Cyclazodone: Difference between revisions

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==Pharmacology==

Cyclazodone is a more potent N-cyclopropyl derivative of [[pemoline]]. Pemoline is considered to be [[dopamine|dopaminergic]], yet its precise mechanism of action remained ~~elusive~~ during its market ~~presence~~.<ref>"Cylert (Pemoline)" (PDF). FDA. December 2002.</ref>

Cyclazodone is a more potent N-cyclopropyl derivative of [[pemoline]], and 4 to 5 times more potent than [[thozalinone]]. Pemoline is considered to be [[dopamine|dopaminergic]], yet its precise mechanism of action remained unclear during its time on the market.<ref>"Cylert (Pemoline)" (PDF). FDA. December 2002.</ref>

Pemoline's mild sympathomimetic side effects and weaker anorectic effects suggest limited affinity for [[noradrenaline]] and potentially [[serotonin]] receptors compared to other central nervous system stimulants. This characteristic appears to be shared with cyclazodone, as demonstrated by the limited sympathomimetic effects observed in dogs following administration, , evidenced by limited sympathomimetic effects observed in dogs following administration.

Pemoline's mild sympathomimetic side effects and weaker anorectic effects suggest limited affinity for [[noradrenaline]] and potentially [[serotonin]] receptors compared to other central nervous system stimulants. This characteristic appears to be shared with cyclazodone, as demonstrated by the limited sympathomimetic effects observed in dogs following administration, evidenced by limited sympathomimetic effects observed in dogs following administration.

According to the patent filed by the inventors, cyclazodone demonstrated significant central nervous system stimulation and antidepressant properties, and relative potency greater than both pemoline and various other N-lower-alkyl-substituted pemoline derivatives. At the time cyclazodone also offered a much more favorable therapeutic index and margin of safety than pemoline and other N-lower-alkyl-substituted pemoline derivatives.<ref name="GuidicelliPatent">{{Citation | vauthors=((Guidicelli, D. P. R. L.)), ((Najer, H.)) | title=5-phenyl-2-cyclopropylamino-4-oxazolinone, and process for making the same | url=https://patents.google.com/patent/US3609159A/en}}</ref>

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===Pharmacodynamics===

Cyclazodone is an [[amphetamine]]-like [[agonist]] of the Trace Amine Associated Receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as [[dopamine]], [[serotonin]] and [[noradrenaline]].<ref>{{cite journal | vauthors=((Miller, G. M.)) | journal=Journal of neurochemistry | title=The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | volume=116 | issue=2 | pages=164–176 | date= January 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/ | issn=0022-3042 | doi=10.1111/j.1471-4159.2010.07109.x}}</ref><ref>{{Citation | title=Amphetamine | url=https://go.drugbank.com/drugs#targets}}</ref><ref>TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364</ref> The agonism of this set of receptors results in the release of increased concentrations of [[dopamine]], [[serotonin]] and [[noradrenaline]] in the [[synaptic cleft]]. This leads to [[Thought acceleration|cognitive]] and [[Stimulation|physical stimulation]] within the user.

Cyclazodone is thought to be an [[amphetamine]]-like [[agonist]] of the Trace Amine Associated Receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as [[dopamine]], [[serotonin]] and [[noradrenaline]].<ref>{{cite journal | vauthors=((Miller, G. M.)) | journal=Journal of neurochemistry | title=The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | volume=116 | issue=2 | pages=164–176 | date= January 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/ | issn=0022-3042 | doi=10.1111/j.1471-4159.2010.07109.x}}</ref><ref>{{Citation | title=Amphetamine | url=https://go.drugbank.com/drugs#targets}}</ref><ref>TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364</ref> The agonism of this set of receptors results in the release of increased concentrations of [[dopamine]], [[serotonin]] and [[noradrenaline]] in the [[synaptic cleft]]. This leads to [[Thought acceleration|cognitive]] and [[Stimulation|physical stimulation]] within the user.

==Subjective effects==

@@ Line 17: / Line 17: @@
 ==Pharmacology==
-Cyclazodone is a more potent N-cyclopropyl derivative of [[pemoline]]. Pemoline is considered to be [[dopamine|dopaminergic]], yet its precise mechanism of action remained elusive during its market presence.<ref>"Cylert (Pemoline)" (PDF). FDA. December 2002.</ref>
+Cyclazodone is a more potent N-cyclopropyl derivative of [[pemoline]], and 4 to 5 times more potent than [[thozalinone]]. Pemoline is considered to be [[dopamine|dopaminergic]], yet its precise mechanism of action remained unclear during its time on the market.<ref>"Cylert (Pemoline)" (PDF). FDA. December 2002.</ref>
-Pemoline's mild sympathomimetic side effects and weaker anorectic effects suggest limited affinity for [[noradrenaline]] and potentially [[serotonin]] receptors compared to other central nervous system stimulants. This characteristic appears to be shared with cyclazodone, as demonstrated by the limited sympathomimetic effects observed in dogs following administration, , evidenced by limited sympathomimetic effects observed in dogs following administration.
+Pemoline's mild sympathomimetic side effects and weaker anorectic effects suggest limited affinity for [[noradrenaline]] and potentially [[serotonin]] receptors compared to other central nervous system stimulants. This characteristic appears to be shared with cyclazodone, as demonstrated by the limited sympathomimetic effects observed in dogs following administration, evidenced by limited sympathomimetic effects observed in dogs following administration.
 According to the patent filed by the inventors, cyclazodone demonstrated significant central nervous system stimulation and antidepressant properties, and relative potency greater than both pemoline and various other N-lower-alkyl-substituted pemoline derivatives. At the time cyclazodone also offered a much more favorable therapeutic index and margin of safety than pemoline and other N-lower-alkyl-substituted pemoline derivatives.<ref name="GuidicelliPatent">{{Citation | vauthors=((Guidicelli, D. P. R. L.)), ((Najer, H.)) | title=5-phenyl-2-cyclopropylamino-4-oxazolinone, and process for making the same | url=https://patents.google.com/patent/US3609159A/en}}</ref>
@@ Line 28: / Line 28: @@
 ===Pharmacodynamics===
-Cyclazodone is an [[amphetamine]]-like [[agonist]] of the Trace Amine Associated Receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as [[dopamine]], [[serotonin]] and [[noradrenaline]].<ref>{{cite journal | vauthors=((Miller, G. M.)) | journal=Journal of neurochemistry | title=The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | volume=116 | issue=2 | pages=164–176 | date= January 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/ | issn=0022-3042 | doi=10.1111/j.1471-4159.2010.07109.x}}</ref><ref>{{Citation | title=Amphetamine | url=https://go.drugbank.com/drugs#targets}}</ref><ref>TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364</ref> The agonism of this set of receptors results in the release of increased concentrations of [[dopamine]], [[serotonin]] and [[noradrenaline]] in the [[synaptic cleft]]. This leads to [[Thought acceleration|cognitive]] and [[Stimulation|physical stimulation]] within the user.
+Cyclazodone is thought to be an [[amphetamine]]-like [[agonist]] of the Trace Amine Associated Receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as [[dopamine]], [[serotonin]] and [[noradrenaline]].<ref>{{cite journal | vauthors=((Miller, G. M.)) | journal=Journal of neurochemistry | title=The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | volume=116 | issue=2 | pages=164–176 | date= January 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/ | issn=0022-3042 | doi=10.1111/j.1471-4159.2010.07109.x}}</ref><ref>{{Citation | title=Amphetamine | url=https://go.drugbank.com/drugs#targets}}</ref><ref>TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364</ref> The agonism of this set of receptors results in the release of increased concentrations of [[dopamine]], [[serotonin]] and [[noradrenaline]] in the [[synaptic cleft]]. This leads to [[Thought acceleration|cognitive]] and [[Stimulation|physical stimulation]] within the user.
 ==Subjective effects==