Compound 21 is a potent designer drug with full agonist activity toward human hM3Dq (EC50 = 1.7 nM by cell-based Ca2+ mobilization assay), a human M3 muscarinic receptor (M3R)-based Gq (M3Dq) DREADD (Designer Receptors Exclusively Activated by Designer Drugs), displaying little activity toward muscarinic acetylcholine receptor M3 (30% M3 activation at 10 μM) and reduced affinity toward H1, 5HT2A, 5HT2C, α1A receptor (fold selectivity = 3.5, 40, 100, 165, respectively). Note: the DREADD hM3Dq exhibits M3 biological activity, but is insensitive to the endogenous ligand acetylcholine (ACh).
Potent designer drug with selective agonist activity for human M3Dq (hM3Dq) DREADD (Designer Receptors Exclusively Activated by Designer Drugs).
ACS chemical neuroscience, 6(3), 476-484 (2015-01-15)
Over the past decade, two independent technologies have emerged and been widely adopted by the neuroscience community for remotely controlling neuronal activity: optogenetics which utilize engineered channelrhodopsin and other opsins, and chemogenetics which utilize engineered G protein-coupled receptors (Designer Receptors
Neurogenesis and differentiation of neural stem cells (NSCs) are controlled by cell-intrinsic molecular pathways that interact with extrinsic signaling cues. In this study, we identify a circuit that regulates neurogenesis and cell proliferation in the lateral ventricle-subventricular zone (LV-SVZ). Our
The Journal of neuroscience : the official journal of the Society for Neuroscience, 43(28), 5221-5240 (2023-06-21)
Thermoregulatory behavior in homeothermic animals is an innate behavior to defend body core temperature from environmental thermal challenges in coordination with autonomous thermoregulatory responses. In contrast to the progress in understanding the central mechanisms of autonomous thermoregulation, those of behavioral
The bidirectional controller of the thermoregulatory center in the preoptic area (POA) is unknown. Using rats, here, we identify prostaglandin EP3 receptor-expressing POA neurons (POAEP3R neurons) as a pivotal bidirectional controller in the central thermoregulatory mechanism. POAEP3R neurons are activated
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