The anxiolytic-like profile of the nociceptin receptor agonist, endo-8-[bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octane-3-carboxamide (SCH 655842): Comparison of efficacy and side effects across rodent species

2011 ◽  
Vol 661 (1-3) ◽  
pp. 63-71 ◽  
Author(s):  
Sherry X. Lu ◽  
Guy A. Higgins ◽  
Robert A. Hodgson ◽  
Lynn A. Hyde ◽  
Robert A. Del Vecchio ◽  
...  
Keyword(s):  
Side Effects ◽  
Receptor Agonist ◽  
Rodent Species ◽  
Nociceptin Receptor

Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics Aspects of Lorcaserin, a Selective Serotonin 5-HT2C Receptor Agonist: An Update

2020 ◽  
Vol 20 (9) ◽  
pp. 768-778
Author(s):  
Sanjay Sharma ◽  
Komal S. Aware ◽  
Ketan Hatware ◽  
Kiran Patil
Keyword(s):  
Side Effects ◽  
Receptor Agonist ◽  
Scale Up ◽  
Mass Spectrometric ◽  
Selective Serotonin ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Step Method ◽  
Comprehensive Information ◽  
Tissue Matrix ◽  
Liquid Chromatographic

This review refers to the all-inclusive details of Lorcaserin Hydrochloride on comprehensive information about the synthesis, analytical methods, pharmacodynamics, pharmacokinetics, drug interactions and adverse effects. Lorcaserin Hydrochloride is chemically (R)-8-Chloro-1-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine hydrochloride. Lorcaserin HCl is a novel, synthetic, centrally-acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients. Headache, dizziness and nausea are the most common side effects associated with this drug. Lorcaserin HCl has two major metabolites, one conjugated with glucuronide called N-carbamoyl glucuronide which is excreted in urine and the second Lorcaserin N-sulfamate, which is circulated in the blood. Lorcaserin HCl is synthesized using four different schemes of which a six-step method that resulted in 92.3% yield with 99.8% of purity is employed for scale-up production. It is analyzed quantitatively in the plasma and brain tissue matrix of rats by Ultra Performance Liquid chromatographic (UPLC) method using MS-MS (Mass Spectrometric) detection.

scholarly journals A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates

2018 ◽  
Vol 10 (456) ◽  
pp. eaar3483 ◽  
Author(s):  
Huiping Ding ◽  
Norikazu Kiguchi ◽  
Dennis Yasuda ◽  
Pankaj R. Daga ◽  
Willma E. Polgar ◽  
...  
Keyword(s):  
Side Effects ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Nonhuman Primates ◽  
Mu Opioid Receptor ◽  
Mu Opioid ◽  
Opioid Receptor Agonist

scholarly journals MP1104, a mixed kappa-delta opioid receptor agonist has anti-cocaine properties with reduced side-effects in rats

2019 ◽  
Vol 150 ◽  
pp. 217-228 ◽  
Author(s):  
Diana V. Atigari ◽  
Rajendra Uprety ◽  
Gavril W. Pasternak ◽  
Susruta Majumdar ◽  
Bronwyn M. Kivell
Keyword(s):  
Side Effects ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Delta Opioid Receptor ◽  
Opioid Receptor Agonist

scholarly journals Buprenorphine C7‐Esters with Improved Nociceptin Receptor Agonist Potency as Analgesics

2019 ◽  
Vol 33 (S1) ◽  
Author(s):  
Keith Mathew Olson ◽  
Gerta Cami‐Kobeci ◽  
Stephen M. Husbands ◽  
John R. Traynor
Keyword(s):  
Receptor Agonist ◽  
Nociceptin Receptor

scholarly journals Retrospective Evaluation of the Use of Romiplostim after Hematopoietic Stem Cell Transplantation0

Blood ◽  
2019 ◽  
Vol 134 (Supplement_1) ◽  
pp. 5660-5660
Author(s):  
Elisabetta Xue ◽  
Tatiana Lawrence ◽  
Terry B. Gernsheimer ◽  
Filippo Milano
Keyword(s):  
Stem Cell ◽  
Platelet Count ◽  
Side Effects ◽  
Median Time ◽  
Research Funding ◽  
Receptor Agonist ◽  
Transfusion Requirement ◽  
Cell Transplant ◽  
Hematopoietic Stem ◽  
Allogeneic Hsct

Background Prolonged thrombocytopenia following hematopoietic stem cell transplant (HSCT) is a common complication associated with risks of major bleeding and high platelet transfusion requirements. Although not approved in the setting of post-HSCT thrombocytopenia, few case series have investigated the use of thrombopoietin (TPO)-receptor agonist romiplostim for patients receiving HSCT. Herein, we reviewed its use in the setting of HSCT at our Institution. Methods From January 2006 to December 2017, 4642 patients received a first HSCT. Of these patients, 2152 (46%) received an autologous HSCT (auto-HSCT) while 2490 (54%) received an allogeneic HSCT (allo-HSCT). Among the patients in the allo-HSCT group, 752 (30%) received a matched related HSCT, 1125 (45%) a matched unrelated HSCT, 278 (11%) a mismatch unrelated HSCT and 335 (13%) a cord blood HSCT. A reduced intensity conditioning regimen was used in 629 (25%) patients receiving an allogeneic HSCT. An adequate clinical response was considered as a reduction of transfusion requirement and a platelet count PLT ≥ 50*103 /µL. This research was approved by the Institutional Review Board (IRB). Results Seven patients (adults n=5, children n=2) received romiplostim for thrombocytopenia. Patients' characteristics are reported in Table 1. All but one (who had CLL-related ITP) received the drug while in remission for the underlying hematologic disease. Romiplostim was used in 6 patients after an allo-HSCT and in 1 after an auto-HCT. Among the allo-HSCT recipients, all 6 reached neutrophil engraftment at a median time of 19 days (range 14-28 days). Romiplostim was administered for ITP (n=2) and poor graft function (PGF, n=4), at a median time of 7.5 months (range 2 - 34 months), with a median of 16 administrations (range 3-18) per patient. All patients received romiplostim weekly, with a median initial and maximum dose of 1 µg/kg (range 1-3 µg/kg) and 9.5 µg/kg (range 3-10 µg/kg), respectively. For the 2 ITP cases, romiplostim was given as third line of therapy, after a lack of response to both high dose steroids and intravenous immunoglobulin. One patient responded to the treatment, achieving a platelet count ≥ 50*103/µL after 2 months, while the other patient did not show any improvement and the drug was discontinued after 3 months. All the 4 PGF cases were thought to be secondary to medications, with one patient also having acute graft versus host disease (GvHD) as possible cause. Romiplostim was given as first line of treatment in all the cases; median platelet counts at the time of starting the treatment was 21*103/µL (range 13-42*103/µL). One patient did not show any response after 4 months of treatment and was subsequently switched to another TPO receptor agonist. Three patients showed a clinical benefit: one patient achieved a stable platelet count ≥50*103/µL after one month, another patient had a partial response achieving transfusion-independence after 3.5 months, but with PLT counts remaining below 50*103/µL; the third patient had a transient increase in platelet counts with decreased transfusion requirement, but the response was lost after two weeks. Overall romiplostim was well tolerated, with no major side effects related to its administration. In two cases mild increase in reticulin stain (grading 0-1) was observed. The auto-HSCT patient receiving romiplostim had Hodgkin's Lymphoma and was diagnosed with recurrent ITP 7.5 years after HSCT, while in complete remission for the underlying disease; he received romiplostim as part of the ITP treatment, and responded to a combination of romiplostim and mycophenolate mofetil without reporting adverse events. Conclusion In our analysis, the use of romiplostim was limited to very few cases of HSCT. The retrospective nature of this study along with a very small and heterogeneous cohort does not allow us to draw any efficacy conclusions. However, our data suggest that romiplostim could be considered a safe option to treat prolonged thrombocytopenia after HSCT. Prospective, randomized clinical trials using TPO-receptor agonists for thrombocytopenia in HSCT are needed to determine efficacy and potential side effects. Disclosures Lawrence: Amgen Inc.: Employment, Equity Ownership. Gernsheimer:Dova pharmaceuticals: Consultancy; Novartis: Honoraria; Amgen: Consultancy, Honoraria; Rigel: Consultancy; Shionogi: Consultancy; Cellphire: Consultancy; Fuji film: Consultancy; Bioverativ: Consultancy. Milano:Amgen: Research Funding; ExCellThera: Research Funding. OffLabel Disclosure: We investigated the use of Romiplostim for thrombocytopenia after hematopoietic cell transplant.

Early clinical experience with subcutaneous GR43175 in acute migraine: An overview

Cephalalgia ◽  
1989 ◽  
Vol 9 (9_suppl) ◽  
pp. 73-77
Author(s):  
P Tfelt-Hansen ◽  
J Brand ◽  
P Dano ◽  
A Doenicke ◽  
LJ Findley ◽  
...  
Keyword(s):  
Side Effects ◽  
Clinical Experience ◽  
Receptor Agonist ◽  
Response Rates ◽  
Acute Migraine ◽  
Double Blind ◽  
Subcutaneous Injections ◽  
Early Clinical Experience ◽  
Dose Ranging ◽  
Blind Trials

In six European clinics 111 migraine patients were treated in a series of open dose-ranging studies with subcutaneous injections of 1 to 4 mg GR43175, a novel 5-HT1-like receptor agonist. Response rates after 20–30 min were dose related and rose from 33% with 1 mg to 96% with 4 mg GR43175. Side effects were minor and transient. These promising results warrant confirmation in placebo-controlled double-blind trials.

scholarly journals The Advantages and Disadvantages of Prokinetics

2021 ◽  
Vol 96 (6) ◽  
pp. 478-483
Author(s):  
Jeongkuk Seo ◽  
Kee Wook Jung
Keyword(s):  
Gastrointestinal Tract ◽  
Side Effects ◽  
Gastrointestinal Motility ◽  
Receptor Agonist ◽  
Serotonin Receptor ◽  
Human Gastrointestinal Tract ◽  
Cardiac Side Effects ◽  
Gastrointestinal Dysmotility ◽  
Advantages And Disadvantages ◽  
Selective Agents

Prokinetics are medications that enhance gastrointestinal contractility; they improve the symptoms of patients with delayed gastrointestinal motility. Prokinetics have conventionally been used to stimulate gastrointestinal propulsion and to treat symptoms correlated with motility problems, including gastroparesis and constipation. 5-Hydroxytryptamine receptor 4 (5-HT4) agonists, such as cisapride, very effectively increased human gastrointestinal tract motility. However, cisapride sometimes induced serious tachyarrhythmia; the drug was thus withdrawn from the market. Thereafter, many prokinetics have been developed to treat delayed gastrointestinal motility. However, some exhibit serious side-effects. Recently, a new, highly selective serotonin receptor agonist, prucalopride, has been introduced; there is as yet no evidence of serious cardiac side- effects. The drug has been approved by the Food and Drug Administration to treat chronic constipation. Thus, recently introduced, highly selective agents appear to show promise as treatments for gastrointestinal dysmotility; there seem to be no serious side-effects.

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