Results 11 to 20 of about 195,829 (332)

PARTIAL AGONISTS IN RECEPTOR THEORY

open access: hybridBehavioural Pharmacology, 1998
A. M. Young
openalex   +3 more sources

Case Report: Functional and Symptomatic Improvement With Cariprazine in Various Psychiatric Patients: A Case Series

open access: yesFrontiers in Psychiatry, 2022
Cariprazine is a third-generation antipsychotic medication approved for the treatment of schizophrenia and bipolar disorder, with unique pharmacodynamic and pharmacokinetic properties.
Tommaso Vannucchi   +2 more
doaj   +1 more source

Partial agonists in schizophrenia [PDF]

open access: yesBritish Journal of Psychiatry, 2005
The editorial by Bolonna & Kerwin ([2005][1]) is both timely and important. The authors succinctly present the case for the use of partial agonists of dopamine receptors, concluding that ‘the reviewed evidence suggests a promising future for dopamine receptor partial agonists’.
A. H. Young, David A. Cousins
openaire   +1 more source

MPL Adjuvant Contains Competitive Antagonists of Human TLR4

open access: yesFrontiers in Immunology, 2020
Monophosphoryl lipid A (MPL®) is the first non-alum vaccine adjuvant to achieve widespread clinical and market acceptance, a remarkable achievement given that it is manufactured from a Salmonella enterica endotoxin.
Yi-Qi Wang   +4 more
doaj   +1 more source

Thiazolidinediones Are Partial Agonists for the Glucocorticoid Receptor [PDF]

open access: yesEndocrinology, 2008
Although thiazolidinediones were designed as specific peroxisome proliferator-activated receptor (PPAR)-γ-ligands, there is evidence for some off-target effects mediated by a non-PPARγ mechanism. Previously we have shown that rosiglitazone has antiinflammatory actions not explicable by activation of PPARγ,but possibly by the glucocorticoid receptor (GR)
Matthews L.   +5 more
openaire   +6 more sources

Quantal Ca2+ release mediated by very few IP3 receptors that rapidly inactivate allows graded responses to IP3

open access: yesCell Reports, 2021
Summary: Inositol 1,4,5-trisphosphate receptors (IP3Rs) are intracellular Ca2+ channels that link extracellular stimuli to Ca2+ signals. Ca2+ release from intracellular stores is “quantal”: low IP3 concentrations rapidly release a fraction of the stores.
Ana M. Rossi   +5 more
doaj   +1 more source

Pindolol‐the pharmacology of a partial agonist. [PDF]

open access: yesBritish Journal of Clinical Pharmacology, 1982
1 Pindolol is a non‐selective beta‐adrenoceptor blocking agent; its affinity to adrenoceptors in guinea pig atria (beta 1) is not significantly different from that in guinea pig trachea (beta 1 + beta 2) and canine vascular smooth muscle (beta 2). 2 Pindolol displays a striking diversity of agonist activities in isolated tissues.
K Menninger, B J Clark, A Bertholet
openaire   +3 more sources

Design of κ-Opioid Receptor Agonists for the Development of Potential Treatments of Pain with Reduced Side Effects

open access: yesMolecules, 2023
The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for the development of pain medications, without deleterious side effects associated with the μ-opioid receptor (MOR).
Federica Santino, Luca Gentilucci
doaj   +1 more source

Functional Stoichiometry at the Nicotinic Receptor. The Photon Cross Section for Phase 1 Corresponds to Two Bis-Q Molecules per Channel [PDF]

open access: yes, 1982
These experiments examine changes in the agonist-induced conductance that occur when the agonist-receptor complex is perturbed. Voltage-clamped Electrophorus electroplaques are exposed to the photoisomerizable agonist trans-Bis-Q A 1-µs laser flash ...
Lester, Henry A., Sheridan, Robert E.
core   +1 more source

Agonists and Partial Agonists of Rhodopsin:  Retinals with Ring Modifications [PDF]

open access: yesBiochemistry, 2005
Activation of the visual pigment rhodopsin is initiated by isomerization of its retinal chromophore to the all-trans geometry, which drives the conformation of the protein to the active state. We have examined by FTIR spectroscopy the impact of a series of modifications at the ring of retinal on the activation process and on molecular interactions ...
Vogel, Reiner   +4 more
openaire   +4 more sources

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