5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced swim test in mice. It increases time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at doses ranging from 30 to 50 mg/kg. 5α-Androst-16-en-3α-ol protects against seizures induced by pentylenetetrazole or electroshock in mice (ED50s = 48.9 and 21.9 mg/kg, respectively).
1.Brooksbank, B.W., Brown, R., and Gustafsson, J.A.The detection of 5α-androst-16-en-3α-ol in human male axillary sweatExperientia30(8)864-865(1974) 2.Kaminski, R.M., Marini, H., Ortinski, P.I., et al.The pheromone androstenol (5α-androst-16-en-3α-ol) is a neurosteroid positive modulator of GABAA receptorsJ. Pharmacol. Exp. Ther.317(2)694-703(2006)
Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide (T0267) is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml)in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons,zonisamide (1-1,000 μM)inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide (T0267)inhibits H. pylori recombinant carbonic anhydrase (CA)and the human CA isoforms I,II,and V with Ki values of 218,56,35,and 21 nM,respectively.4,5 In mice,it has anticonvulsant activity against maximal electroshock seizure (MES)and pentylenetetrazole-induced maximal,but not minimal,seizures (ED50s = 19.6,9.3,and >500 mg/kg,respectively). Zonisamide (T0267) (40 mg/kg,p.o.)prevents MPTP-induced decreases in the levels of dopamine ,but not homovanillic acid or dihydroxyphenyl acetic acid ,and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy.
2-(Isopentylamino)naphthalene-1,4-dione is a vitamin K analog.1It inhibits spasms induced by pentylenetetrazole and tonic hindlimb extension induced by maximal electroshock (MES) in mice (ED50s = 349.2 and 108.1 mg/kg, respectively). It also protects mice against seizures in the 6 Hz psychomotor seizure test (ED50s = 152.7 and 263.7 mg/kg at stimulus intensities of 32 and 44 mA, respectively).
1.Li, X., Himes, R.A., Prosser, L.C., et al.Discovery of the first vitamin K analogue as a potential treatment of pharmacoresistant seizuresJ. Med. Chem.63(11)5865-5878(2020)
Phenytoin-D10 is a deuterated isotope-labelled phenytoin for isotope tracing. Phenytoin (T0939)acts as a voltage-gated Na⁺ channel blocker and t-type Ca²⁺ channel inhibitor,exhibiting antiepileptic activity.
Methazolamide-D6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide (T0106) is a carbonic anhydrase inhibitor. It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide (T0106)reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg/kg. It also inhibits production of reactive oxygen species (ROS)in a primary cortical neuron (PCN)cellular model of subarachnoid hemorrhage (SAH)and reduces cerebral edema in a mouse model of SAH.3 Methazolamide (T0106) is larvicidal,with a 50% larvicidal concentration (LC50)value of 724 ppm,but has no activity when administered in the diet to adult A. aegypti. Formulations containing methazolamide have been used in the treatment of glaucoma.