Nalorphine

 ( Abandoned Drugs ) 

Nalorphine (; also known as N-allylnormorphine; brand names Lethidrone and Nalline) is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties.

It was introduced in 1954

Anil Aggrawal9788177394412, Avichal Publishing Company. . ISBN 9788177394412

and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence.

Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine ( N-allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963. Due to potent activation of the κ-opioid receptor, nalorphine produces such as dysphoria, anxiety, confusion, and , and for this reason, is no longer used medically.

---

Pharmacology

---

Pharmacodynamics Nalorphine acts at two — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (K_i = 1.6 nM; EC₅₀ = 483 nM; E_max = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics.

---

Chemistry

---

Analogues Nalorphine has a number of analogues including niconalorphine (the nicomorphine analogue), diacetylnalorphine (heroin analogue), dihydronalorphine (dihydromorphine), and a number of others as well as a number of codeine-based analogues.

(2013). 9781489905857, Springer Science & Business Media. . ISBN 9781489905857

---

Synthesis More recently, it has become much more commonplace to use ethyl chloroformate instead of cyanogen bromide for the Von Braun degradation demethylation step. See for example the list of phenyltropanes or the synthesis of paroxetine for further examples of this.

---

See also

• Diacetylnalorphine
• Levallorphan
• Nalbuphine
• Nalorphine dinicotinate

Post Comment