42) occurs at multiple high affinity states with...
3H-Spiroperidol labels multiple high affinity states with serotonergic selectivity in human prefrontal cortex and with ... Decreased serotonin S2 and increased dopamine D2 receptors in chronic schizophrenics. Biol Psychiatry 21:1407-1414Google ... 2 receptor, while a third affinity state may represent the 5-HT1A receptor. ... Altar CA, Kim H, Marshall JF (1985) Computer imaging and analysis of dopamine (D2) and serotonin (S2) binding sites in rat ...
  https://link.springer.com/article/10.1007/BF00589902
*  Aripiprazole Tablets (Aripiprazole Tablets): Side Effects, Interactions, Warning, Dosage & Uses
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors (Ki values of 0.34 nM, 0.8 nM ... which has been shown to have affinities for D2 receptors similar to the parent drug and represents 40% of the parent drug ... In healthy human volunteers administered 0.5 to 30 mg/day aripiprazole for 14 days, there was dose-dependent D2 receptor ... HT1A, and 5-HT2A may explain some of the other clinical effects of aripiprazole (e.g., the orthostatic hypotension observed ...
  https://www.rxlist.com/aripiprazole-tablets-drug.htm
*  Brexpiprazole - Wikipedia
It is a dopamine D2 receptor partial agonist and has been described as a "serotonin-dopamine activity modulator" (SDAM). The ... and α2C-adrenergic receptors. The drug has negligible affinity for the muscarinic acetylcholine receptors, and hence has no ... September 2014). "Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator". J. ... "Preclinical Pharmacology of Brexpiprazole (Opc-34712): A Novel Compound with Dopamine D2 Receptor Partial Agonist Activity". ...
  https://en.wikipedia.org/wiki/Brexpiprazole
*  MIN-117 - Wikipedia
... and is also reported to possess affinity for the α1A- and α1B-adrenergic receptors. As of May 2015, MIN-117 is in phase II ... "Presynaptic Selectivity of a Ligand for Serotonin 1A Receptors Revealed by In Vivo PET Assays of Rat Brain". PLoS ONE. 7 (8): ... It is described as a 5-HT1A and 5-HT2A receptor antagonist and inhibitor of serotonin and dopamine reuptake, ...
  https://en.wikipedia.org/wiki/MIN-117
*  Aristada (Aripiprazole Lauroxil Extended-release Injection): Side Effects, Interactions, Warning, Dosage & Uses
Aripiprazole exhibits high affinity for dopamine D2 and D3 (Kis 0.34 and 0.8 nM respectively), serotonin 5-HT1A and 5-HT2A ... receptors (Kis 1.7 and 3.4 nM respectively), moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic ... Aripiprazole may cause orthostatic hypotension, perhaps due to its α1-adrenergic receptor antagonism. Associated adverse ... and moderate affinity for the serotonin reuptake site (Ki 98 nM). Aripiprazole has no appreciable affinity for cholinergic ...
  https://www.rxlist.com/aristada-drug.htm
*  Inverse Agonist Actions of Typical and Atypical Antipsychotic Drugs at the Human 5-Hydroxytryptamine2C Receptor | Journal of...
2A serotonin receptors and relatively low affinities for D2-dopamine receptors. It has recently been proposed that these ... 1991) Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature (Lond) ... 1995) D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs. ... 1995) Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J ...
  http://jpet.aspetjournals.org/content/299/1/83.long
*  General Information | John T. Williams, Ph.D. | OHSU People | OHSU
"Depression of serotonin synaptic transmission by the dopamine Precursor L-DOPA." Cell Reports In: , Vol. 12, No. 6, 2015, p. ... "Increased agonist affinity at the μ-opioid receptor induced by prolonged agonist exposure." Journal of Neuroscience In: , Vol. ... "Activation of μ-opioid receptors and block of K IR3 potassium channels and NMDA receptor conductance by l- and d-methadone in ... "Cocaine Decreases Metabotropic Glutamate Receptor mGluR1 Currents in Dopamine Neurons by Activating mGluR5." ...
  http://www.ohsu.edu/people/john-t-williams/AFE02BBACAFF2527F18B1D57F1EF8044
*  DFL23448, A Novel Transient Receptor Potential Melastin 8-Selective Ion Channel Antagonist, Modifies Bladder Function and...
... muscarinic receptors (M2, M3), neurokinin-1 receptor, opioid receptors (δ, κ, µ), opioid receptor like-1, serotonin 5-HT1A ... receptor, cannabinoid CB2 receptor, dopamine receptors (D2, D3), and bradykinin BK1 receptor was determined by radioligand ... Evaluation of the affinity of DFL23448 for human adrenoceptors (α1A, α2A, β1, β2), histamine receptors (H1, H2, M2), ... transient receptor potential ankyrin. TRPM8. transient receptor potential melastin 8 ion channel. TRPV. transient receptor ...
  http://jpet.aspetjournals.org/content/356/1/200
*  Aripiprazole (Abilify) Full Prescribing Information | HealthyPlace
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors (Ki values of 0.34 nM, 0.8 nM ... which has been shown to have affinities for D2 receptors similar to the parent drug and represents 40% of the parent drug ... In healthy human volunteers administered 0.5 to 30 mg/day aripiprazole for 14 days, there was dose-dependent D2 receptor ... moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors (Ki values of 44 nM ...
  https://www.healthyplace.com/other-info/psychiatric-medications/aripiprazole-abilify-full-prescribing-information