User profiles for Spyros P Nikas

Spyros P. Nikas

Research Associate Professor, Northeastern University
Verified email at northeastern.edu
Cited by 3440

Crystal structures of agonist-bound human cannabinoid receptor CB1

T Hua, K Vemuri, SP Nikas, RB Laprairie, Y Wu, L Qu… - Nature, 2017 - nature.com
The cannabinoid receptor 1 (CB 1 ) is the principal target of the psychoactive constituent of
marijuana, the partial agonist Δ 9 -tetrahydrocannabinol (Δ 9 -THC) 1 . Here we report two …

Synthon-based ligand discovery in virtual libraries of over 11 billion compounds

…, MK Jain, O Savych, DS Radchenko, SP Nikas… - Nature, 2022 - nature.com
Abstract Structure-based virtual ligand screening is emerging as a key paradigm for early drug
discovery owing to the availability of high-resolution target structures 1 , 2 , 3 – 4 and ultra-…

[PDF][PDF] Activation and signaling mechanism revealed by cannabinoid receptor-Gi complex structures

…, Y Wang, M Wu, L Shen, CA Brust, SP Nikas… - Cell, 2020 - cell.com
Human endocannabinoid systems modulate multiple physiological processes mainly through
the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low …

[HTML][HTML] Structural basis for activation of CB1 by an endocannabinoid analog

…, CM Suomivuori, AS Powers, L Ji, SP Nikas… - Nature …, 2023 - nature.com
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …

CB1 cannabinoid receptor ligands

GA Thakur, SP Nikas… - Mini reviews in medicinal …, 2005 - ingentaconnect.com
The CB1 receptor is expressed in the central nervous system and numerous other tissues
including heart, lung and uterus and has been recognized as an important therapeutic target …

Δ9-Tetrahydrocannabinol acts as a partial agonist/antagonist in mice

CA Paronis, SP Nikas, VG Shukla… - Behavioural …, 2012 - journals.lww.com
Δ 9-Tetrahydrocannabinol (THC) has been characterized as a partial agonist at cannabinoid
CB1 receptors in vitro; however, it often produces the same maximum effects in vivo as …

[PDF][PDF] Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects

G Godlewski, SO Alapafuja, S Bátkai, SP Nikas… - Chemistry & biology, 2010 - cell.com
The enzyme fatty acid amide hydrolase (FAAH) catalyzes the in vivo degradation of the
endocannabinoid anandamide, thus controlling its action at receptors. A novel FAAH inhibitor, …

Novel 1′, 1′-chain substituted hexahydrocannabinols: 9β-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 …

SP Nikas, SO Alapafuja, I Papanastasiou… - Journal of medicinal …, 2010 - ACS Publications
In pursuit of a more detailed understanding of the structural requirements for the key side
chain cannabinoid pharmacophore, we have extended our SAR to cover a variety of …

Fluorescent probes for G-protein-coupled receptor drug discovery

…, RN Kulkarni, A Makriyannis, SP Nikas - Expert Opinion on …, 2018 - Taylor & Francis
Introduction: G-protein-coupled receptors (GPCRs) mediate the effects of approximately 33%
of all marketed drugs. The development of tools to study GPCR pharmacology is urgently …

Cannabinoid CB2 agonist AM1710 differentially suppresses distinct pathological pain states and attenuates morphine tolerance and withdrawal

…, AC Thomaz, LM Carey, Y Liu, SP Nikas… - Molecular …, 2019 - ASPET
AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a
cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced …