| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Emma D Deek. Flibanserin: First Global Approval. Drugs. vol 75. issue 15. 2016-07-29. PMID:26412054. |
the drug has a high affinity for serotonin 5-ht1a and 5-ht2a receptors (5-ht1a agonist/5-ht2a antagonist) and is believed to treat hsdd by increasing levels of dopamine and noradrenaline and lowering levels of serotonin in the brain. |
2016-07-29 |
2023-08-13 |
Not clear |
| Claire Chevreuil, Elisabeth Polard, Eric Lemonnier, Paul Guillemot, Danièle Bentué-Ferre. [Not Available]. Therapie. vol 66. issue 2. 2016-07-12. PMID:27393647. |
its mechanism of action is different as aripiprazole is a partial dopamine d2 and serotonin 5-ht1a receptor agonist and 5-ht2a receptor antagonist. |
2016-07-12 |
2023-08-13 |
Not clear |
| Haydyn Lloyd, Chao Den. Interaction of Dopamine D2 and 5-HT1A Receptor Partial Agonism on Antipsychotic Efficacy. Journal of clinical psychopharmacology. vol 36. issue 2. 2016-06-30. PMID:26848788. |
interaction of dopamine d2 and 5-ht1a receptor partial agonism on antipsychotic efficacy. |
2016-06-30 |
2023-08-13 |
Not clear |
| Ling Huang, Wenjun Zhang, Xiaohua Zhang, Lei Yin, Bangyin Chen, Jinchun Son. Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. Bioorganic & medicinal chemistry letters. vol 25. issue 22. 2016-06-28. PMID:26483200. |
the present study describes the optimization of a series of novel benzoxazole-piperidine (piperazine) derivatives combining high dopamine d2 and serotonin 5-ht1a, 5-ht2a receptor affinities. |
2016-06-28 |
2023-08-13 |
human |
| Sarah L Grei. Brexpiprazole: First Global Approval. Drugs. vol 75. issue 14. 2016-06-24. PMID:26310190. |
brexpiprazole is a novel serotonin-dopamine activity modulator that acts as a partial agonist of serotonin 1a (5-ht1a) and dopamine d2 receptors, as well as a potent antagonist of 5-ht2a receptors and noradrenergic α1b and α2c receptors. |
2016-06-24 |
2023-08-13 |
Not clear |
| Joseph McEvoy, Leslie Citrom. Brexpiprazole for the Treatment of Schizophrenia: A Review of this Novel Serotonin-Dopamine Activity Modulator. Clinical schizophrenia & related psychoses. vol 9. issue 4. 2016-05-12. PMID:26757416. |
brexpiprazole acts as a partial agonist at dopamine d2 and serotonin 5-ht1a receptors, and as an antagonist at serotonin 5-ht2a and at adrenergic alpha1b and alpha2c receptors. |
2016-05-12 |
2023-08-13 |
Not clear |
| Agnieszka Zagórska, Marcin Kołaczkowski, Adam Bucki, Agata Siwek, Grzegorz Kazek, Grzegorz Satała, Andrzej J Bojarski, Anna Partyka, Anna Wesołowska, Maciej Pawłowsk. Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity. European journal of medicinal chemistry. vol 97. 2016-04-12. PMID:25965777. |
a spectrum of receptor activities was observed for compounds with a substituent at the 7-position of the imidazo[2,1-f]purine-2,4-dione system and some potent 5-ht1a (18, 25), 5-ht7 (14) and mixed 5-ht1a/5-ht7 (8, 9) receptor ligands with additional affinity for dopamine d2 receptors (15) has been identified. |
2016-04-12 |
2023-08-13 |
Not clear |
| Shigeru Hasebe, Naoki Hiramatsu, Yukio Ago, Kazuya Mori, Yuji Watabe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsud. Role of the 5-HT1A autoreceptor in the enhancement of fluvoxamine-induced increases in prefrontal dopamine release by adrenalectomy/castration in mice. Journal of pharmacological sciences. vol 127. issue 2. 2016-02-29. PMID:25727963. |
role of the 5-ht1a autoreceptor in the enhancement of fluvoxamine-induced increases in prefrontal dopamine release by adrenalectomy/castration in mice. |
2016-02-29 |
2023-08-13 |
mouse |
| Shigeru Hasebe, Naoki Hiramatsu, Yukio Ago, Kazuya Mori, Yuji Watabe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsud. Role of the 5-HT1A autoreceptor in the enhancement of fluvoxamine-induced increases in prefrontal dopamine release by adrenalectomy/castration in mice. Journal of pharmacological sciences. vol 127. issue 2. 2016-02-29. PMID:25727963. |
we have found that fluvoxamine-induced increases in prefrontal dopamine release are enhanced by adrenalectomy/castration and 5-ht1a receptors are involved in the enhancement. |
2016-02-29 |
2023-08-13 |
mouse |
| Shigeru Hasebe, Naoki Hiramatsu, Yukio Ago, Kazuya Mori, Yuji Watabe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsud. Role of the 5-HT1A autoreceptor in the enhancement of fluvoxamine-induced increases in prefrontal dopamine release by adrenalectomy/castration in mice. Journal of pharmacological sciences. vol 127. issue 2. 2016-02-29. PMID:25727963. |
adrenalectomy/castration-induced enhancement of fluvoxamine-induced increase in the dopamine release was not blocked by local perfusion with the 5-ht1a receptor antagonist way100635 (10 μm), while it was blocked by systemic administration of way100635 at low dose (0.1 mg/kg) which blocked preferentially autoreceptor-mediated responses. |
2016-02-29 |
2023-08-13 |
mouse |
| Shigeru Hasebe, Naoki Hiramatsu, Yukio Ago, Kazuya Mori, Yuji Watabe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsud. Role of the 5-HT1A autoreceptor in the enhancement of fluvoxamine-induced increases in prefrontal dopamine release by adrenalectomy/castration in mice. Journal of pharmacological sciences. vol 127. issue 2. 2016-02-29. PMID:25727963. |
these finding suggests that 5-ht1a autoreceptors play a key role in the enhancement of prefrontal dopamine release. |
2016-02-29 |
2023-08-13 |
mouse |
| Anna Czopek, Marcin Kołaczkowski, Adam Bucki, Hanna Byrtus, Maciej Pawłowski, Grzegorz Kazek, Andrzej J Bojarski, Agata Piaskowska, Justyna Kalinowska-Tłuścik, Anna Partyka, Anna Wesołowsk. Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent. Bioorganic & medicinal chemistry. vol 23. issue 13. 2016-02-26. PMID:25936259. |
a series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-ht1a, 5-ht2a, 5-ht7 and dopamine d2 receptors. |
2016-02-26 |
2023-08-13 |
mouse |
| Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Adam Bucki, Marcin Kołaczkowski, Maciej Pawłowski, Grzegorz Satała, Andrzej J Bojarski, Anna Partyka, Anna Wesołowska, Elżbieta Pękala, Karolina Słoczyńsk. New arylpiperazinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and dihydro[1,3]oxazolo[2,3-f]purinedione targeting the serotonin 5-HT1A /5-HT2A /5-HT7 and dopamine D2 receptors. Archiv der Pharmazie. vol 348. issue 4. 2016-01-21. PMID:25773907. |
new arylpiperazinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and dihydro[1,3]oxazolo[2,3-f]purinedione targeting the serotonin 5-ht1a /5-ht2a /5-ht7 and dopamine d2 receptors. |
2016-01-21 |
2023-08-13 |
mouse |
| Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Adam Bucki, Marcin Kołaczkowski, Maciej Pawłowski, Grzegorz Satała, Andrzej J Bojarski, Anna Partyka, Anna Wesołowska, Elżbieta Pękala, Karolina Słoczyńsk. New arylpiperazinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and dihydro[1,3]oxazolo[2,3-f]purinedione targeting the serotonin 5-HT1A /5-HT2A /5-HT7 and dopamine D2 receptors. Archiv der Pharmazie. vol 348. issue 4. 2016-01-21. PMID:25773907. |
to obtain potential antidepressants and/or antipsychotics, a series of new long-chain arylpiperazine derivatives of 8-alkoxy-purine-2,6-dione (10-24) and dihydro[1,3]oxazolo[2,3-f]purinedione (30-34) were synthesized and their serotonin (5-ht1a , 5-ht2a , 5-ht6 , 5-ht7 ) and dopamine (d2 ) receptor affinities were determined. |
2016-01-21 |
2023-08-13 |
mouse |
| Satoko Baba, Takeshi Murai, Tomokazu Nakako, Takeshi Enomoto, Michiko Ono, Isao Shimizu, Kazuhito Iked. The serotonin 5-HT₁A receptor agonist tandospirone improves executive function in common marmosets. Behavioural brain research. vol 287. 2016-01-19. PMID:25804359. |
the results of this study also indicate that the putative mechanism of action of tandospirone might be related to enhancement of dopamine neurotransmission via activation of the 5-ht1a receptor. |
2016-01-19 |
2023-08-13 |
Not clear |
| Antony Loebel, Leslie Citrom. Lurasidone: a novel antipsychotic agent for the treatment of schizophrenia and bipolar depression. BJPsych bulletin. vol 39. issue 5. 2016-01-12. PMID:26755968. |
in addition to full antagonist activity at dopamine d2 (k i(d2) = 1 nm) and serotonin 5-ht2a (k i(5-ht2a) = 0.5 nm) receptors, the pharmacodynamic profile of lurasidone is notable for its high affinity for serotonin 5-ht7 receptors (k i(5-ht7) = 0.5 nm) and its partial agonist activity at 5-ht1a receptors (k i(5-ht1a) = 6.4 nm). |
2016-01-12 |
2023-08-13 |
Not clear |
| Tamaki Ishima, Takashi Futamura, Yuta Ohgi, Noriko Yoshimi, Tetsuro Kikuchi, Kenji Hashimot. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. vol 25. issue 4. 2016-01-11. PMID:25687838. |
the selective 5-ht1a receptor antagonist, way-100,635, was able to block the effects of brexpiprazole on neurite outgrowth, unlike the selective dopamine d2 receptor antagonist, raclopride. |
2016-01-11 |
2023-08-13 |
Not clear |
| Masaru Ihara, Asuka Inoue, Seiya Hanamoto, Han Zhang, Junken Aoki, Hiroaki Tanak. Detection of physiological activities of G protein-coupled receptor-acting pharmaceuticals in wastewater. Environmental science & technology. vol 49. issue 3. 2015-12-04. PMID:25556879. |
we applied the in vitro transforming growth factor-α (tgfα) shedding assay, which accurately and sensitively detect gpcr activation, to investigate the agonistic/antagonistic activities of wastewater extracts against receptors for angiotensin (at1), dopamine (d2, d4), adrenergic family members (α1b, α2a, β1, β3), acetylcholine (m1, m3), cannabinoid (cb1), vasopressin (v1a, v2), histamine (h1, h2, h3), 5-hydroxytryptamine (5-ht1a, 5-ht2c), prostanoid (ep3), and leukotriene (blt1). |
2015-12-04 |
2023-08-13 |
Not clear |
| Beate Schmitz, Christoph Ullmer, Daniel Segelcke, Mirella Gwarek, Xin-Ran Zhu, Hermann Lübber. BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. European journal of pharmacology. vol 751. 2015-12-01. PMID:25666387. |
in comparison to pimethixene, it lacked high affinities to 5-ht1a, 5-ht2a, 5-ht2c, histamine h1, dopamine d1 and d2 as well as muscarinic m1 and m2 receptors. |
2015-12-01 |
2023-08-13 |
human |
| Anna Partyka, Grażyna Chłoń-Rzepa, Anna Wasik, Magdalena Jastrzębska-Więsek, Adam Bucki, Marcin Kołaczkowski, Grzegorz Satała, Andrzej J Bojarski, Anna Wesołowsk. Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT₁A receptor functional profile. Bioorganic & medicinal chemistry. vol 23. issue 1. 2015-10-22. PMID:25435254. |
continuing our earlier study in a group of purine-2,6-dione derivatives of long chain arylpiperazines (lcaps), a series of 8-unsubstituted 7-phenylpiperazin-4-yl-alkyl (4-14) and 7-tetrahydroisoquinolinyl-alkyl (15-17) analogues were synthesized and their serotonin 5-ht1a, 5-ht2a, 5-ht6, 5-ht7 and dopamine d2 receptor affinities were determined. |
2015-10-22 |
2023-08-13 |
mouse |