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Last update 08 May 2025

5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

Last update 08 May 2025

Basic Info

Drugs associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

Lisuride Maleate

Target

5-HT1A receptor x 5-HT2A receptor x 5-HT2B receptor x 5-HT2C receptor x D2 receptor

Mechanism

5-HT1A receptor agonists [+4]

Active Org.

Neuroventi Co., Ltd.

Originator Org.

Bayer Schering Pharma AG

Active Indication

Parkinson Disease [+2]

Inactive Indication

Restless Legs Syndrome

Drug Highest PhaseApproved

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

EUCTR2012-001675-37-AT

/ Not yet recruitingNot Applicable

A Prospective, Open-label, Exploratory Study to Investigate the Safety, Efficacy, and Haemodynamics of Lisuride Subcutaneous Infusion as Add-on to Conventional Treatment in Patients with Pulmonary Arterial Hypertension - Lis-Safe

Start Date07 Aug 2012

Sponsor / Collaborator

Sinoxa Pharma GmbH

NCT00408915

/ CompletedPhase 3

Double-blind, Placebo-controlled, Randomized, Multicentre Phase II/III Study to Evaluate the Efficacy and Safety of Lisuride, Applied Subcutaneously by Means of a Minipump in Patients With Advanced Parkinson's Disease Refractory to Conventional Oral Therapy

The aim of the study is to evaluate the long-term efficacy, local tolerability and safety of Lisuride applied as subcutaneous infusion compared to placebo in patients with advanced Parkinson's disease with motor fluctuations and "OFF" periods refractory to conventional treatment.

Start Date01 Jul 2006

Sponsor / Collaborator

axxonis Pharma AG

EUCTR2004-001589-42-AT

/ Unknown statusNot Applicable

Transdermal lisuride:Phase II/III study (efficacy and tolerance) of transdermal lisuride (patches) in patients with Restless Legs Syndrome (RLS)

Start Date25 Dec 2004

Sponsor / Collaborator-

100 Clinical Results associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

100 Translational Medicine associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

0 Patents (Medical) associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

Literatures (Medical) associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

01 Jan 2009·Journal of PsychopharmacologyQ3 · MEDICINE

Asenapine: a novel psychopharmacologic agent with a unique human receptor signature

Q3 · MEDICINE

Article

Author: Wong, Ehf ; Zorn, SH ; Shahid, M. ; Walker, GB

Asenapine is a novel psychopharmacologic agent under development for the treatment of schizophrenia and bipolar disorder. We determined and compared the human receptor binding affinities and functional characteristics of asenapine and several antipsychotic drugs. Compounds were tested under comparable assay conditions using cloned human receptors. In comparison with the antipsychotics, asenapine showed high affinity and a different rank order of binding affinities (p Ki) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT 5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (α1 [8.9], α2A [8.9], α2B [9.5] and α2C [8.9]), dopamine receptors (D1 [8.9], D 2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2]). It had much lower affinity (p Ki ≤ 5) for muscarinic receptors and was the only agent with affinity for H2 receptors. Relative to its D2 receptor affinity, asenapine had a higher affinity for 5-HT 2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT 6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaved as a potent antagonist (p KB) at 5-HT1A (7.4), 5-HT 1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT 2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors. These functional effects differed from those of risperidone (p KB < 5 for 5-HT6) and olanzapine (p KB < 5 for 5-HT 1A and α2). Our results indicate that asenapine has a unique human receptor signature, with binding affinity and antagonistic properties that differ appreciably from those of antipsychotic drugs.

01 Feb 2006·Biochemical PharmacologyQ2 · MEDICINE

Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms

Q2 · MEDICINE

Article

Author: Kowal, Dianne M. ; Nawoschik, Stanley P. ; Dunlop, John ; Zhang, Jean Y. ; Lou, Zhuangwei

In this study we have functionally characterized aripiprazole (OPC-14597; 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy-3,4-dihydro-2-(1H)-quinolinone), the prototype of a new generation antipsychotic drug termed dopamine-serotonin-system stabilizer, in cells expressing 5-hydroxytryptamine2 (5-HT2) receptor subtypes in comparison with olanzapine. In Chinese hamster ovary (CHO) cells stably expressing 5-HT2 receptors, aripiprazole displayed a dual agonist/antagonist profile for 5-HT2C receptor (VNI isoform) mediated calcium signaling (EC50 1070 nM, IC50 281 nM). It exhibited no appreciable 5-HT2A or 5-HT2B agonism, whereas it antagonized 5-HT-stimulated calcium increase at either 5-HT2A or 5-HT2B receptor expressed in CHO cells (IC50s of 369 and 0.46 nM, respectively). In comparison, olanzapine was devoid of agonism but was an antagonist at all three subtypes, with a potency rank order of 5-HT2A (IC50, 2.5 nM)>5-HT2B (47 nM)>5-HT2C (69 nM). In human embryonic kidney (HEK) cells transiently expressing 5-HT2C receptor isoforms, aripiprazole exhibited full agonism at the unedited INI, but partial agonism at the partially edited VNI and fully edited VSV isoforms (EC50s of 571, 1086 and 2099 nM, respectively). A partial antagonism was also observed for aripiprazole at the two edited isoforms (IC50s of 1138 and 1000 nM, respectively). In contrast, while lacking agonist activity at the VNI and VSV, olanzapine showed inverse agonism at the INI isoform (IC50 594 nM), reaching a maximal attenuation of 20%. In addition, olanzapine was a full antagonist at all three isoforms, with a rank order of potency of VNI (IC50, 79 nM)>VSV (101 nM)>INI (3856 nM). The modest 5-HT2A antagonism and 5-HT2C partial agonism, along with reported D2 and 5-HT1A partial agonism, may allow aripiprazole to stabilize the disturbed dopamine-serotonin interplay in schizophrenia with a moderate yet adequate pharmacological intervention. 5-HT2C agonism may also underlie the minimal weight gain seen with aripiprazole.

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5-HT1A receptor x 5-HT2C receptor x 5-HT2A receptor x D2 receptor x 5-HT2B receptor

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