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}}
-{{Chembox new
+{{Drugbox
-|ImageFile=
+| IUPAC_name = ''N'''-[(4-chlorophenyl)methyl]-1-[3-(3''H''-imidazol-4-yl)propylsulfanyl]formamidine
-|ImageSize=
+| image = Clobenpropit.svg
-|IUPACName=N'-[(4-chlorophenyl)methyl]-1-[3-(3H-imidazol-4-yl)propylthio]formamidine
-|OtherNames=
+<!--Clinical data-->
-|Section1= {{Chembox Identifiers
+| tradename =
-|  CASNo=
+| pregnancy_category =
-|  PubChem=2790
+| legal_US = IND
-|  SMILES=C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl
+| routes_of_administration =
-  }}
-|Section2= {{Chembox Properties
+<!--Pharmacokinetic data-->
-|  Formula=C<sub>14</sub>H<sub>17</sub>ClN<sub>4</sub>S
+| bioavailability =
-|  MolarMass=308.82958
+| metabolism =
-|  Appearance=
+| elimination_half-life =
-|  Density=
+| excretion =
-|  MeltingPt=
-|  BoilingPt=
+<!--Identifiers-->
-|  Solubility=
+| CAS_number = 145231-45-4
-  }}
+| UNII_Ref = {{fdacite|correct|FDA}}
-|Section3= {{Chembox Hazards
+| UNII = RKU631JF4H
-|  MainHazards=
+| ATC_prefix = None
-|  FlashPt=
+| ATC_suffix =
-|  Autoignition=
+| PubChem = 2790
-  }}
+| IUPHAR_ligand = 1223
+| ChemSpiderID = 2688
+| ChEMBL = 14690
+<!--Chemical data-->
+| C=14 | H=17 | Cl=1 | N=4 | S=1
+| smiles = C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl
 }}
-'''Clobenpropit''' is a [[H3 antagonist|histamine H<sub>3</sub> 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>
-==References==
+== References ==
 {{Reflist}}
+{{Histaminergics}}
-{{biochem-stub}}
-{{pharma-stub}}
-{{Histamine antagonist}}
 [[Category:H3 receptor antagonists]]
+[[Category:Imidazoles]]
+[[Category:Chloroarenes]]
+{{nervous-system-drug-stub}}