Spiradoline
Encyclopedia
Spiradoline is a drug which acts as a highly selective κ-opioid
agonist
. It has analgesic
, diuretic
and antitussive effects, and produces subjective effects in animals similar to those of ketocyclazocine and allylnormetazocine
. The main effect in humans is sedation
, along with analgesic and diuretic effects, but significant side effects such as dysphoria
and hallucinations have stopped it from being used clinically. Kappa-agonists have been shown to react negatively with the Mu-receptor, instead of having an assumed synergy since they are both opiate receptors, such as with the Mu and Delta receptors(which both mediate pain-relief, euphoria(mainly Mu) and overall potency of Opiate/Opioid effects).
Kappa Opioid receptor
The κ-opioid receptor is a protein that in humans is encoded by the OPRK1 gene. The κ-opioid receptor is one of five related receptors that bind opium-like compounds in the brain and are responsible for mediating the effects of these compounds...
agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
. It has analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
, diuretic
Diuretic
A diuretic provides a means of forced diuresis which elevates the rate of urination. There are several categories of diuretics. All diuretics increase the excretion of water from bodies, although each class does so in a distinct way.- Medical uses :...
and antitussive effects, and produces subjective effects in animals similar to those of ketocyclazocine and allylnormetazocine
Allylnormetazocine
Alazocine , or -N-allylnormetazocine , was the first drug discovered to act as a σ1 receptor agonist . It has no significant affinity for the σ2 receptor. Alazocine also acts as a κ-opioid receptor agonist , and to a much lesser extent, as an NMDA receptor antagonist ....
. The main effect in humans is sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
, along with analgesic and diuretic effects, but significant side effects such as dysphoria
Dysphoria
Dysphoria is medically recognized as a mental and emotional condition in which a person experiences intense feelings of depression, discontent and indifference to the world around them.Mood disorders can induce dysphoria, often with a heightened risk of suicide, especially in...
and hallucinations have stopped it from being used clinically. Kappa-agonists have been shown to react negatively with the Mu-receptor, instead of having an assumed synergy since they are both opiate receptors, such as with the Mu and Delta receptors(which both mediate pain-relief, euphoria(mainly Mu) and overall potency of Opiate/Opioid effects).