Clobenpropit: Difference between revisions

Clobenpropit
Clinical data
ATC code	None;
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name N'-[(4-chlorophenyl)methyl]-1-[3-(3H-imidazol-4-yl)propylsulfanyl]formamidine;
CAS Number	145231-45-4;
PubChem CID	2790;
IUPHAR/BPS	1223;
ChemSpider	2688;
UNII	RKU631JF4H;
ChEMBL	ChEMBL14690;
CompTox Dashboard (EPA)	DTXSID3043738 ;
Chemical and physical data
Formula	C14H17ClN4S
Molar mass	308.83 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl;

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Latest revision as of 01:31, 13 November 2022

Clobenpropit is a histamine H₃ receptor antagonist.^[1] It has neuroprotective effects via stimulation of GABA release in brain cells in vitro.^[2]

References[edit]

^ Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes". European Journal of Pharmacology. 567 (3): 206–210. doi:10.1016/j.ejphar.2007.04.032. PMID 17537431.
^ Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons". European Journal of Pharmacology. 563 (1–3): 117–123. doi:10.1016/j.ejphar.2007.01.069. PMID 17350613.

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

[pmid17537431-1] Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes". European Journal of Pharmacology. 567 (3): 206–210. doi:10.1016/j.ejphar.2007.04.032. PMID 17537431.

[2] Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons". European Journal of Pharmacology. 563 (1–3): 117–123. doi:10.1016/j.ejphar.2007.01.069. PMID 17350613.

[1]

[2]

@@ Line 1: / Line 1: @@
+{{short description|Chemical compound}}
 {{Drugbox
-| IUPAC_name               = ''N'''-[(4-chlorophenyl)methyl]-1-[3-(3''H''-imidazol-4-yl)propylsulfanyl]formamidine
+| IUPAC_name = ''N'''-[(4-chlorophenyl)methyl]-1-[3-(3''H''-imidazol-4-yl)propylsulfanyl]formamidine
-| image                    = Clobenpropit.svg
+| image = Clobenpropit.svg
-| CAS_number               = 145231-45-4
+<!--Clinical data-->
-| ATC_prefix               = none
+| tradename =
-| ATC_suffix               =
+| pregnancy_category =
-| PubChem                  = 2790
+| legal_US = IND
+| routes_of_administration =
+<!--Pharmacokinetic data-->
+| bioavailability =
+| metabolism =
+| elimination_half-life =
+| excretion =
+<!--Identifiers-->
+| CAS_number = 145231-45-4
+| UNII_Ref = {{fdacite|correct|FDA}}
+| UNII = RKU631JF4H
+| ATC_prefix = None
+| ATC_suffix =
+| PubChem = 2790
 | IUPHAR_ligand = 1223
-| ChemSpiderID             = 2688
+| ChemSpiderID = 2688
 | ChEMBL = 14690
-| C = 14 | H = 17 | Cl = 1 | N = 4 | S = 1
+<!--Chemical data-->
-| molecular_weight         = 308.83 g/mol
+| C=14 | H=17 | Cl=1 | N=4 | S=1
-| smiles                   = C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl
+| smiles = C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl
-| bioavailability          =
-| metabolism               =
-| elimination_half-life    =
-| excretion                =
-| pregnancy_category       =
-| legal_status             =
-| routes_of_administration =
 }}
-'''Clobenpropit''' is a [[histamine]] [[H3 antagonist|H<sub>3</sub> receptor]] [[receptor antagonist|antagonist]].<ref name="pmid17537431">{{cite journal |author=Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P |title=The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes |journal=Eur. J. Pharmacol. |volume=567 |issue=3 |pages=206–10 |year=2007 |pmid=17537431 |doi=10.1016/j.ejphar.2007.04.032}}</ref> It has [[neuroprotective]] effects via stimulation of [[GABA]] release in the brain.<ref>Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. ''European Journal of Pharmacology''. 2007 Jun 1;563(1-3):117-23. PMID 17350613</ref>
+'''Clobenpropit''' is a [[histamine]] [[H3 antagonist|H<sub>3</sub> receptor antagonist]].<ref name="pmid17537431">{{cite journal | vauthors = Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P | title = The human histamine H3 receptor couples to GIRK channels in ''Xenopus'' oocytes | journal = European Journal of Pharmacology | volume = 567 | issue = 3 | pages = 206–210 | year = 2007 | pmid = 17537431 | doi = 10.1016/j.ejphar.2007.04.032 }}</ref> It has [[neuroprotective]] effects via stimulation of [[GABA]] release in brain cells ''[[in vitro]]''.<ref>{{ cite journal | vauthors = Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z | title = The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons | journal = European Journal of Pharmacology | year = 2007 | volume = 563 | issue = 1–3 | pages = 117–123 | pmid = 17350613 | doi = 10.1016/j.ejphar.2007.01.069 }}</ref>
-== See also ==
-* [[H3 antagonist|H<sub>3</sub> receptor antagonist]]
 == References ==
-{{Reflist|2}}
+{{Reflist}}
 {{Histaminergics}}
@@ Line 34: / Line 41: @@
 [[Category:H3 receptor antagonists]]
 [[Category:Imidazoles]]
-[[Category:Organochlorides]]
+[[Category:Chloroarenes]]
-{{pharmacology-stub}}
+{{nervous-system-drug-stub}}
-[[pt:Clobenpropit]]