hyperthermia

Dantrolene 是一种肌肉松弛剂，是人红细胞谷胱甘肽还原酶的非竞争性抑制剂，其Ki 和IC50值分别为 111.6 μM 和 52.3 μM。它是兰尼碱受体拮抗剂及Ca2+信号稳定剂。它可用于研究恶性高热、亨廷顿病、肌肉痉挛和其他神经阻滞剂恶性综合征。

rac-BHFF ((R,S)-BHFF) 是具有口服活性的 GABAB 受体的异构增强剂，有抗焦虑活性。

Modaline sulfate 是一种 MAO 抑制剂，用于研究抑郁症。

SR59230A 是可透过血脑屏障的、选择性的 β3-肾上腺素能受体拮抗剂，对 β3，β1 和 β2 受体的 IC50分别为 40、408 和 648 nM。

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

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

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

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.

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].

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.

PL-017 TFA 是高效、选择性的 μ 阿片受体(μopioid receptor)激动剂，具有 5.5 nM 对125I-FK 33,824 与 μ 位点结合的 IC50 值。该化合物在大鼠中展现出持久且可逆的缓解疼痛效果。