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Public Health At its core, Catherine Demery’s research  is about receptors and signaling pathways—how mu-opioid And because naloxone cannot reverse xylazine, the interventions that once worked for opioid overdoses And because naloxone only targets opioids, it cannot reverse xylazine. By displacing opioids from the mu-opioid receptor, it restores breathing within minutes. First responders describe revivals that don’t feel like revivals, as if the body is still trapped in a pharmacological

There, she chose to write a review on genetic variation in susceptibility to alcoholism and opioid addiction—a Returning to the Opioid Questions That Mattered Now, as a PhD candidate in the Traynor and Anand labs at the University of Michigan, Catherine is focused on the mechanisms of opioid-induced respiratory It’s rigorous pharmacology, but deeply tied to urgent public health needs. "I've always been really passionate and somewhat sensitive to people who struggle with opioid abuse.

While writing a literature review on opioid and alcohol addiction susceptibility, something shifted. Rather than treating opioid pharmacology as a purely theoretical exercise, she collaborates with harm-reduction This approach makes her models not just rigorous, but translational—bridging the gap between receptor pharmacology That personal loss transforms complex receptor pharmacology into something immediate and human. And GPCR pharmacology isn’t just an academic pursuit—it’s essential to understanding and responding to

Redefining Opioid Pharmacology Ben and his colleagues discovered that PAMs can dramatically increase the efficacy of existing opioids. .” – Ben Clements By combining chronic pain models with receptor-level pharmacology, Ben is bridging Beyond Acute Pain: Into the Chronic Unknown Opioids work well for acute pain. Chronic pain? Neuropathic conditions like neuromas often resist standard opioid treatments.

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid The current frontline approach for pain-management is the use of opioid analgesics. The primary analgesic target of opioids is the μ-opioid receptor (MOR). Knockout of PLCβ3, or pharmacological inhibition of its upstream regulators, Gβγ or Gq, ex vivo in periaqueductal could lead to identification of new non-MOR targets that would allow for lower dose utilization of opioid

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled develop drugs with less side effects, and tools to explore the ORs nature and function, various (poly)pharmacological

Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest The potentially low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor, because opioid drugs typically have a protonated amino group that contributes In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors from the perspective of the usefulness of computational studies to evaluate protonation-coupled opioid-receptor

Are you ready to truly understand how pharmacologists predict whole-body drug response from a single straight to it:   Why models are vital for translating lab data into clinical forecasts The 4 types of pharmacologic Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent activation of EGFR "Background Fentanyl is an opioid analgesic and is widely used

September 2022 To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from inactive conformation using molecular dynamic simulations "The δ-opioid receptor (DOR) is a critical

September 2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid only slight structural changes compared to morphine, exhibits inhibitory effect, and is used to treat opioid

Ben Clements   In Episode 166, Ben Clements dives into opioid pharmacology, GPCR-targeted PAMs, and how review walks us through the evolving clinical landscape of class B GPCRs—reminding us that precision pharmacology

Whether working on opioid withdrawal, addiction vulnerability, or chronic pain, GPCR-related signaling the core mediator  — demonstrating the reach of these signaling pathways beyond classical receptor pharmacology hitting a GPCR... and honestly, like with the trials, they were not really that sufficiently better than opioids pain. ___________ Keyword Cloud: RGS4 , GPCR data platform , GPCR training program , pain research , opioid

His work spans deep academic research, startup life, and the application of machine learning and pharmacology The company’s scientific approach relied on targeting GPCRs — specifically opioid receptors — using biased to bring a novel, safer class of pain therapeutics to patients — an urgent need in the midst of the opioid Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling Despite decades of progress in structural biology and pharmacology, predicting how  a GPCR will respond

Welcome Back, Discovery Drivers   Terry’s Corner is live, on-demand pharmacology built for drug discovery Dr.GPCR Updates Terry’s Corner is Live - Pharmacology at your fingertips Terry’s Corner is now open! Better pharmacology leads to better decisions—unlock it now with Terry’s Corner.

When pharmacologists misinterpret how an antagonist interacts with its receptor, the consequences ripple Terry Kenakin reframes one of pharmacology’s most foundational ideas: the difference between competitive Inside the Lesson: Antagonist Behavior by the Numbers Terry walks through both the pharmacologic and If you want to avoid costly misinterpretations and strengthen your pharmacology toolkit, Terry’s Corner Brief today  ➤   #GPCRantagonism #CompetitiveAntagonists #NonCompetitiveAntagonists #DoseResponseCurve #Pharmacology

In the newest foundational lesson from Terry Kenakin’s Pharmacology Vault , we unlock the visual language of pharmacology: dose-response curves . 👉 Discover why dose-response curves are the backbone of all pharmacology.

Terry's Corner - The Truth About Allosteric Displacement Allosteric binding isn’t just a twist in the pharmacology GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

Attrition rates in early pharmacology remain painfully high. The High Cost of Pharmacology Gaps Every experienced drug hunter knows this: validation isn’t the problem Terry puts it bluntly: “Once you have a molecule, everything boils down to pharmacology—hit, lead, candidate invaluable for mechanistic understanding—assay volume control, expression system contrasts, predictive pharmacology Corner Terry’s Corner  is a living, growing knowledge hub led by Terry Kenakin—a world authority in pharmacology

Recognizing, predicting, and leveraging these interactions is the essence of enzyme inhibition pharmacology This lesson reframes enzyme interaction not as background noise, but as a core pharmacological event. Clark , laid the foundation for today’s quantitative pharmacology. Enzyme Inhibition Pharmacology: Orthosteric vs. Pharmacology isn’t just about hitting the receptor—it’s about surviving the enzymes first.

Welcome to Terry’s Corner , where foundational pharmacology is demystified by someone who’s spent over In his newest lesson, “The Uniqueness of Pharmacology in Drug Discovery,” Terry Kenakin explains why pharmacology isn’t a clean-cut science—it’s a dynamic dialogue between molecule and system. You’ll uncover: Why pharmacology is the glue between chemistry and biology How to interpret drug behavior the story it’s telling. 👉 Start your journey with Terry’s foundational series Unlock "Unique Role of Pharmacology

Welcome back GPCR lovers, In pharmacology, the wrong interpretation of antagonist behavior can derail This week in Terry’s Corner , we go beyond the dose-response curves to explore the kinetic and pharmacologic edge by staying on top of the latest breakthroughs in allostery, biased signaling, and computational pharmacology Keywords: GPCR, drug discovery, pharmacology, antagonism, competitive, non-competitive, Terry's Corner excellence, drug development, pharmaceutical, scientific career Hashtags: #DrGPCR #GPCR #DrugDiscovery #Pharmacology

using the Hall allosteric cube The Allosteric Shift: When Receptors Become Something New In orthosteric pharmacology Function: Two Different Worlds One of the most common—and dangerous—mistakes in allosteric pharmacology When a PAM increases radioligand binding but suppresses functional response, it’s not broken pharmacology—it The takeaway:  what looks like pharmacology failure may be a systems problem . Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or

Terry's Corner - New Course on Pharmacologic Models The latest Terry’s Corner unlocks clinical forecasting in the full newsletter   Secure Your Access Now ➤ 🗣️ “Thank you for bringing this (Principles of Pharmacology

Terry Kenakin takes you on a captivating tour through the history of pharmacology : a journey that spans Whether you're stepping into pharmacology for the first time or rekindling your interest, this lesson Terry’s Corner, your essential launchpad into the world of therapeutic science Unlock "The History of Pharmacology

As Chief Matchmaker, I recently had the pleasure of speaking with Beth Fleck, Director of In Vitro Pharmacology Beth is also the hiring manager for their open Principal Scientist, In Vitro Pharmacology role posted Top candidates will have a solid foundation in GPCR pharmacology as well as some experience in drug discovery

August 2022 "Background and purpose: Misuse of opioids has greatly affected our society. One potential solution is to develop analgesics that act at targets other than opioid receptors. These can be used either as stand-alone therapeutics or to improve the safety profile of opioid drugs The aim of this study was to test this hypothesis pharmacologically by using potent and selective Gq/

October 2022 Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment The network pharmacology method was used to constructe the "herb-component-target" network, and elucidated

This study demonstrated the pharmacological properties and functions of PxOctβ3 in P. xylostella, thus

It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. Acta Pharmacol Sin   2019 , 40  (3), 324–335. https://doi.org/10.1038/s41401-018-0164-x . (8)         J Pharmacol Exp Ther   1996 , 278 (3), 989–999. (12)      Martín-Fontecha, M.; Angelina, A.; Rückert Pharmacological Evaluation of New Constituents of “Spice”: Synthetic Cannabinoids Based on Indole, Indazole 1,4-Dihydroquinoline-3-Carboxamide Derivatives as New CB2 Cannabinoid Receptors Agonists: Synthesis, Pharmacological