21416-53-5 Usage
Description
Picrotin, a natural picrotoxane, is a compound that primarily functions as a glycine receptor (GlyR) antagonist. It is found in the plant-derived poison picrotoxin, where it coexists with picrotoxinin in equimolar concentrations. Picrotin selectively targets and inhibits α1, α2, and α3 homodimeric GlyRs, with IC50s of 57 and 117 μM for α1 and α2 homodimeric GlyRs, respectively. Notably, it does not exhibit any significant activity in inhibiting γ-aminobutyric acid (GABA) type A and type C receptors.
Uses
Used in Pharmaceutical Industry:
Picrotin is used as a GABAa receptor antagonist for its ability to selectively target and inhibit glycine receptors. This property makes it a valuable compound in the development of drugs aimed at modulating the activity of these receptors, which can be beneficial in treating various neurological and psychiatric disorders.
Used in Research and Development:
In the field of research, Picrotin is utilized as a tool to study the function and role of glycine receptors in the central nervous system. Its selective inhibition of GlyRs allows scientists to better understand the underlying mechanisms of these receptors and their potential involvement in different pathological conditions.
Used in Neuropharmacology:
Picrotin is employed as a research compound in neuropharmacology to investigate the interactions between glycine receptors and other neurotransmitter systems, such as GABA receptors. This knowledge can contribute to the development of novel therapeutic strategies for conditions like epilepsy, where both GlyRs and GABA receptors play crucial roles in regulating neuronal excitability.
Check Digit Verification of cas no
The CAS Registry Mumber 21416-53-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,1,4,1 and 6 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 21416-53:
(7*2)+(6*1)+(5*4)+(4*1)+(3*6)+(2*5)+(1*3)=75
75 % 10 = 5
So 21416-53-5 is a valid CAS Registry Number.
InChI:InChI=1/C15H18O7/c1-12(2,18)6-7-10(16)20-8(6)9-13(3)14(7,19)4-5-15(13,22-5)11(17)21-9/h5-9,18-19H,4H2,1-3H3/t5-,6+,7-,8-,9-,13-,14-,15+/m1/s1
21416-53-5Relevant articles and documents
Total synthesis of picrotin
Corey,Pearce
, p. 1823 - 1824 (1980)
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Stereoselective Total Synthesis of (-)-Picrotoxnin and (-)-Picrotin
Miyashita, Masaaki,Suzuki, Toshio,Yoshikoshi, Akira
, p. 3728 - 3734 (2007/10/02)
The stereoselective total synthesis of (-)-picritoxnin (1) and (-)-picrotin (2), starting from (+)-5β-hydroxycarvone (3), is described.Eight contiguous asymmetric centers on a cis-fused hydrindane ring system were stereoselectively prepared via three key