Results 41 to 50 of about 38,061 (191)

Histamine H1‐receptor‐mediated modulation of NMDA receptors signaling responses

Pharmacology Research & Perspectives
This study attempted to clarify the role of histamine H1 receptors in epilepsy by exploring the effects of agonists and inverse agonists on the rundown of the current induced by iterative applications of NMDA or GABA in primary neuronal culture ...
J.‐M. Arrang, V. Armand
doaj   +1 more source

Non-canonical Opioid Signaling Inhibits Itch Transmission in the Spinal Cord of Mice

Cell Reports, 2018
Summary: Chronic itch or pruritus is a debilitating disorder that is refractory to conventional anti-histamine treatment. Kappa opioid receptor (KOR) agonists have been used to treat chronic itch, but the underlying mechanism remains elusive.
Admire Munanairi, Xian-Yu Liu, Devin M. Barry, Qianyi Yang, Jun-Bin Yin, Hua Jin, Hui Li, Qing-Tao Meng, Jia-Hang Peng, Zhen-Yu Wu, Jun Yin, Xuan-Yi Zhou, Li Wan, Ping Mo, Seungil Kim, Fu-Quan Huo, Joseph Jeffry, Yun-Qing Li, Rita Bardoni, Michael R. Bruchas, Zhou-Feng Chen   +20 more
doaj   +1 more source

Signal transduction mechanism of biased ligands at histamine H2 receptors [PDF]

, 2014
7TMRs (seven-transmembrane receptors) exist as conformational collections in which different conformations would lead to differential downstream behaviours such as receptor phosphorylation, G-protein activation and receptor internalization.
Alonso, Natalia, Davio, Carlos Alberto, Echeverría, Emiliana Beatriz, Fernández, Natalia Brenda, Monczor, Federico, Shayo, Carina Claudia   +5 more
core   +1 more source

Therapeutic potential of histamine H3 receptor agonists and antagonists

Trends in Pharmacological Sciences, 1998
The histamine H3 receptor was discovered 15 years ago, and many potent and selective H3 receptor agonists and antagonists have since been developed. Currently, much attention is being focused on the therapeutic potential of H3 receptor ligands. In this review, Rob Leurs, Patrizio Blandina, Clark Tedford and Henk Timmerman describe the available H3 ...
R. LEURS, BLANDINA, PATRIZIO, C. TEDFORD, H. TIMMERMAN   +3 more
openaire   +5 more sources

FFAR1 activation attenuates histamine-induced myosin light chain phosphorylation and cortical tension development in human airway smooth muscle cells

Respiratory Research, 2020
Background Activation of free fatty acid receptors (FFAR1 and FFAR4) which are G protein-coupled receptors (GPCRs) with established (patho)physiological roles in a variety of obesity-related disorders, induce human airway smooth muscle (HASM) cell ...
Shengjie Xu, Anthony Schwab, Nikhil Karmacharya, Gaoyuan Cao, Joanna Woo, Nicholas Kim, Steven S. An, Reynold A. Panettieri Jr, Joseph A. Jude   +8 more
doaj   +1 more source

Physiological implications of biased signaling at histamine H2 receptors [PDF]

, 2015
Histamine mediates numerous functions acting through its four receptor subtypes all belonging to the large family of seven transmembrane G-protein coupled receptors. In particular, histamine H2 receptor (H2R) is mainly involved in gastric acid production,
Carina Shayo, Carlos A. Davio, Carlos D. Zappia, Federico Monczor, Maia Cabrera, Natalia Alonso, Natalia C. Fernández   +6 more
core   +1 more source

Selective histamine H2 receptor agonists alleviate blood-brain barrier disruption by promoting the expression of vascular protective factors following traumatic brain injury in mice

Journal of Pharmacological Sciences, 2022
Histamine is a major neurotransmitter and alleviates neuronal damage after ischemic injury via H2 receptors. Herein, we investigated the effects of H2 receptor agonists on the blood-brain barrier (BBB) disruption after traumatic brain injury (TBI).
Shotaro Michinaga, Kiyomi Sonoda, Naoki Inazuki, Manae Ezaki, Hiroki Awane, Kahori Shimizu, Shigeru Hishinuma, Hiroyuki Mizuguchi   +7 more
doaj   +1 more source

Selective inhibition of histamine-evoked Ca2+ signals by compartmentalized cAMP in human bronchial airway smooth muscle cells. [PDF]

, 2018
Intracellular Ca2+ and cAMP typically cause opposing effects on airway smooth muscle contraction. Receptors that stimulate these pathways are therapeutic targets in asthma and chronic obstructive pulmonary disease.
Dale, Philippa, Dowling, Mark R, Head, Victoria, Taylor, Colin W   +3 more
core   +1 more source

Prodrugs Activated by Vascular Ectopeptidases: Proof of Concept

Medical Sciences Forum, 2022
Several vascular ectopeptidases reside in blood vessels and efficiently regulate peptide hormones. For instance, bradykinin (BK) is inactivated by angiotensin converting enzyme (ACE) or arginine-carboxypeptidases (Arg-CPs), and aminopeptidase N (APN ...
François Marceau
doaj   +1 more source

Sites of action of sleep and wake drugs: insights from model organisms [PDF]

, 2013
Small molecules have been used since antiquity to regulate our sleep. Despite the explosion of diverse drugs to treat problems of too much or too little sleep, the detailed mechanisms of action and especially the neuronal targets by which these compounds
Rihel, J, Schier, AF
core   +1 more source