hyperthermia

Dantrolene is a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

BCTP is a polymodal inhibitor of TRPV1. It has a reduced liability for hyperthermia.

Selective μ opioid receptor agonist (IC50 values are 5.5 and > 10000 nM for inhibition of 125I-FK 33,824 and 125I-DADLE binding to μ and δ sites respectively). Produces naloxone-reversible analgesia, catalepsy and hyperthermia following central administra

Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 |Gavva et al (2007) The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J.Neurosci. 27 3366 PMID:17392452

Modaline was a 2-methyl-3-piperidinopyrazine derivative found to inhibit monoamine oxidase (MAO) and showed a curative effect for the anti-depressant. Similar to other MAO inhibitors, it enhanced convulsions induced by tryptamine and hyperthermia induced

rac-BHFF ((R,S)-BHFF) is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). It exhibits anxiolytic activity in vivo and is orally active.

Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits basal activity of mGluR5. Fenobam reduces stress-induced hyperthermia, exhibits anxiolytic-like activity, and may induce analgesia.

2-Aminotetralin acts as a neuromodulatory agent by inhibiting serotonin (5-HT) and norepinephrine reuptake in the rat brain at a dose of 39.4 mg/kg. It triggers hypothermia in rats through intracisternal or intraperitoneal injection, while the implantation of crystals in the hypothalamus' medial preoptic area leads to hyperthermia. Additionally, it mimics (+)-amphetamine in a two-lever drug discrimination test among rats in a dose-dependent manner.

CBiPES, a potent mGlu2 positive allosteric modulator with an EC50 value of 92.8 nM, attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity, and can be used for research of neurological diseases [1] [2].

SR59230A is a potent, selective antagonist of β3-adrenergic receptor(β3, β1, and β2 receptors with IC50s of 40, 408, and 648 nM , respectively).