Muskarinski acetilholinski receptor M1

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Muskarinski acetilholinski receptor M1‎‎
Identifikatori
Simboli CHRM1; HM1; M1; M1R; MGC30125
Vanjski ID OMIM118510 MGI88396 HomoloGene20189 IUPHAR: M1 GeneCards: CHRM1 Gene
Ortolozi
Vrsta Čovek Miš
Entrez 1128 12669
Ensembl ENSG00000168539 ENSMUSG00000032773
UniProt P11229 Q52KQ0
RefSeq (mRNA) NM_000738 NM_007698
RefSeq (protein) NP_000729 NP_031724
Lokacija (UCSC) Chr 11:
62.68 - 62.69 Mb
Chr 19:
8.74 - 8.76 Mb
PubMed pretraga [1] [2]

Muskarinski acetilholinski receptor M1 (holinergički receptor, muskarinski 1) je muskarinski receptor.

Za ovaj receptor je nađeno da posreduje spori ekscitatorni postsinaptički potencijal u ganglionima postganglionskim nervima.[1] On je visoko zastupljen u eksokrinim žlezdama i u CNS-u.[2][3]

On se predominantno vezuje za Gq klasu G proteina,[4] koja stimuliše dejstvo fosfolipaze C i stoga inozitol trisfosfata i signalnog puta intracelularnog kalcijuma.

Efekti[uredi - уреди]

Mehanizam[uredi - уреди]

On formira spregu sa Gq, i u manjoj meri Gi i Gs. To dovodi do sporog EPSP i umanjene K+ provodnosti.[6][7]

Ligandi[uredi - уреди]

Agonisti

Alosterni modulatori

  • benzilhinolon karboksilna kiselina[8]
  • VU-0090157[9]
  • VU-0029767[9]

Antagonisti

Gen[uredi - уреди]

Ovaj receptor je kodiran humanim genom CHRM1.[5] On se nalazi na 11q13.[5]

Reference[uredi - уреди]

  1. Messer, Jr, WS (20. 1. 2000.). "Acetylcholine". University of Toledo. http://www.neurosci.pharm.utoledo.edu/MBC3320/acetylcholine.htm. pristupljeno 27. 10. 2007.. 
  2. Johnson, Gordon (2002). PDQ Pharmacology (2nd izd.). Hamilton, Ontario: BC Decker Inc. str. 311 pages. ISBN 1-55009-109-3. 
  3. Richelson, Elliott (2000). "Cholinergic Transduction, Psychopharmacology - The Fourth Generation of Progress". American College of Neuropsychopharmacology. http://www.acnp.org/g4/GN401000011/Default.htm. pristupljeno 27. 10. 2007.. 
  4. Burford NT, Nahorski SR (1996). "Muscarinic m1 receptor-stimulated adenylate cyclase activity in Chinese hamster ovary cells is mediated by Gs alpha and is not a consequence of phosphoinositidase C activation". Biochem. J. 315 (Pt 3): 883–8. PMC 1217289. PMID 8645172. 
  5. 5.0 5.1 5.2 5.3 "Entrez Gene: CHRM1 cholinergic receptor, muscarinic 1". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1128. 
  6. 6.0 6.1 6.2 6.3 6.4 6.5 6.6 6.7 6.8 6.9 Rang HP, Dale MM, Ritter JM, Moore PK (2003). "10". Pharmacology (5th izd.). Elsevier Churchill Livingstone. str. 139. ISBN 0-443-07145-4. 
  7. Uchimura N, North RA (1. 3. 1990.). "Muscarine reduces inwardly rectifying potassium conductance in rat nucleus accumbens neurones". J. Physiol. (Lond.) 422 (1): 369–80. PMC 1190137. PMID 1693682. 
  8. Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ (November 2009). "A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning". J. Neurosci. 29 (45): 14271–86. doi:10.1523/JNEUROSCI.3930-09.2009. PMC 2811323. PMID 19906975. 
  9. 9.0 9.1 Marlo JE, Niswender CM, Days EL, et al. (2008). "Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity". Mol. Pharmacol. 75 (3): 577–88. doi:10.1124/mol.108.052886. PMC 2684909. PMID 19047481. 

Literatura[uredi - уреди]

  • Rang HP, Dale MM, Ritter JM, Moore PK (2003). "10". Pharmacology (5th izd.). Elsevier Churchill Livingstone. str. 139. ISBN 0-443-07145-4. 
  • Johnson, Gordon (2002). PDQ Pharmacology (2nd izd.). Hamilton, Ontario: BC Decker Inc. str. 311 pages. ISBN 1-55009-109-3. 

Vidi još[uredi - уреди]