Diberal Explained

Diberal, also known as 5-(1,3-Dimethylbutyl)-5-ethylbarbituric acid or DMBB, is an atypical barbiturate. This compound can be either convulsant or anticonvulsant depending on which enantiomer is used.

Pharmacology

Diberal, unlike most barbiturates, can have convulsant actions. This is uncommon, as barbiturates typically enhance the function of GABA as allorestic modulators and agonists (at higher doses),[1] therefore having anticonvulsant properties. Depending on which isomer is used, it can have either convulsant or anticonvulsant actions.

The different pharmacological profile between isomers is thought to be due to the differences in the formation of hydrogen bonds at the binding sites.[2]

(+)-Isomer

(+)-DMBB is the atypical enantiomer of diberal. It is atypical in the means that it has convulsant action, unlike most barbiturate drugs.[3]

(−)-Isomer

Unlike (+)-DMBB, the (−)-isomer is similar to most barbiturates by having anticonvulsant action. It has been found that administration of (−)-DMBB reverses the convulsant actions of (+)-DMBB. (−)-DMBB is slightly more potent than pentobarbital in its depressant properties.[4]

See also

Notes and References

  1. Book: Suddock JT, Kent KJ, Regina AC, Cain MD . https://www.ncbi.nlm.nih.gov/books/NBK499875/ . 29763050 . 2024 . Barbiturate Toxicity . StatPearls . Treasure Island (FL) . StatPearls Publishing .
  2. Ho IK, Harris RA . Mechanism of action of barbiturates . Annual Review of Pharmacology and Toxicology . 21 . 83–111 . 1981 . 6263177 . 10.1146/annurev.pa.21.040181.000503 .
  3. Desai R, Savechenkov PY, Zolkowska D, Ge RL, Rogawski MA, Bruzik KS, Forman SA, Raines DE, Miller KW . Contrasting actions of a convulsant barbiturate and its anticonvulsant enantiomer on the α1 β3 γ2L GABAA receptor account for their in vivo effects . The Journal of Physiology . 593 . 22 . 4943–4961 . November 2015 . 26378885 . 4650410 . 10.1113/JP270971 .
  4. Downes H, Perry RS, Ostlund RE, Karler R . A study of the excitatory effects of barbiturates . The Journal of Pharmacology and Experimental Therapeutics . 175 . 3 . 692–699 . December 1970 . 5489924 .