Davis M

References (5)

Title : Subacute pyridostigmine exposure increases heart rate recovery and cardiac parasympathetic tone in rats - Bharadwaj_2017_Clin.Exp.Pharmacol.Physiol_44_872
Author(s) : Bharadwaj M , Pope C , Davis M , Katz S , Cook C , Maxwell L
Ref : Clinical & Experimental Pharmacology & Physiology , 44 :872 , 2017
Abstract : Heart rate recovery (HRR) describes the rapid deceleration of heart rate after strenuous exercise and is an indicator of parasympathetic tone. A reduction in parasympathetic tone occurs in patients with congestive heart failure, resulting in prolonged HRR. Acetylcholinesterase inhibitors, such as pyridostigmine, can enhance parasympathetic tone by increasing cholinergic input to the heart. The objective of this study was to develop a rodent model of HRR to test the hypothesis that subacute pyridostigmine administration decreases cholinesterase activity and accelerates HRR in rats. Ten days after implantation of radiotelemetry transmitters, male Sprague Dawley rats were randomized to control (CTL) or treated (PYR; 0.14 mg/mL pyridostigmine in the drinking water, 29 days) groups. Rats were exercised on a treadmill to record HRR, and blood samples were collected on days 0, 7, 14, and 28 of pyridostigmine administration. Total cholinesterase and acetylcholinesterase (AChE) activity in plasma was decreased by 32%-43% and 57%-80%, respectively, in PYR rats on days 7-28, while plasma butyrylcholinesterase activity did not significantly change. AChE activity in red blood cells was markedly reduced by 64%-66%. HRR recorded 1 minute after exercise was higher in the PYR group on days 7, 14 and 28, and on day 7 when HRR was estimated at 3 and 5 minutes. Autonomic tone was evaluated pharmacologically using sequential administration of muscarinic (atropine) and adrenergic (propranolol) blockers. Parasympathetic tone was increased in PYR rats as compared with the CTL group. These data support the study hypothesis that subacute pyridostigmine administration enhances HRR by increasing cardiac parasympathetic tone.
ESTHER : Bharadwaj_2017_Clin.Exp.Pharmacol.Physiol_44_872
PubMedSearch : Bharadwaj_2017_Clin.Exp.Pharmacol.Physiol_44_872
PubMedID: 28440910

Title : A suspected case of intermediate syndrome in a dog with carbamate toxicosis - Tinson_2017_Aust.Vet.J_95_201
Author(s) : Tinson E , Boller E , Davis M
Ref : Australian Veterinary Journal , 95 :201 , 2017
Abstract : CASE REPORT: A 7-year-old female spayed Labrador Retriever was managed for suspected carbamate toxicosis after confirmed ingestion of a large amount of methiocarb. Therapy included decontamination, supportive care and management for aspiration pneumonia. On the third day of hospitalisation, after an initial clinical improvement, the dog developed respiratory muscle weakness, inspiratory dyspnoea and pronounced cervical muscle weakness. These delayed clinical signs were consistent with the 'intermediate syndrome' described in some cases of organophosphate and carbamate toxicoses in humans and also described in one case of organophosphate toxicosis in the dog. Intermediate syndrome has not been reported in carbamate toxicosis in the dog. CONCLUSION: This case report highlights the necessity for veterinarians to monitor for additional complications not commonly considered in acute carbamate toxicoses.
ESTHER : Tinson_2017_Aust.Vet.J_95_201
PubMedSearch : Tinson_2017_Aust.Vet.J_95_201
PubMedID: 28555948

Title : Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2\/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence - Dhanya_2014_J.Med.Chem_57_4154
Author(s) : Dhanya RP , Sheffler DJ , Dahl R , Davis M , Lee PS , Yang L , Nickols HH , Cho HP , Smith LH , D'Souza MS , Conn PJ , Der-Avakian A , Markou A , Cosford ND
Ref : Journal of Medicinal Chemistry , 57 :4154 , 2014
Abstract : As part of our ongoing small-molecule metabotropic glutamate (mGlu) receptor positive allosteric modulator (PAM) research, we performed structure-activity relationship (SAR) studies around a series of group II mGlu PAMs. Initial analogues exhibited weak activity as mGlu2 receptor PAMs and no activity at mGlu3. Compound optimization led to the identification of potent mGlu2/3 selective PAMs with no in vitro activity at mGlu1,4-8 or 45 other CNS receptors. In vitro pharmacological characterization of representative compound 44 indicated agonist-PAM activity toward mGlu2 and PAM activity at mGlu3. The most potent mGlu2/3 PAMs were characterized in assays predictive of ADME/T and pharmacokinetic (PK) properties, allowing the discovery of systemically active mGlu2/3 PAMs. On the basis of its overall profile, compound 74 was selected for behavioral studies and was shown to dose-dependently decrease cocaine self-administration in rats after intraperitoneal administration. These mGlu2/3 receptor PAMs have significant potential as small molecule tools for investigating group II mGlu pharmacology.
ESTHER : Dhanya_2014_J.Med.Chem_57_4154
PubMedSearch : Dhanya_2014_J.Med.Chem_57_4154
PubMedID: 24735492

Title : Two Novel Mutations in ABHD12: Expansion of the Mutation Spectrum in PHARC and Assessment of Their Functional Effects - Chen_2013_Hum.Mutat_34_1672
Author(s) : Chen DH , Naydenov A , Blankman JL , Mefford HC , Davis M , Sul Y , Barloon AS , Bonkowski E , Wolff J , Matsushita M , Smith C , Cravatt BF , Mackie K , Raskind WH , Stella N , Bird TD
Ref : Hum Mutat , 34 :1672 , 2013
Abstract : PHARC (polyneuropathy, hearing loss, ataxia, retinitis pigmentosa, and cataracts) is a recently described autosomal-recessive neurodegenerative disease caused by mutations in the alpha-beta-hydrolase domain-containing 12 gene (ABHD12). Only five homozygous ABHD12 mutations have been reported and the pathogenesis of PHARC remains unclear. We evaluated a woman who manifested short stature as well as the typical features of PHARC. Sequence analysis of ABHD12 revealed a novel heterozygous c.1129A>T (p.Lys377*) mutation. Targeted comparative genomic hybridization detected a 59-kb deletion that encompasses exon 1 of ABHD12 and exons 1-4 of an adjacent gene, GINS1, and includes the promoters of both genes. The heterozygous deletion was also carried by the patient's asymptomatic mother. Quantitative reverse transcription-PCR demonstrated approximately 50% decreased expression of ABHD12 RNA in lymphoblastoid cell lines from both individuals. Activity-based protein profiling of serine hydrolases revealed absence of ABHD12 hydrolase activity in the patient and 50% reduction in her mother. This is the first report of compound heterozygosity in PHARC and the first study to describe how a mutation might affect ABHD12 expression and function. The possible involvement of haploinsufficiency for GINS1, a DNA replication complex protein, in the short stature of the patient and her mother requires further studies.
ESTHER : Chen_2013_Hum.Mutat_34_1672
PubMedSearch : Chen_2013_Hum.Mutat_34_1672
PubMedID: 24027063
Gene_locus related to this paper: human-ABHD12

Title : Letter: Replacement drug for edrophonium bromide -
Author(s) : Jones CR , Davis M
Ref : Med J Aust , 2 :650 , 1975
PubMedID: 1207545